Ontology highlight
ABSTRACT:
SUBMITTER: Graham J
PROVIDER: S-EPMC6263154 | biostudies-literature | 2018 Oct
REPOSITORIES: biostudies-literature
Graham James J Wong Christina E CE Day Joshua J McFaddin Elizabeth E Ochsner Urs U Hoang Teresa T Young Casey L CL Ribble Wendy W DeGroote Mary A MA Jarvis Thale T Sun Xicheng X
Bioorganic & medicinal chemistry letters 20180825 19
From a high throughput screening of commercially available libraries against nontuberculous mycobacteria and Mycobacterium tuberculosis, numerous hits were identified with moderate activity. Extensive medicinal chemistry optimization has led to a series of potent benzothiazole amide antimycobacterial agents. Replacement of the adamantyl group with cyclohexyl derivatives and further development of this series resulted in an advanced lead compound, CRS400393, which demonstrated excellent potency a ...[more]