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Synthesis and evaluation of delta lactams as nonpeptide HIV-protease inhibitors

โœ Scribed by George V. De Lucca

Publisher
Elsevier Science
Year
1997
Tongue
English
Weight
208 KB
Volume
7
Category
Article
ISSN
0960-894X

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โœฆ Synopsis

The cyclizatlon of the linear hydroxyethylene isostere based HIV-PR inhibitors gave the delta lactam XQ921, which was found to have a K i = 9.4 uM. It is proposed that a major reason for the weaker potency of the lactam XQ921 compared to cycliv urea based inhibitors is the lack of a PI' substituent that could interact with the S 1' pocket of HIV-PR.

๐Ÿ“œ SIMILAR VOLUMES

Discovery and optimization of nonpeptide
Discovery and optimization of nonpeptide HIV-1 protease inhibitors
โœ Peter J. Tummino; J.V.N. Vara Prasad; Donna Ferguson; Carolyn Nouhan; Neil Graha ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 779 KB

Several small, achiral nonpeptide inhibitors of HIV-1 protease with low micromolar activity were identified by mass screening of the Parke-Davis compound library. Two of the compounds, structurally similar, were both found to be competitive and reversible inhibitors [compound 1, 4-hydroxy-3-(3-pheno