title: Synthesis of some novel 3-(1-(1-substitutedpiperidin-4-yl)-1H-1,2,3-triazol-4-yl)-5-substituted phenyl-1,2,4-oxadiazoles as antifungal agents.
abstract: A novel series of 3-(1-(1-substituted piperidin-4-yl)-1H-1,2,3-triazol-4-yl)-5-substituted phenyl-1,2,4-oxadiazoles bearing 1,2,3-triazole and piperidine ring has been synthesized in one step from amidoxime using Carbonyl diimidazole (CDI) and K(2)CO(3). All the synthesized compounds (4a-4r) are novel and evaluated for their in vitro antifungal activities. SAR for the series has been developed by comparing their MIC values with miconazole and fluconazole. Some of the compounds from the series like 4j was equipotent with miconazole against Cryptococcus neoformans whereas activities of compound 4m against Aspergillus niger and Aspergillus flavus were comparable to miconazole. Also compound 4r shows activity comparable to miconazole against Candida albicans, A. niger and A. flavus.
authors.affiliation: Department of Chemical Technology, Dr Babasaheb Ambedkar Marathwada University, Aurangabad, 431004 MS, India.
authors.forename: Jaiprakash N
authors.initials: JN
authors.lastname: Sangshetti
authors.forename: Devanand B
authors.initials: DB
authors.lastname: Shinde
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001565:Benzoates / Q000737:chemistry; D002254:Carbonates / Q000737:chemistry; D005658:Fungi / Q000187:drug effects*; D007093:Imidazoles / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011188:Potassium / Q000737:chemistry; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000935:Antifungal Agents; D001565:Benzoates; D002254:Carbonates; D007093:Imidazoles; D010069:Oxadiazoles; D014230:Triazoles; C037593:potassium carbonate; D011188:Potassium