期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 8, 页码 2127-2129出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.01.050
关键词
abacavir; prodrugs; anti-HIV activity; Schiff bases
The synthesis of a new series of abacavir prodrugs involving N-2-substitution with various substituted benzaldehyde and ketone derivatives is described. The in vitro anti-HIV activities indicated that compound (3-(2-(4-methylaminobenzylideneamino)-6-(cyclopropylamino)-9H-purin-9-yl)cyclopentyl)methanol (3) was found to be most potent compound with EC50 of 0.05 mu M and CC50 of >100 mu M With selectivity index of >2000. Compound 3 was found to be 32 times more potent than the parent drug (EC50 of 1.6 mu M). At pH 7.4, 37 degrees C, the hydrolytic t(1/2) ranged between 120 and 240 min. (C) 2006 Elsevier Ltd. All rights reserved.
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