Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors
LQ Al-Mawsawi, R Dayam, L Taheri, M Witvrouw… - Bioorganic & medicinal …, 2007 - Elsevier
Bioorganic & medicinal chemistry letters, 2007•Elsevier
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 …
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 …
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.
Elsevier
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