Bis tertiary amide inhibitors of the HIV-1 protease generated via protein structure-based iterative design

…, H Dawson, JF Davies, K Appelt, BW Wu…

Index: Melnick, Michael; Reich, Siegfried H.; Lewis, Kathy K.; Mitchell Jr., Lennert J.; Nguyen, Dzuy; Trippe, Anthony J.; Dawson, Heather; Davies II, Jay F.; Appelt, Krzysztof; Wu, Bor-Wen; Musick, Linda; Gehlhaar, Dan K.; Webber, Stephanie; Shetty, Bhasker; Kosa, Maha; Kahil, Deborah; Andrada, Dominic Journal of Medicinal Chemistry, 1996 , vol. 39, # 14 p. 2795 - 2811

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Citation Number: 26

Abstract

A series of potent nonpeptide inhibitors of the HIV protease have been identified. Using the structure of compound 3 bound to the HIV protease, bis tertiary amide inhibitor 9 was designed and prepared. Compound 9 was found to be about 17 times more potent than 3, and the structure of the protein-ligand complex of 9 revealed the inhibitor binds in an inverted binding mode relative to 3. Examination of the protein-ligand complex of 9 ...

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