title: Synthesis and biological evaluation of some novel N-aryl-1,4-dihydropyridines as potential antitubercular agents.
abstract: 1,4-Dihydropyridines are the emerging class of antitubercular agent. Recently, studies have revealed that 1,4-dihydropyridine-3,5-dicarbamoyl derivatives with lipophilic groups have demonstrated excellent antitubercular activity. We have synthesized new N-aryl-1,4-dihydropyridines bearing carbethoxy and acetyl group at C-3 and C-5 of the DHP ring. In addition, 1H-pyrazole ring is substituted at C-4 position. The lowest minimum inhibitory concentration value, 0.02 μg/mL, was found for diethyl 1-(2-chlorophenyl)-1,4-dihydro-2,6-dimethyl-4-(1,3-diphenyl-1H-pyrazol-4-yl)pyridine-3,5-dicarboxylate 4e making it more potent than first line antitubercular drug isoniazid. In addition, this compound exhibited relatively low cytotoxicity.
authors.affiliation: Department of Chemistry, Saurashtra University, Kalawad Road, Rajkot 360005, Gujarat, India. drartrivedi@gmail.com
authors.forename: Amit R
authors.initials: AR
authors.lastname: Trivedi
authors.forename: Dipti K
authors.initials: DK
authors.lastname: Dodiya
authors.forename: Bipin H
authors.initials: BH
authors.lastname: Dholariya
authors.forename: Vipul B
authors.initials: VB
authors.lastname: Kataria
authors.forename: Vimal R
authors.initials: VR
authors.lastname: Bhuva
authors.forename: Viresh H
authors.initials: VH
authors.lastname: Shah
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D004095:Dihydropyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000995:Antitubercular Agents; D004095:Dihydropyridines; C038806:1,4-dihydropyridine