Cover Picture: Preparation and Evaluation of Potent Pentafluorosulfanyl‐Substituted Anti‐Tuberculosis Compounds (ChemMedChem 14/2017). (17th July 2017)

• Record Type: Journal Article
• Authors: Moraski, Garrett C.; Bristol, Ryan; Seeger, Natalie; Boshoff, Helena I.; Tsang, Patricia Siu‐Yee; Miller, Marvin J.
• Is Part Of: ChemMedChem. Volume 12:Number 14(2017)
• Page Start: 1102
• Page End: 1102
• Publication Date: 2017-07-17
• Subjects: drug resistance -- imidazo[1, 2-a]pyridines -- imidazo[2, 1-b]thiazoles -- Mycobacterium tuberculosis -- pentafluorosulfanyl; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201700398
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract : The front cover picture shows promising pentafluorosulfanyl (SF5 ) anti‐tuberculosis compounds 6‐chloro‐2‐ethyl‐ N ‐(3‐(pentafluoro‐λ 6 ‐sulfaneyl)benzyl)imidazo[1, 2‐ a ]pyridine‐3‐carboxamide (18 ) and 2, 6‐dimethyl‐ N ‐(4‐(pentafluoro‐λ 6 ‐sulfaneyl)benzyl)imidazo[2, 1‐ b ]thiazole‐5‐carboxamide (19 ) ascending a mountain of in vitro assessments (including replicating, nonreplicating, and intracellular potency, toxicity, solubility, and ADME). These SF5 ‐bearing compounds were also compared with similar CF3 ‐bearing compounds 2, 6‐dimethyl‐ N ‐(4‐(trifluoromethyl)benzyl)imidazo[1, 2‐ a ]pyridine‐3‐carboxamide (1 ) and 2, 6‐dimethyl‐ N ‐(4‐(trifluoromethyl)benzyl)imidazo[2, 1‐ b ]thiazole‐5‐carboxamide (5 ). The overarching goal is to advance compounds within the next "mountains" of preclinical evaluation. Cover art created by Rebecca Rausch. More information can be found in the Full Paper by Garrett C. Moraski, Marvin J. Miller et al. onpage 1108 in Issue 14, 2017 (DOI:10.1002/cmdc.201700170 ).