Novel cyclized Pifithrin-α p53 inactivators: Synthesis and biological studies
Starting from various cyclic or bicyclic ketones, we have synthesized novel Pifithrin-α analogues bearing different methyl substituted phenyl ketone groups at the N3-position of the 2-iminothiazole heterocycle. From stability studies in a biolo
Discovery of imidazo[2,1- b ]thiazole HCV NS4B inhibitors exhibiting synergistic effect with other direct-acting antiviral agents
The design, synthesis, and SAR studies of novel inhibitors of HCV NS4B based on the imidazo[2,1-b]thiazole scaffold were described. Optimization of potency with respect to genotype 1b resulted in the discovery of two potent leads 26f (EC50 = 16
A novel and efficient one pot synthesis of 2,4-disubstituted thiazoles and oxazoles using phenyltrimethylammoniumtribromide in ionic liquid
A novel and efficient one-pot procedure has been described for synthesis of 2,4-disubstituted thiazoles and oxazoles from substituted ketones using phenyltrimethylammoniumtribromide as in situ brominating agent followed by reaction with thioamide/thiourea and amides/ureas, respectively in [bmim][BF4] ionicliquid. The advantages of the procedure include avoiding the handling of lacrymetric compounds, hazardous and toxic organic solvents along with good to excellent yield of the products.
Muthyala, Manoj Kumar,Kumar, Anil
p. 959 - 964
(2012/10/29)
Discovery and hit-to-lead optimization of novel allosteric glucokinase activators
We report on a hit generation and hit-to-lead program of a novel class of glucokinase activators (GKAs). Hit compounds, activators at low glucose concentration only were identified by vHTS. Scaffold modification reliably afforded activators also at high s