Design and synthesis of novel conformationally restricted HIV protease inhibitors

F G Salituro; C T Baker; J J Court; D D Deininger; E E Kim; B Li; P M Novak; B G Rao; S Pazhanisamy; M D Porter; W C Schairer; R D Tung

doi:10.1016/s0960-894x(98)00670-2

Design and synthesis of novel conformationally restricted HIV protease inhibitors

Bioorg Med Chem Lett. 1998 Dec 15;8(24):3637-42. doi: 10.1016/s0960-894x(98)00670-2.

Authors

F G Salituro¹, C T Baker, J J Court, D D Deininger, E E Kim, B Li, P M Novak, B G Rao, S Pazhanisamy, M D Porter, W C Schairer, R D Tung

Affiliation

¹ Vertex Pharmaceuticals Incorporated, Cambridge, MA 02139, USA.

PMID: 9934485
DOI: 10.1016/s0960-894x(98)00670-2

Abstract

A set of HIV protease inhibitors represented by compound 2 has previously been described. Structural and conformational analysis of this compound suggested that conformational restriction of the P1/P2 portion of the molecule could lead to a novel set of potent protease inhibitors. Thus, probe compounds 3-7 were designed, synthesized, and found to be potent inhibitors of HIV protease.

MeSH terms

Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / chemistry
Anti-HIV Agents / pharmacology
Crystallography, X-Ray
Drug Design*
HIV Protease Inhibitors / chemical synthesis*
HIV Protease Inhibitors / chemistry
HIV Protease Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Anti-HIV Agents
HIV Protease Inhibitors