Makane, Vitthal B. published the artcileSynthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis, Name: 2-Chloroisonicotinic acid, the publication is European Journal of Medicinal Chemistry (2019), 665-677, database is CAplus and MEDLINE.
Synthesis, SAR and evaluation of α-aminoacyl amides R1C(O)N(R2)CH(R3)C(O)NHR4 [R1 = 2-pyrrolyl, 2-furyl, 2-thienyl, etc.; R2 = Ph, 4-MeC6H4, 2-HOC6H4, etc.; R3 = Ph, 3-ClC6H4, 4-MeOC6H4, etc.; R4 = t-Bu, cyclohexyl, Bn, 2-naphthyl] as antitubercular agents were reported via Ugi reaction of benzaldehydes, isocyanides, anilines and carboxylic acids. The systematic medicinal chem. approach led to identification of optimal substitutions required for the activity. Compound R1C(O)N(R2)CH(R3)C(O)NHR4 [R1 = 2,4-di-methylthiazol-5-yl; R2 = 2,4-di-MeC6H3; R3 = 3-pyridyl; R4 = cyclohexyl] was identified as antitubercular lead with drug like properties. Further, R1C(O)N(R2)CH(R3)C(O)NHR4 [R1 = 2,4-di-methylthiazol-5-yl; R2 = 2,4-di-MeC6H3; R3 = 3-pyridyl; R4 = cyclohexyl] selectively inhibited M. tuberculosis H37Rv with MIC value of 0.78 μM and was found to be non-toxic to CHO-K1 cells. The lead compound inhibited multi drug resistant and Pre-Extensively drug resistant strains of Mycobacterium at 2 μg/mL and 8 μg/mL resp.
European Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Name: 2-Chloroisonicotinic acid.
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