Nonpeptidal P 2 Ligands for HIV Protease Inhibitors: Structure-Based Design, Synthesis, and Biological Evaluation
β Scribed by Ghosh, Arun K.; Kincaid, John F.; Walters, D. Eric; Chen, Yan; Chaudhuri, Narayan C.; Thompson, Wayne J.; Culberson, Chris; Fitzgerald, Paula M. D.; Lee, Hee Yoon; McKee, Sean P.; Munson, Peter M.; Duong, Tien T.; Darke, Paul L.; Zugay, Joan A.; Schleif, William A.; Axel, Melinda G.; Lin, Juinn; Huff, Joel R.
- Book ID
- 125527048
- Publisher
- American Chemical Society
- Year
- 1996
- Tongue
- English
- Weight
- 467 KB
- Volume
- 39
- Category
- Article
- ISSN
- 0022-2623
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π SIMILAR VOLUMES
The cocrystal structures of LY289612 and LY297135 were used as a starting point in the design of nonpeptidic HIV-1 protease inhibitors. This report details the discovery of a series of novel aromatic P2 replacement groups. The 3-hydroxy-2-methyl benzoic acid group, discovered in AG1254, was incorpor
A combination of structure-activity studies, kinetic analysis, X-ray crystallographic analysis, and modeling were employed in the design of a novel series of HIV-1 protease (HIV PR) inhibitors. The crystal structure of a complex of HIV PR with SRSS-2,5-bis[N-(tert-butyloxycarbonyl)amino]-3,4-dihydro
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