1027346-55-9Relevant academic research and scientific papers
HYDRAZIDE, AMIDE, PHTHALIMIDE AND PHTHALHYDRAZIDE ANALOGS AS INHIBITORS OF RETROVIRAL INTEGRASE
-
Page/Page column 51, (2009/04/25)
The present invention provides catechol-containing hydrazides, amides, phthalimide and phthalhydrazide analogs. These compounds are inhibitors of retroviral integrase, an essential enzyme for the proliferation of retroviruses such as HIV-1. Also provided are pharmaceutical compositions comprising at least one of the catechol-containing hydrazides, amides, phthalimide or phthalhydrazide analogs and a method of using the hydrazide, amide, phthalimide and phthalhydrazide analogs to inhibit retroviral proliferation and as therapeutics for the treatment of AIDS.
2,3-Dihydro-6,7-dihydroxy-1H-isoindol-1-one-based HIV-1 integrase inhibitors
Xue, Zhi Zhao,Semenova, Elena A.,Vu, B. Christie,Maddali, Kasthuraiah,Marchand, Christophe,Hughes, Stephen H.,Pommier, Yves,Burke Jr., Terrence R.
, p. 251 - 259 (2008/09/19)
The bis-salicylhydrazides class of HIV-1 integrase (IN) inhibitors has been postulated to function by metal chelation. However, members of this series exhibit potent inhibition only when Mn2+ is used as cofactor. The current study found that bis-aroylhydrazides could acquire inhibitory potency in Mg2+ using dihydroxybenzoyl substituents as both the right and left components of the hydrazide moiety. Employing a 2,3-dihydro-6,7-dihydroxy-1H- isoindol-1-one ring system as a conformationally constrained 2,3-dihydroxybenzoyl equivalent provided good selectivity for IN-catalyzed strand transfer versus the 3′-processing reactions as well as antiviral efficacy in cells using HIV-1 based vectors.
