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Structure-based design of achiral anthranilamides as P2/P2′ surrogates for symmetry-based HIV protease inhibitors: design, synthesis, X-ray structure, enzyme inhibition and antiviral activity

✍ Scribed by Ramnarayan S. Randad; Lucyna Lubkowska; Anna Bujacz; Rajan H. Naik; Sergei V. Gulnik; Betty Yu; Abelardo Silva; Sanjeev Munshi; Tracy M. Lynch; David J. Clanton; T.Narayana Bhat; John W. Erickson

Publisher: Elsevier Science
Year: 1995
Tongue: English
Weight: 314 KB
Volume: 5
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(95)00449-4

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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