1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position
作者:Brian A. Johns、Jason G. Weatherhead、Scott H. Allen、James B. Thompson、Edward P. Garvey、Scott A. Foster、Jerry L. Jeffrey、Wayne H. Miller
DOI:10.1016/j.bmcl.2009.01.089
日期:2009.3
The use of a 1,3,4-oxadiazole in combination with an 8-hydroxy-1,6-naphthyridine ring system has been shown to deliver potent enzyme and antiviral activity through inhibition of viral DNA integration. This report presents a detailed structure-activity investigation of the C5 position resulting in low nM potency for several analogs with an excellent therapeutic index. (C) 2009 Elsevier Ltd. All rights reserved.
Franchimont; Rouffaer, Recueil des Travaux Chimiques des Pays-Bas, 1894, vol. 13, p. 339