67525-89-7Relevant academic research and scientific papers
Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor
Romines, Karen R.,Freeman, George A.,Schaller, Lee T.,Cowan, Jill R.,Gonzales, Steve S.,Tidwell, Jeffrey H.,Andrews III, Clarence W.,Stammers, David K.,Hazen, Richard J.,Ferris, Robert G.,Short, Steven A.,Chan, Joseph H.,Boone, Lawrence R.
, p. 727 - 739 (2007/10/03)
Despite the progress of the past two decades, there is still considerable need for safe, efficacious drugs that target human immunodeficiency virus (HIV). This is particularly true for the growing number of patients infected with virus resistant to currently approved HIV drugs. Our high throughput screening effort identified a benzophenone template as a potential nonnucleoside reverse transcriptase inhibitor (NNRTI). This manuscript describes our extensive exploration of the benzophenone structure-activity relationships, which culminated in the identification of several compounds with very potent inhibition of both wild type and clinically relevant NNRTI-resistant mutant strains of HIV. These potent inhibitors include 70h (GW678248), which has in vitro antiviral assay IC50 values of 0.5 nM against wild-type HIV, 1 nM against the K103N mutant associated with clinical resistance to efavirenz, and 0.7 nM against the Y181C mutant associated with clinical resistance to nevirapine. Compound 70h has also demonstrated relatively low clearance in intravenous pharmacokinetic studies in three species, and it is the active component of a drug candidate which has progressed to phase 2 clinical studies.
A synthesis of 2-acyl-3-hydroxythiophenes
Adamczewska,Barker,Huddleston,Wood
, p. 1083 - 1096 (2007/10/03)
2-Acyl-3-hydroxythiophenes have been made by the reaction of the anion of a mercaptoketone with dimethyl acetylenedicarboxylate to give a hydroxythiophene ester which is then hydrolysed and decarboxylated.
Thiophene compounds and their manufacture
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, (2008/06/13)
New thiophene compounds and a new process for the manufacture of thiophene compounds by dehydrogenating dihydrothiophene with certain halogen compounds. The products are starting materials for the manufacture of pharmaceuticals, dyes and plant protection agents and, in particular, for the manufacture of additives to foodstuffs, feeds, beverages and pharmaceuticals.
Aromatization of Dihydrothiophenes. Thiophenesaccharin: A Sweet Surprise
Rossy, Phillip A.,Hoffmann, Werner,Mueller, Norbert
, p. 617 - 620 (2007/10/02)
Sulfuryl chloride has been shown to be highly effective in the dehydrogenation of 3,4-disubstituted-2,5-dihydrothiophenes and 2,3-disubstituted-4,5-dihydrothiophenes, in which the 3,4 and 2,3 substitutents are part of a β-keto carbonyl functionality or it
