921596-28-3Relevant articles and documents
Synthesis and Antichlamydial Activity of Molecules Based on Dysregulators of Cylindrical Proteases
Seleem, Mohamed A.,Rodrigues De Almeida, Nathalia,Chhonker, Yashpal Singh,Murry, Daryl J.,Guterres, Zaira Da Rosa,Blocker, Amanda M.,Kuwabara, Shiomi,Fisher, Derek J.,Leal, Emilse S.,Martinefski, Manuela R.,Bollini, Mariela,Monge, María Eugenia,Ouellette, Scot P.,Conda-Sheridan, Martin
, p. 4370 - 4387 (2020/05/22)
Chlamydia trachomatis is the most common sexually transmitted bacterial disease globally and the leading cause of infertility and preventable infectious blindness (trachoma) in the world. Unfortunately, there is no FDA-approved treatment specific for chlamydial infections. We recently reported two sulfonylpyridines that halt the growth of the pathogen. Herein, we present a SAR of the sulfonylpyridine molecule by introducing substituents on the aromatic regions. Biological evaluation studies showed that several analogues can impair the growth of C. trachomatis without affecting host cell viability. The compounds did not kill other bacteria, indicating selectivity for Chlamydia. The compounds presented mild toxicity toward mammalian cell lines. The compounds were found to be nonmutagenic in a Drosophila melanogaster assay and exhibited a promising stability in both plasma and gastric fluid. The presented results indicate this scaffold is a promising starting point for the development of selective antichlamydial drugs.
Copper-catalyzed O-arylation of N-protected 1,2-aminoalcohols using functionalized trivalent organobismuth reagents
Petiot, Pauline,Dansereau, Julien,Hbert, Martin,Khene, Imene,Ahmad, Tabinda,Samaali, Samira,Leroy, Maxime,Pinsonneault, Francis,Legault, Claude Y.,Gagnon, Alexandre
supporting information, p. 1322 - 1327 (2015/01/30)
The O-arylation of 1,2-aminoalcohols using functionalized triarylbismuth reagents is reported. The reaction can be performed using substoichiometric amounts of copper acetate and operates under mild conditions. Good functional group tolerance is observed, giving access to a range of β-aryloxyamines. The effect provided by the amino group in the arylation reaction is investigated.
THIAZOLE DERIVATIVES AS STEAROYL COA DESATURASE INHIBITORS
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Page/Page column 34-35, (2010/04/03)
The present invention provides thiazole derivatives as Stearoyl CoA Desaturase (SCD) inhibitors. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase
