Literature DB >> 30294073

CYCLIC SULFONE-3-CARBOXAMIDES AS NOVEL P2-LIGANDS FOR Ro 31-8959 BASED HIV-1 PROTEASE INHIBITORS.

Arun K Ghosh1, Wayne J Thompson2, Peter M Munson2, Wenming Liut1, Joel R Huff2.   

Abstract

Cyclic sulfone-3-carboxamides are effective P2-1igands for HIV-1 protease inhibitors. Incorporation of 3S-tetrahydro-2H-thiopyrancarboxamide-l, l-dioxide in the hydroxyethylamine series resulted in inhibitor 14 (IC50=9 nM, CIC95=200 nM) with improved potency compared to its corresponding urethane derivative 18 (IC50=2.0 μM).

Entities:  

Year:  2000        PMID： 30294073      PMCID： PMC6173326          DOI： 10.1016/0960-894X(94)00463-P

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  Tetrahydrothiophene (thiophane) derivatives.

Authors:  R B WOODWARD; R H EASTMAN
Journal:  J Am Chem Soc       Date:  1946-11       Impact factor: 15.419

2.  Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.

Authors:  W J Thompson; P M Fitzgerald; M K Holloway; E A Emini; P L Darke; B M McKeever; W A Schleif; J C Quintero; J A Zugay; T J Tucker
Journal:  J Med Chem       Date:  1992-05-15       Impact factor: 7.446

3.  Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.

Authors:  A K Ghosh; W J Thompson; H Y Lee; S P McKee; P M Munson; T T Duong; P L Darke; J A Zugay; E A Emini; W A Schleif
Journal:  J Med Chem       Date:  1993-04-02       Impact factor: 7.446

4.  Rational design of peptide-based HIV proteinase inhibitors.

Authors:  N A Roberts; J A Martin; D Kinchington; A V Broadhurst; J C Craig; I B Duncan; S A Galpin; B K Handa; J Kay; A Kröhn
Journal:  Science       Date:  1990-04-20       Impact factor: 47.728

5.  The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors.

Authors:  A K Ghosh; H Y Lee; W J Thompson; C Culberson; M K Holloway; S P McKee; P M Munson; T T Duong; A M Smith; P L Darke
Journal:  J Med Chem       Date:  1994-04-15       Impact factor: 7.446

6.  3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors.

Authors:  A K Ghosh; W J Thompson; S P McKee; T T Duong; T A Lyle; J C Chen; P L Darke; J A Zugay; E A Emini; W A Schleif
Journal:  J Med Chem       Date:  1993-01-22       Impact factor: 7.446

7.  Affinity purification of the HIV-1 protease.

Authors:  J C Heimbach; V M Garsky; S R Michelson; R A Dixon; I S Sigal; P L Darke
Journal:  Biochem Biophys Res Commun       Date:  1989-11-15       Impact factor: 3.575
  7 in total
  2 in total

1.  Asymmetric Aldol Route to Hydroxyethylamine Isostere: Stereoselective Synthesis of the Core Unit of Saquinavir.

Authors:  Arun K Ghosh; Khaja Azhar Hussain; Steve Fidanze
Journal:  J Org Chem       Date:  1997-08-22       Impact factor: 4.354

2.  Chiral Auxiliary Mediated Conjugate Reduction and Asymmetric Protonation: Synthesis of High Affinity Ligands for HIV Protease Inhibitors.

Authors:  Arun K Ghosh; Wenming Liu
Journal:  J Org Chem       Date:  1995-09-01       Impact factor: 4.354
  2 in total

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