K Waisser

Summary

Affiliation: Charles University
Country: Czech Republic

Publications

  1. ncbi request reprint [Where does the development of new antituberculotics aim at?]
    Karel Waisser
    Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové, Heyrovskeho 1203, 500 05 Hradec Kralove, Česká Republika
    Ceska Slov Farm 61:150-8. 2012
  2. ncbi request reprint High active potential antimycobacterial agents against Mycobacterium avium
    Waisser Karel
    Charles University, Prague, Czech Republic
    Ceska Slov Farm 61:127-9. 2012
  3. ncbi request reprint [Derivatives of phenylcarbamic acid as potential antituberculotics]
    Karel Waisser
    Farmaceutická fakulta Univerzity Karlovy Heyrovského 1025, 500 05 Hradec Kralove
    Ceska Slov Farm 61:17-20. 2012
  4. ncbi request reprint Antimycobacterial 3-aryl-2H-1,3-benzoxazine-2,4(3H)-diones
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Pharmazie 58:83-94. 2003
  5. ncbi request reprint Relationship between the structure and antimycobacterial activity of substituted salicylanilides
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Heyrovskeho 1203, CZ 500 05 Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 336:53-71. 2003
  6. ncbi request reprint [New groups of potential antitubercular agents: 3-(4-ethoxythiocarbonylphenyl)-2-H-benzoxazin-2,4(3H)-diones and 3-(4-ethoxythiocarbonylphenyl)-4-thioxy-2H-benzoxazin-2(3H)-ones]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 52:42-7. 2003
  7. ncbi request reprint [Advances in the development of antitubercular agents containing no heterocyclics in the pharmacophore. Part 1. Derivatives of carboxylic acid]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 52:73-81. 2003
  8. ncbi request reprint The oriented development of antituberculotics: salicylanilides
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy, Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 339:616-20. 2006
  9. ncbi request reprint Antimycobacterial and antifungal isosters of salicylamides
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 336:322-35. 2003
  10. ncbi request reprint 3-Benzyl-2H-1,3-benzoxazine-2,4(3H)-diones, a new group of antimycobacterial compounds against potentially pathogenic strains
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hcyrovsky Str 1203, 50005 Hradec Kralove, Czech Republic
    Farmaco 58:1137-49. 2003

Collaborators

Detail Information

Publications56

  1. ncbi request reprint [Where does the development of new antituberculotics aim at?]
    Karel Waisser
    Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové, Heyrovskeho 1203, 500 05 Hradec Kralove, Česká Republika
    Ceska Slov Farm 61:150-8. 2012
    ..It is a selection from almost three thousand reports aiming to help our scientists. The article presents topical information which may be of interest to several pharmaceutical professions...
  2. ncbi request reprint High active potential antimycobacterial agents against Mycobacterium avium
    Waisser Karel
    Charles University, Prague, Czech Republic
    Ceska Slov Farm 61:127-9. 2012
    ..The activity against M. avium was poor. It can be concluded that a new group of compounds with an excellent activity against M. avium has been found...
  3. ncbi request reprint [Derivatives of phenylcarbamic acid as potential antituberculotics]
    Karel Waisser
    Farmaceutická fakulta Univerzity Karlovy Heyrovského 1025, 500 05 Hradec Kralove
    Ceska Slov Farm 61:17-20. 2012
    ..avium and M. kansasii. The carbamates produced by Prof. Vinsová and co-workers published in the last year show that carbamates can be still topical...
  4. ncbi request reprint Antimycobacterial 3-aryl-2H-1,3-benzoxazine-2,4(3H)-diones
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Pharmazie 58:83-94. 2003
    ..The activity of the compounds increases with increasing hydrophobicity and electron-withdrawing properties of the substituents on the phenyl ring, whereas the effect of the substituents on the benzoxazine ring seems to be more complex...
  5. ncbi request reprint Relationship between the structure and antimycobacterial activity of substituted salicylanilides
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Heyrovskeho 1203, CZ 500 05 Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 336:53-71. 2003
    ..The relationships between the antimycobacterial activity and physico-chemical parameters of all substituents were also explored. The quadratic representation of lipophilicity parameters did not lead to significant correlations...
  6. ncbi request reprint [New groups of potential antitubercular agents: 3-(4-ethoxythiocarbonylphenyl)-2-H-benzoxazin-2,4(3H)-diones and 3-(4-ethoxythiocarbonylphenyl)-4-thioxy-2H-benzoxazin-2(3H)-ones]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 52:42-7. 2003
    ....
  7. ncbi request reprint [Advances in the development of antitubercular agents containing no heterocyclics in the pharmacophore. Part 1. Derivatives of carboxylic acid]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 52:73-81. 2003
    ..The communication includes papers published after 1980 in order to link up with a review paper devoted to the same topic published in the present series in 1982...
  8. ncbi request reprint The oriented development of antituberculotics: salicylanilides
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy, Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 339:616-20. 2006
    ..The Free-Wilson method was used to evaluate structure-antimycobacterial activity relationships. 4-Chloro-N-(4-propylphenyl)salicylamide and 5-chloro-N-(4-propylphenyl)salicylamide were selected for preclinical studies...
  9. ncbi request reprint Antimycobacterial and antifungal isosters of salicylamides
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 336:322-35. 2003
    ..gypseum were analyzed by the Free-Wilson method. An increase in antimycobacterial activity was observed only for the sulfanylbenzoic acid derivatives, especially those with the benzyl moiety. The antifungal activity was not significant...
  10. ncbi request reprint 3-Benzyl-2H-1,3-benzoxazine-2,4(3H)-diones, a new group of antimycobacterial compounds against potentially pathogenic strains
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hcyrovsky Str 1203, 50005 Hradec Kralove, Czech Republic
    Farmaco 58:1137-49. 2003
    ..The antimycobacterial activity of N-benzylsalicylamides correlates with that of 3-benzyl-2H-1,3-benzoxazin-2,4(3H)-diones and depends on the partition coefficients and electronic indexes...
  11. ncbi request reprint [A new group of potential antitubercular agents: antimycobacterial N-benzylsalicylamides]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 52:291-4. 2003
    ..The obtained data were analyzed by Free-Wilson method in comparison with their isosteric analogues of 3-hydroxypicolinic and 2-sulfanylbenzoic acids described in the previous communication...
  12. ncbi request reprint New antimycobacterial 2,3-dihydro-1-alkylindole-2-thiones
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czechia
    Folia Microbiol (Praha) 51:25-6. 2006
    ..avium. 2,3-Dihydro-1-methyl-2-thioxoindole-3-one and 2,3-dihydro-1-butyl-2-thioxoindole-3-one were the most active substances against potentially pathogenic strains, being more active than isoniazide...
  13. ncbi request reprint New antimycobacterial S-alkylisothiosemicarbazones
    K Waisser
    Department of Inorganic and Organic Chemistry, Charles University, Faculty of Pharmacy, Hradec Kralove, Czechia
    Folia Microbiol (Praha) 50:479-81. 2005
    ..kansasii, M. fortuitum, two strains of M. intracellulare and three strains of M. avium. Quinoline-4-carbaldehyde-S-hexyl-isothiohydrazone was found to be more active against potentially pathogenic strains than isoniazide...
  14. ncbi request reprint [Advances in the development of antitubercular agents containing no heterocyclic compounds in the pharmacophore. Part 2. Other derivatives except carboxylic acids]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 53:124-30. 2004
    ..The communication records papers published since 1980 because it intends to link up with a review paper published in 1982 (Ceskoslov. Farm., 1982; 31, 353-360)...
  15. ncbi request reprint Antimycobacterial N-pyridinylsalicylamides, isosters of salicylamides
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovsky Strasse 1203, Hradec Kralove 50005, Czech Republic
    Farmaco 59:615-25. 2004
    ..5-chloro-pyridin-2-yl, and the substitution of the salicyl moiety by chlorine in position 4 or 5 had the strongest influence on the increase in antimycobacterial activity...
  16. ncbi request reprint [Advances in the development of new antitubercular agents from a group of ortho-condensed heterocyclic compounds. Part 1. Compounds containing one heteroatom per six-membered ring]
    K Waisser
    Katedra anorganické a organické chemie, Farmaceutické fakulty, Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 50:159-65. 2001
    ..Polycyclic systems make it possible to widely model the structures, and therefore the present review paper can inspire a search for new structures of antimycobacterial agents...
  17. ncbi request reprint In vitro antifungal activity of 3-phenyl-2H-benzoxazine-2,4(3H)-diones
    K Waisser
    Department of Inorganic and Organic Chemistry, Charles University, Faculty of Pharmacy, 500 05 Hradec Kralove, Czechia
    Folia Microbiol (Praha) 47:488-92. 2002
    ..In vitro antifungal activity becomes higher with increasing electron-accepting ability of the substituents on the phenyl ring, and with increasing lipophilicity...
  18. ncbi request reprint 1-Aryl-5-benzylsulfanyltetrazoles, a new group of antimycobacterial compounds against potentially pathogenic strains
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czechia
    Folia Microbiol (Praha) 50:195-7. 2005
    ..kansasii. We tried to use the Hansch approach, the Free-Wilson approach and their combination for structure-activity correlation but the calculations were statistically insignificant...
  19. ncbi request reprint New groups of antimycobacterial agents: 6-chloro-3-phenyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 6-chloro-3-phenyl-2H-1,3-benzoxazine-2,4(3H)-dithiones
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 500 05, Hradec Kralove, Czech Republic
    Eur J Med Chem 35:733-41. 2000
    ..tuberculosis and M. kansasii. The Free-Wilson method and procedure developed by the authors were used to analyse the structure-activity and structure-antimycobacterial profile relationships, respectively...
  20. ncbi request reprint [Antimicrobial salicylanilides and 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy
    Ceska Slov Farm 50:148-52. 2001
    ..As the values of regression coefficients were not substantially changed after the complementation of the group, the present authors consider the problem under study to be solved...
  21. ncbi request reprint A note to the biological activity of benzoxazine derivatives containing the thioxo group
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Heyrovský Str 1203, 50005 Hradec Kralove, Czech Republic
    Eur J Med Chem 45:2719-25. 2010
    ..The most active derivatives were more active than isonicotinhydrazide (INH). The cytotoxicity and the antiproliferative activity were studied as well...
  22. ncbi request reprint [Advances in the development of new antitubercular agents from a group of orthocondensed heterocyclic compounds. Part 2. Substances containing more nitrogen atoms in the 6-membered ring]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 50:211-8. 2001
    ..Current Awareness in Biomedicine is, however, a very imperfect literature search source, recording only a fraction of communications...
  23. ncbi request reprint Influence of the replacement of the oxo function with the thioxo group on the antimycobacterial activity of 3-aryl-6,8-dichloro-2H-1,3-benzoxazine-2,4(3H)-diones and 3-arylquinazoline-2,4(1H,3H)-diones
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Farmaco 56:803-7. 2001
    ..4(3H)-diones and 3-arylquinazoline-2,4(1H,3H)-diones gave rise to an increase of antimycobacterial activity. The most active compound was 3-(3-chlorophenyl)-6,8-dichloro-2H-1,3-benzoxazine-2,4(3H)-dithione...
  24. ncbi request reprint [Advances in the development of new antitubercular agents from orthocondensed heterocyclic compounds. Part 3. Substances containing several types of heteroatoms in the six-membered ring]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 50:267-73. 2001
    ..Review papers about five-membered heterocyclic antituberculotic ortho-condensed compounds was published in the present journal in 1999...
  25. ncbi request reprint Highly active potential antituberculotics: 3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 3-(4-alkylphenyl)-2H-1,3-benzoxazine-2,4(3H)-dihiones substituted in ring-B by halogen
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 341:800-3. 2008
    ..The replacement of the oxo group by thioxo group of 3-(4-alkylphenyl)-2H-1,3-benzoxazine-2,4(3H)-diones often led to an improvement in the antimycobacterial activity against M. tuberculosis...
  26. ncbi request reprint [Antimycobacterial effects of pyrrolidinoethylester alkoxysubstituted phenylcarbamic acids]
    K Waisser
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 51:140-4. 2002
    ..Their effect increases with the length of the alkyl chain in the alkoxy group bound to the phenyl. The influence of the position of the alkoxyl chain on the phenyl is not too marked, but it seems to decrease in the series m-, p-, o-...
  27. ncbi request reprint The oriented development of antituberculotics (Part II): halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones
    Karel Waisser
    Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Heyrovskeho, Czech Republic
    Arch Pharm (Weinheim) 340:264-7. 2007
    ..6-Bromo-3-(4-butylphenyl)-1,3-benzoxazine-2,4-(3H)-dione 3b proved to be the most active compound of the series...
  28. ncbi request reprint Hybrid molecules of estrone: new compounds with potential antibacterial, antifungal, and antiproliferative activities
    J Adamec
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, Hradec Kralove, 500 05, Czech Republic
    Bioorg Med Chem 15:2898-906. 2007
    ..e., the hybrid molecules with estrone, tetrazole-5-thiols, and 5-benzylsulfanyl-1-phenyltetrazoles) with the same substituents on phenyl ring were compared. Amongst them, the 5-benzylsulfanyl-1-phenyltetrazoles were the most potent...
  29. ncbi request reprint Antimycobacterial activity of basic ethyl esters of alkoxy-substituted phenylcarbamic acids
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 500 05 Hradec Kralove, Czechia
    Folia Microbiol (Praha) 48:45-50. 2003
    ..The p- and m-substituted derivatives were more active than the o-substituted ones. Direct relationship between the structure of the basic substituents and the activity was not found...
  30. ncbi request reprint QSAR study of antimycobacterial activity of quaternary ammonium salts of piperidinylethyl esters of alkoxysubstituted phenylcarbamic acids
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czechia
    Folia Microbiol (Praha) 51:21-4. 2006
    ..The activity increased with the increasing lipophilicity of the compounds...
  31. ncbi request reprint Antimycobacterial activity of piperidinylpropyl esters of alkoxy-substituted phenylcarbamic acids
    K Waisser
    Department of Inorganic and Organic Chemistry, Charles University, Faculty of Pharmacy, 500 05 Hradec Kralove, Czechia
    Folia Microbiol (Praha) 48:585-7. 2003
    ..The change of ethyl to propyl moiety increases the activity to M. tuberculosis but decreases the antimycobacterial activity to all potentially pathogenic strains under study...
  32. ncbi request reprint Quinazoline derivatives with antitubercular activity
    J Kunes
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Farmaco 55:725-9. 2000
    ..4-(S-Butylthio)quinazoline (3c) was even more active than isoniazide against atypical strains of mycobacteria...
  33. ncbi request reprint A new group of potential antituberculotics: hydrochlorides of piperidinylalkyl esters of alkoxy-substituted phenylcarbamic acids
    K Waisser
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 500 05 Hradec Kralove, Czechia
    Folia Microbiol (Praha) 49:265-8. 2004
    ..tuberculosis, a similar substitution by ethoxymethyl increased the activity against M. kansasii. The most active compounds were piperidinyl-1-(ethoxymethyl)ethylesters of heptoxyphenylcarbamic acids...
  34. doi request reprint New S-benzylisothiosemicarbazones with antimycobacterial activity
    E Petrlíková
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, 500 05, Hradec Kralove, Czech Republic
    Folia Microbiol (Praha) 56:10-2. 2011
    ..Benzaldehyde-S-4-bromobenzylisothiosemicarbazone and salicylaldehyde-S-4-chlorobenzylisothiosemicarbazone have the most promising antimycobacterial properties...
  35. ncbi request reprint New pyridine derivatives as potential antimicrobial agents
    V Klimesova
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Farmaco 54:666-72. 1999
    ..The most active compound was 2-cyanomethylthiopyridine-4-carbonitrile (7) with MIC against Mycobacterium kansasii in the range of 8-4 mumol/l. The antifungal activities of the compounds were relatively low...
  36. doi request reprint N-benzylsalicylthioamides: highly active potential antituberculotics
    Rafael Dolezal
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 342:113-9. 2009
    ..The most active compounds are more active than isoniazid (INH) and are active against INH-resistant potential pathogenic strains of mycobacterium...
  37. ncbi request reprint Evaluation of in vitro antifungal activity of N-benzylsalicylamide derivatives
    P Kubanová
    Department of Biological and Medical Sciences, Faculty of Pharmacy, Charles University, 500 05 Hradec Kralove, Czechia
    Folia Microbiol (Praha) 48:346-50. 2003
    ..The most efficient derivatives had MIC < or = 7.8 mumol/L against T. mentagrophytes. Regression analysis suggested an indirect relationship between MIC values and lipophilicity (log P)...
  38. ncbi request reprint QSAR analysis of salicylamide isosteres with the use of quantum chemical molecular descriptors
    R Dolezal
    Department of Inorganic and Organic Chemistry, Charles University, Heyrovskeho 1203, Hradec Kralove 50003, Czech Republic
    Eur J Med Chem 44:869-76. 2009
    ..92; q(2)=0.89), and somewhat less good QSAR models were found for Mycobacterium avium (r(2)=0.84; q(2)=0.78) and Mycobacterium kansasii (r(2)=0.80; q(2)=0.56). All QSAR models were cross-validated using the leave-10-out procedure...
  39. ncbi request reprint 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring
    M Pour
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Bioorg Med Chem Lett 10:1893-5. 2000
    ..25 micromol/L). In terms of microg/mL, the substance was more active (7.6 microg/mL) than this standard antifungal drug (16.6 microg/mL)...
  40. ncbi request reprint Synthesis and antimycobacterial activity of pyridylmethylsulfanyl and naphthylmethylsulfanyl derivatives of benzazoles, 1, 2, 4-triazole, and pyridine-2-carbothioamide/-2-carbonitrile
    Lenka Zahajská
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 337:549-55. 2004
    ..The most active substances were 4-(3-pyridylmethylsulfanyl)pyridine-2-carbothioamide (7b) (MIC = 2 - >62.5 micromol/L) and 4-(1-naphthylmethylsulfanyl)pyridine-2-carbothioamide (7d) (MIC = 2 - >32 micromol/L)...
  41. ncbi request reprint Heterocyclic benzazole derivatives with antimycobacterial in vitro activity
    Jan Kocí
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 50005 Hradec Kralove, Czech Republic
    Bioorg Med Chem Lett 12:3275-8. 2002
    ..The most active compounds were subjected to the toxicity assay and were evaluated as moderately cytotoxic...
  42. ncbi request reprint Biological activity of 2-hydroxythiobenzanilides and related compounds
    L Kubicova
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Kralove, Charles University, Prague, Czech Republic
    Cent Eur J Public Health 12:S57-9. 2004
    ....
  43. doi request reprint Preparation and in vitro evaluation of benzylsulfanyl benzoxazole derivatives as potential antituberculosis agents
    Věra Klimešová
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, Hradec, Kralove, 500 05, Czech Republic
    Eur J Med Chem 44:2286-93. 2009
    ..We demonstrated that lower lipophilicity has significant contribution to activity. Dinitrobenzylsulfanyl derivative of benzoxazole represents the promising small-molecule synthetic antimycobacterials...
  44. ncbi request reprint Combination of molecular modeling and quantitative structure-activity relationship analysis in the study of antimycobacterial activity of pyridine derivatives
    V Klimesova
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 500 05, Hradec Kralove, Czech Republic
    Int J Pharm 207:1-6. 2000
    ..Additionally, the results of multiple linear regression indicate the differences between Mycobacterium tuberculosis and M. avium. The hydrophobicity of studied compounds is important for activity against M. avium...
  45. ncbi request reprint Synthesis and antimycobacterial activity of 1,2,4-triazole 3-benzylsulfanyl derivatives
    Věra Klimešová
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 50005 Hradec Kralove, Czech Republic
    Farmaco 59:279-88. 2004
    ..The most active substances bear two nitro groups or a thioamide group on the benzyl moiety. As regards the cytotoxicity effect, the evaluated compounds can be considered as moderately toxic...
  46. doi request reprint N-Benzylsalicylthioamides as novel compounds with promising antimycotic activity
    Eva Petrlíková
    Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Heyrovskeho, Hradec Kralove, Czech Republic
    Bioorg Med Chem Lett 20:4535-8. 2010
    ..The compounds exhibited an in vitro antifungal activity against the fluconazole-susceptible as well as the fluconazole-resistant fungal strains. The biological activity was analyzed by quantitative structure-activity relationship (QSAR)...
  47. ncbi request reprint New benzimidazole derivatives as antimycobacterial agents
    Věra Klimešová
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Farmaco 57:259-65. 2002
    ..The effect of the most active compound in the set, 3,5-dinitro derivative 3t, exceeded that of the standard isoniazide against M. kansasii and Mycobacterium avium...
  48. ncbi request reprint Synthesis and preliminary evaluation of benzimidazole derivatives as antimicrobial agents
    Věra Klimešová
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, CZ 50005 Hradec Kralove, Czech Republic
    Eur J Med Chem 37:409-18. 2002
    ..The antifungal activities of the compounds were relatively low. A weak antifungal effect was observed against the dermatophyte Trichophyton mentagrophytes. None of the compounds showed significant inhibitory activity against yeasts...
  49. ncbi request reprint On the relationship between the substitution pattern of thiobenzanilides and their antimycobacterial activity
    Jiri Kunes
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic
    Farmaco 57:777-82. 2002
    ....
  50. ncbi request reprint A note on the antitubercular activities of 1-aryl-5-benzylsulfanyltetrazoles
    Jan Adamec
    Department of Inorganic and Organic Chemistry, Charles University, Faculty of Pharmacy, Hradec Kralove, Czech Republic
    Arch Pharm (Weinheim) 338:385-9. 2005
    ..The activity against M. tuberculosis becomes higher with increasing electron-accepting properties of the substituents on the phenyl ring. On the other hand, any substitution on the benzylic moiety decreases the activity...
  51. ncbi request reprint Highly active antimycobacterial derivatives of benzoxazine
    Eva Petrlíková
    Department of Inorganic and Organic Chemistry, Charles University in Prague, Hradec Kralove, Czech Republic
    Bioorg Med Chem 18:8178-87. 2010
    ..The most active derivatives were more active than isonicotinhydrazide (INH). Free-Wilson analysis was also carried out and the activity contribution was examined...
  52. ncbi request reprint [Development of chemotherapy in tuberculosis]
    J Hladůvková
    Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Kralove
    Ceska Slov Farm 50:4-11. 2001
    ..Whereas the other review papers of the series survey the development of structures of novel potential drugs, the present paper aims to show possible treatment of tuberculosis and its problems, concentrating on the contemporary situation...
  53. ncbi request reprint Heterocyclic isosters of antimycobacterial salicylanilides
    Josef Matyk
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Heyrovskeho 1203, CZ 500 05 Hradec Kralove, Czech Republic
    Farmaco 60:399-408. 2005
    ..The molecules were separated on the heterocyclic and salicyl moieties and the study of influences of electronic and hydrophobic properties was used as well. The compounds are a new group of potential anti-tuberculotics...
  54. doi request reprint Antibacterial activity of N-benzylsalicylthioamides
    E Petrlíková
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, 500 03 Hradec Králové, Czechia
    Folia Microbiol (Praha) 55:418-21. 2010
    ..The antibacterial activity increased with lipophilicity, with the presence of halogens and with increasing value of Hammet substituent constant σ...
  55. ncbi request reprint Similarity approach to QSAR. Application to antimycobacterial benzoxazines
    Ana Gallegos
    Institute of Computational Chemistry, University of Girona, Campus Montilivi 17071, Girona, Spain
    Int J Pharm 269:51-60. 2004
    ..The replacement of the oxo group by the thioxo group in position 4 on the benzoxazine ring of the antitubercular 3-(phenyl)-2H-benzoxazine-2,4(3H)-diones increases the activity, as well as the similar replacement in position 2...
  56. ncbi request reprint QSPR modeling of the half-wave potentials of benzoxazines by optimal descriptors calculated with the SMILES
    Andrey Toropov
    Uzbek Academy of Sciences, Institute of Geology and Geophysics, Khodzhibaev Street 49, 700041 Tashkent, Uzbekistan
    Comput Biol Chem 30:434-7. 2006
    ....