Tien L Huang

Summary

Affiliation: Xavier University of Louisiana
Country: USA

Publications

  1. ncbi request reprint N,N'-bis[4-(N-alkylamidino)phenyl]homopiperazines as anti-Pneumocystis carinii agents
    T L Huang
    Xavier University of Louisiana, College of Pharmacy, New Orleans, LA 70125, USA
    Bioorg Med Chem Lett 11:2679-81. 2001
  2. pmc Synthesis and SAR of alkanediamide-linked bisbenzamidines with anti-trypanosomal and anti-pneumocystis activity
    Tien L Huang
    Xavier University of Louisiana, College of Pharmacy, 1 Drexel Drive, New Orleans, LA 70125, USA
    Bioorg Med Chem Lett 19:5884-6. 2009
  3. ncbi request reprint Trypanocidal activity of piperazine-linked bisbenzamidines and bisbenzamidoxime, an orally active prodrug
    Tien L Huang
    College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA
    Int J Antimicrob Agents 30:555-61. 2007
  4. ncbi request reprint Anti-plasmodial and anti-leishmanial activity of conformationally restricted pentamidine congeners
    Tien L Huang
    Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, New Orleans, 70125, USA
    J Pharm Pharmacol 58:1033-42. 2006
  5. ncbi request reprint Parallel solution-phase synthesis of conformationally restricted congeners of pentamidine and evaluation of their antiplasmodial activities
    Annie Mayence
    College of Pharmacy, Division of Basic Pharmaceutical Sciences, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, Louisiana 70125, USA
    J Med Chem 47:2700-5. 2004
  6. doi request reprint Novel bisbenzimidazoles with antileishmanial effectiveness
    Annie Mayence
    Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans, LA 70125, USA
    Bioorg Med Chem Lett 18:2658-61. 2008
  7. ncbi request reprint Piperazine-linked bisbenzamidines: a novel class of antileishmanial agents
    Annie Mayence
    Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA
    Eur J Med Chem 39:547-53. 2004
  8. pmc Alkanediamide-Linked Bisbenzamidines Are Promising Antiparasitic Agents
    Jean J Vanden Eynde
    College of Pharmacy, Xavier University of Louisiana, New Orleans, LA 70125, USA
    Pharmaceuticals (Basel) 9:. 2016
  9. doi request reprint Bis(oxyphenylene)benzimidazoles: a novel class of anti-Plasmodium falciparum agents
    Annie Mayence
    Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans, LA 70125, USA
    Bioorg Med Chem 19:7493-500. 2011
  10. ncbi request reprint Novel bisbenzamidines as potential drug candidates for the treatment of Pneumocystis carinii pneumonia
    Jean Jacques Vanden Eynde
    Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans 70125, USA
    Bioorg Med Chem Lett 14:4545-8. 2004

Collaborators

Detail Information

Publications19

  1. ncbi request reprint N,N'-bis[4-(N-alkylamidino)phenyl]homopiperazines as anti-Pneumocystis carinii agents
    T L Huang
    Xavier University of Louisiana, College of Pharmacy, New Orleans, LA 70125, USA
    Bioorg Med Chem Lett 11:2679-81. 2001
    ..Compounds 2 and 8 were the most potent and caused about 70% inhibition of Pneumocystis carinii growth in a cell culture model at 1 microM concentrations...
  2. pmc Synthesis and SAR of alkanediamide-linked bisbenzamidines with anti-trypanosomal and anti-pneumocystis activity
    Tien L Huang
    Xavier University of Louisiana, College of Pharmacy, 1 Drexel Drive, New Orleans, LA 70125, USA
    Bioorg Med Chem Lett 19:5884-6. 2009
    ..carinii, and was non-cytotoxic in the A549 human lung carcinoma cell line. The inhibitory bioactivity was significantly reduced when the amidine groups in 4 were moved from the para to the meta positions or replaced with amides...
  3. ncbi request reprint Trypanocidal activity of piperazine-linked bisbenzamidines and bisbenzamidoxime, an orally active prodrug
    Tien L Huang
    College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA
    Int J Antimicrob Agents 30:555-61. 2007
    ..Three compounds (7, 11 and 15) provided 100% cure when administered parenterally. The results indicate that the nature of the substituents at the amidinium nitrogens of bisbenzamidines strongly influence their trypanocidal activity...
  4. ncbi request reprint Anti-plasmodial and anti-leishmanial activity of conformationally restricted pentamidine congeners
    Tien L Huang
    Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, New Orleans, 70125, USA
    J Pharm Pharmacol 58:1033-42. 2006
    ..These compounds provide important structure-activity relationship data for the design of improved chemotherapeutic agents against parasitic infections...
  5. ncbi request reprint Parallel solution-phase synthesis of conformationally restricted congeners of pentamidine and evaluation of their antiplasmodial activities
    Annie Mayence
    College of Pharmacy, Division of Basic Pharmaceutical Sciences, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, Louisiana 70125, USA
    J Med Chem 47:2700-5. 2004
    ..DNA binding affinity, as estimated by DeltaT(m), did not correlate with either antiparasite effects or cytotoxicity. Each of the active bisbenzamidines interfered with the formation of hemozoin in cell-free systems...
  6. doi request reprint Novel bisbenzimidazoles with antileishmanial effectiveness
    Annie Mayence
    Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans, LA 70125, USA
    Bioorg Med Chem Lett 18:2658-61. 2008
    ..Among the six tested compounds two derivatives emerged as promising hits characterized by IC(50) values lower than that determined for pentamidine against L. donovani...
  7. ncbi request reprint Piperazine-linked bisbenzamidines: a novel class of antileishmanial agents
    Annie Mayence
    Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA
    Eur J Med Chem 39:547-53. 2004
    ..Among these compounds, 1,4-bis[4-(1H-benzimidazol-2-yl)phenyl]piperazine (14) emerged as the most active compound with an IC(50) value of 0.41 microM which is about sevenfold more potent than pentamidine...
  8. pmc Alkanediamide-Linked Bisbenzamidines Are Promising Antiparasitic Agents
    Jean J Vanden Eynde
    College of Pharmacy, Xavier University of Louisiana, New Orleans, LA 70125, USA
    Pharmaceuticals (Basel) 9:. 2016
    ..Thermal melting of DNA and molecular modeling studies indicate AT-rich DNA sequences as possible binding sites for these compounds. Several of the tested compounds are suitable leads for the development of improved antiparasitic agents. ..
  9. doi request reprint Bis(oxyphenylene)benzimidazoles: a novel class of anti-Plasmodium falciparum agents
    Annie Mayence
    Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans, LA 70125, USA
    Bioorg Med Chem 19:7493-500. 2011
    ..falciparum K1 strain) varying between 92 and more than 450. Two of the eight novel drug leads, namely compounds 19 and 32, were also active against G. intestinalis and L. donovani with selectivity indexes of 122 and >164 respectively...
  10. ncbi request reprint Novel bisbenzamidines as potential drug candidates for the treatment of Pneumocystis carinii pneumonia
    Jean Jacques Vanden Eynde
    Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans 70125, USA
    Bioorg Med Chem Lett 14:4545-8. 2004
    ....
  11. doi request reprint Design and synthesis of N¹,N⁵-bis[4-(5-alkyl-1,2,4-oxadiazol-3-yl)phenyl]glutaramides as potential antifungal prodrugs
    Nageswara Rao Kode
    College of Pharmacy, Xavier University of Louisiana, New Orleans, LA 70125, USA
    Molecules 18:11250-63. 2013
    ..These products are designed to function as masked bis-amidine prodrugs of a promising N1,N5-bis[4-(N'-(carbamimidoyl)phenyl]glutaramide antifungal lead. ..
  12. ncbi request reprint Evidences for the formation of bisbenzamidine-heme complexes in cell-free systems
    Annie Mayence
    Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans, LA 70125, USA
    Bioorg Med Chem Lett 14:1625-8. 2004
    ..0 the interaction yielded insoluble complexes for which a sandwich-type structure of stoichiometry 2:1, heme-drug, is tentatively proposed...
  13. doi request reprint Small-molecule inhibitors of Wnt signaling pathway: towards novel anticancer therapeutics
    Shilong Zheng
    RCMI Cancer Research Center, Xavier University of Louisiana, New Orleans, LA 70125, USA
    Future Med Chem 7:2485-505. 2015
    ....
  14. doi request reprint Some non-conventional biomolecular targets for diamidines. A short survey
    Tien L Huang
    Xavier University of Louisiana, Department of Basic Pharmaceutical Science, College of Pharmacy, 1 Drexel Drive, New Orleans, LA 70125, USA
    Bioorg Med Chem 22:1983-92. 2014
    ..A summary of the most striking results obtained to date in those domains is presented is this review. ..
  15. pmc Histone deacetylase inhibitors in clinical studies as templates for new anticancer agents
    Madhusoodanan Mottamal
    RCMI Cancer Research Center, Xavier University of Louisiana, New Orleans, LA 70125, USA
    Molecules 20:3898-941. 2015
    ....
  16. ncbi request reprint Trypanocidal activity of conformationally restricted pentamidine congeners
    Isaac O Donkor
    Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, 847 Monroe Avenue, Room 327E, Johnson Building, Memphis, Tennessee 38163, USA
    J Med Chem 46:1041-8. 2003
    ....
  17. pmc In vitro selection and in vivo efficacy of piperazine- and alkanediamide-linked bisbenzamidines against Pneumocystis pneumonia in mice
    Melanie T Cushion
    Research Service, Veterans Affairs Medical Center, Cincinnati, OH 45220, USA
    Antimicrob Agents Chemother 50:2337-43. 2006
    ..We conclude that a number of these bisbenzamidine compounds, especially compound 100, may show promise as new anti-Pneumocystis drugs...
  18. pmc Highly active anti-Pneumocystis carinii compounds in a library of novel piperazine-linked bisbenzamidines and related compounds
    Melanie T Cushion
    University of Cincinnati College of Medicine, Division of Infectious Diseases, 231 Albert Sabin Way, Cincinnati, OH 45267 0560, USA
    Antimicrob Agents Chemother 48:4209-16. 2004
    ..The strategy of substitution of 1,4-piperazine-linked bisbenzamidines produced compounds with the highest level of activity observed in the ATP assay and holds great promise for the development of efficacious anti-P. carinii therapy...
  19. ncbi request reprint Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics
    Isaac O Donkor
    Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 38163, USA
    Bioorg Med Chem Lett 13:783-4. 2003
    ..The ring size of the P(2)-constraining residue influenced the inhibitory potency and selectivity of the compounds for calpain I compared to the other proteases...