| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377152 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
Abstract
The previously discovered salicylhydrazide class of compounds displayed potent HIV-1 integrase (IN) inhibitory activity. The development of this class of compounds as antiretroviral agents was halted due to cytotoxicity in the nanomolar to sub-micromolar range. We identified a novel class of non-cytotoxic hydrazide IN inhibitors utilizing the minimally required salicylhydrazide substructure as a template in a small-molecule database search. The novel hydrazides displayed low micromolar IN inhibitory activity and are several hundred-fold less cytotoxic than previously disclosed salicylhydrazide IN inhibitors.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Laith Q. Al-Mawsawi, Raveendra Dayam, Laleh Taheri, Myriam Witvrouw, Zeger Debyser, Nouri Neamati,