Title of article
Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors
Author/Authors
Haolun Jin، نويسنده , , Ruby Z. Cai، نويسنده , , Laura Schacherer، نويسنده , , Salman Jabri، نويسنده , , Manuel Tsiang، نويسنده , , Maria Fardis، نويسنده , , Xiaowu Chen، نويسنده , , James M. Chen، نويسنده , , Choung U. Kim، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
3989
To page
3992
Abstract
A novel class of tri-cyclic HIV integrase inhibitors were designed based on conformational analysis of 1,6-naphthyridine carboxamide compound L-870810 and docking the designed inhibitor into the active site of our integrase enzyme model. The efficient syntheses of pyrroloquinoline tri-cyclic analogs are described. The SAR studies resulted in the identification of a lead compound that is more potent and more soluble than L-870810.
Keywords
HIV , integrase , inhibitors , Pyrolloquinoline , modeling , Tri-cyclic
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797119
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