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DMPK and Safety Profile of Compounds 6 , 12 , 13 , 14 , 22 , 23 , 27 , 36 , 40 , 47 and BM635

Journal: ACS Medicinal Chemistry Letters

Article Title: Novel Pyrazole-Containing Compounds Active against Mycobacterium tuberculosis

doi: 10.1021/acsmedchemlett.9b00204

Figure Lengend Snippet: DMPK and Safety Profile of Compounds 6 , 12 , 13 , 14 , 22 , 23 , 27 , 36 , 40 , 47 and BM635

Article Snippet: Moreover, compounds with MICs < 1 μM were evaluated to determine the drug metabolism and pharmacokinetics (DMPK) profile (Chrom log D pH7.4 values, artificial membrane permeability, percentage of binding to human serum albumin (HSA), kinetic solubility, solubility in the biorelevant medium to simulate fasted states in vivo (FaSSIF), and human ether-a-go-go-related gene (hERG)) binding, and those providing the best profile were selected to determine their efficacy in vivo.

Techniques: Membrane, Permeability