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[4-R-(4-ALPHA,6-BETA,7-BETA]-HEXAHYDRO-5,6-DI(HYDROXY)-1,3-DI(ALLYL)-4,7-BISPHENYLMETHYL)-2H-1,3-DIAZEPINONE

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
01

Overview

This compound is a synthetic small molecule belonging to the class of cyclic urea-based inhibitors designed to target HIV protease. It features a hexahydro 1,3-diazepinone core with two hydroxy groups and bulky bis(phenylmethyl) and allyl substituents. The molecule acts as an HIV protease inhibitor by binding in the active site of the enzyme through multiple hydrogen bonds and van der Waals interactions. Its design aims to overcome resistance mutations in HIV by maximizing binding affinity via preorganized C2-symmetric scaffolds and strategic P1/P2 group modifications. This compound was developed as part of research into potent antiretroviral agents but is not known to be marketed or approved for clinical use[8][9].

Other names
(4R,5S,6S,7R)-1,3-diallyl-4,7-dibenzyl-5,6-dihydroxy-1,3-diazepan-2-one(4R-(4α,5α,6β,7β))-1,3-diallyl-5,6-dihydroxy-4,7-dibenzyl-1,3-diazepin-2-one153223–14–4
02

Targets

PR (Progesterone receptor)

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