title: Synthesis and antimicrobial evaluation of ester-linked 1,4-disubstituted 1,2,3-triazoles with a furyl/thienyl moiety.
abstract: Twenty ester-linked 1,4-disubstituted 1,2,3-triazoles having a furyl/thienyl moiety have been synthesized from heteroaryl prop-2-yn-1-yl carboxylate and aromatic azides via a Cu(I) catalyzed 1,3-dipolar cycloaddition. All the synthesized compounds were characterized by FTIR, [Formula: see text]H NMR, [Formula: see text]C NMR spectroscopy and HRMS. Synthesized triazoles were tested in vitro for antimicrobial evaluation against Gram-negative bacteria-Escherichia coli, Enterobacter aerogenes and Klebsiella pneumoniae; Gram-positive bacteria-Staphylococcus aureus and two fungal strains-Candida albicans and Aspergillus niger, reflecting moderate to good activity. The structure of compound 6f was also confirmed by X-ray crystallography (CCDC 1469326).
authors.affiliation: Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India. kaushikcp@gmail.com.
authors.forename: C P
authors.initials: CP
authors.lastname: Kaushik
authors.affiliation: Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.
authors.forename: Raj
authors.initials: R
authors.lastname: Luxmi
authors.affiliation: Centre for Research & Development, IPCA Lab Ltd., Kandivali, Mumbai, Maharashtra, India.
authors.forename: Dharmendra
authors.initials: D
authors.lastname: Singh
authors.affiliation: Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.
authors.forename: Ashwani
authors.initials: A
authors.lastname: Kumar
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001234:Aspergillus niger / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D020134:Catalytic Domain; D060326:Chemistry Techniques, Synthetic; D027081:DNA Gyrase / Q000737:chemistry / Q000378:metabolism; D004952:Esters / Q000737:chemistry*; D005663:Furans / Q000737:chemistry*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D062105:Molecular Docking Simulation; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D000890:Anti-Infective Agents; D004952:Esters; D005663:Furans; D014230:Triazoles; D027081:DNA Gyrase; C039281:furan
keywords: Antibacterial activity; Antifungal activity; Click chemistry; Disubstituted 1,2,3-triazoles; Synthesis