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Birla Institute of Technology & Science, Rajasthan

Abacavir prodrug is found to be more potent than the parent drug against HIV

Published in Health Risk Factor Week, May 16th, 2006

An abacavir prodrug synthesized with an N2-substitution demonstrates better potency than its parent drug against HIV.

"The synthesis of a new series of abacavir prodrugs involving N2-substitution with various substituted benzaldehyde and ketone derivatives is described," investigators in India report.

"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 microM and CC50 of >100 microM with selectivity index of >2000. Compound 3 was found to be...

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