title: Synthesis of 1H-1,2,3-triazole linked β-lactam-isatin bi-functional hybrids and preliminary analysis of in vitro activity against the protozoal parasite Trichomonas vaginalis.
abstract: Twenty-two different triazoles were prepared to examine the anti-Trichomonas vaginalis structure-activity relationships (SAR) within the β-lactam-isatin-triazole conjugate family. The compounds were synthesized by copper-catalyzed 'click chemistry.'In vitro activity against T. vaginalis was determined at 10 and 100 μM for each compound, with eighteen of the synthesized hybrids showing 100% growth inhibition at 100 μM. The compound 5i, with no cytotoxicity on cultured CHO-K1 cells, is considered a good compound for further analysis.
authors: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
authors: Raghu
authors: R
authors: Raj
authors: Pardeep
authors: P
authors: Singh
authors: Nathan T
authors: NT
authors: Haberkern
authors: Ryan M
authors: RM
authors: Faucher
authors: Neal
authors: N
authors: Patel
authors: Kirkwood M
authors: KM
authors: Land
authors: Vipan
authors: V
authors: Kumar
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016466:CHO Cells; D002470:Cell Survival / Q000187:drug effects; D006224:Cricetinae; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D020128:Inhibitory Concentration 50; D007510:Isatin / Q000737:chemistry*; D008956:Models, Chemical; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014246:Trichomonas vaginalis / Q000187:drug effects; D047090:beta-Lactams / Q000737:chemistry*
chemical_list: D000981:Antiprotozoal Agents; D014230:Triazoles; D047090:beta-Lactams; D007510:Isatin