1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent Anti-HIV activity
- 23 August 2001
- journal article
- research article
- Published by Elsevier in Bioorganic & Medicinal Chemistry Letters
- Vol. 11 (20) , 2741-2745
- https://doi.org/10.1016/s0960-894x(01)00545-5
Abstract
No abstract availableKeywords
This publication has 12 references indexed in Scilit:
- Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure–Activity relationships for 1-[N-(Methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanesBioorganic & Medicinal Chemistry Letters, 2001
- 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirementsBioorganic & Medicinal Chemistry Letters, 2001
- Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure–activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl)butanesBioorganic & Medicinal Chemistry Letters, 2001
- Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure–activity relationships for substituted 2-aryl-1-[ N -(methyl)- N -(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanesBioorganic & Medicinal Chemistry Letters, 2001
- HIV-1 entry – an expanding portal for drug discoveryDrug Discovery Today, 2000
- Inhibitors of Strand Transfer That Prevent Integration and Inhibit HIV-1 Replication in CellsScience, 2000
- A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activityProceedings of the National Academy of Sciences, 1999
- Potent suppression of HIV-1 replication in humans by T-20, a peptide inhibitor of gp41-mediated virus entryNature Medicine, 1998
- HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5Nature, 1996
- Identification of a major co-receptor for primary isolates of HIV-1Nature, 1996