Publication Abstract from PubMed
Abstract 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.
Design, Synthesis and X-ray crystallographic analysis of a Novel Class of HIV-1 Protease Inhibitors.,Ganguly AK, Alluri SS, Caroccia D, Biswas D, Wang CH, Kang E, Zhang Y, McPhail AT, Carroll SS, Burlein C, Munshi V, Orth P, Strickland C J Med Chem. 2011 Sep 14. PMID:21916489[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.