Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5174
Title: An approach to the stereo-controlled synthesis of polycyclic derivatives of L-4-thiazolidinecarboxilic acid active against HIV-1 integrase
Authors: F., Aiello
Brizzi, Antonella 
O., DE GRAZIA
A., Garofalo
F., Grande
M. S., Sinicropi
R., Dayam
N., Neamati
Issue Date: 2006
Project: None 
Journal: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Abstract: 
Herein, we describe a new strategy for the preparation of thiazolothiazepine-based inhibitors of human immunodeficiency virus type-1 integrase (IN). The present method allows facile preparation of the title compounds in a single enantiomeric form starting from l-4-thiazolidinecarboxylic acid. This method could be easily extended to the synthesis of several analogs derived from optically active cyclic aminoacids. We also present a putative model showing the interaction between l- and d-isomers of compound 1 in the IN active site. A sensibly lower IC(50) value was found for (-)-1 over racemic-1 in an anti-IN assay.
Description: 
26342
URI: http://hdl.handle.net/20.500.12779/5174
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2006.03.032
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