Inhibition of HIV-1 capsid assembly: optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold.

Authors :: Tremblay M
Bonneau P
Bousquet Y
DeRoy P
Duan J
Duplessis M
Gagnon A
Garneau M
Goudreau N
Guse I
Hucke O
Kawai SH
Lemke CT
Mason SW
Simoneau B
Surprenant S
Titolo S
Yoakim C
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Dec 15; Vol. 22 (24), pp. 7512-7. Date of Electronic Publication: 2012 Oct 16.
Publication Year :: 2012
Abstract: A uHTS campaign led to the discovery of a 5-(5-furan-2-ylpyrazol-1-yl)-1H-benzimidazole series that inhibits assembly of HIV-1 capsid. Synthetic manipulations at N1, C2 and C16 positions improved the antiviral potency by a . The X-ray structure of 33 complexed with the capsid N-terminal domain allowed identification of major interactions between the inhibitor and the protein.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Subjects :: Antiviral Agents chemical synthesis
Antiviral Agents chemistry
Benzimidazoles chemical synthesis
Benzimidazoles chemistry
Dose-Response Relationship, Drug
Microbial Sensitivity Tests
Models, Molecular
Molecular Structure
Structure-Activity Relationship
Antiviral Agents pharmacology
Benzimidazoles pharmacology
Capsid Proteins antagonists & inhibitors
HIV-1 drug effects

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