TY - JOUR
T1 - Design, synthesis, and X-ray crystallographic analysis of a novel class of Hiv-1 protease inhibitors
AU - Ganguly, Ashit K.
AU - Alluri, Sesha S.
AU - Caroccia, Danielle
AU - Biswas, Dipshikha
AU - Wang, Chih Hung
AU - Kang, Eunhee
AU - Zhang, Yong
AU - McPhail, Andrew T.
AU - Carroll, Steven S.
AU - Burlein, Christine
AU - Munshi, Vandna
AU - Orth, Peter
AU - Strickland, Corey
PY - 2011/10/27
Y1 - 2011/10/27
N2 - In the present paper, design, synthesis, X-ray crystallographic analysis, and HIV-1 protease inhibitory activities of a novel class of compounds are disclosed. Compounds 28-30, 32, 35, and 40 were synthesized and found to be inhibitors of the HIV-1 protease. The crucial step in their synthesis involved an unusual endo radical cyclization process. Absolute stereochemistry of the three asymmetric centers in the above compounds have been established to be (4S,2′R,3′S) for optimal potency. X-ray crystallographic analysis has been used to determine the binding mode of the inhibitors to the HIV-1 protease.
AB - In the present paper, design, synthesis, X-ray crystallographic analysis, and HIV-1 protease inhibitory activities of a novel class of compounds are disclosed. Compounds 28-30, 32, 35, and 40 were synthesized and found to be inhibitors of the HIV-1 protease. The crucial step in their synthesis involved an unusual endo radical cyclization process. Absolute stereochemistry of the three asymmetric centers in the above compounds have been established to be (4S,2′R,3′S) for optimal potency. X-ray crystallographic analysis has been used to determine the binding mode of the inhibitors to the HIV-1 protease.
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U2 - 10.1021/jm200778q
DO - 10.1021/jm200778q
M3 - Article
C2 - 21916489
AN - SCOPUS:80054882601
SN - 0022-2623
VL - 54
SP - 7176
EP - 7183
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 20
ER -
