Lu, Guo-Liang published the artcileSynthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis, Computed Properties of 209919-30-2, the publication is Bioorganic & Medicinal Chemistry (2020), 28(22), 115784, database is CAplus and MEDLINE.
A series of 5,8-disubstituted tetrahydroisoquinolines e.g., 2-((5-(4-chlorophenyl)pyridin-2-yl)methyl)-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydroisoquinoline were shown to be effective inhibitors of M. tb in culture and modest inhibitors of M. tb ATP synthase. There was a broad general trend of improved potency with higher lipophilicity. Large substituents (e.g., Bn) at the tetrahydroquinoline 5-position were well-tolerated, while N-methylpiperazine was the preferred 8-substituent. Structure-activity relationships for 7-linked side chains showed that the nature of the 7-linking group was important; -CO- and -COCH2– linkers were less effective than -CH2– or -CONH- ones. This suggests that the positioning of a terminal aromatic ring is important for target binding. Selected compounds showed much faster rates of microsomal clearance than the clin. ATP synthase inhibitor bedaquiline, and modest inhibition of mycobacterial ATP synthase.
Bioorganic & Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Computed Properties of 209919-30-2.
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https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics