title: Expeditious Synthesis, Antimicrobial and Antimalarial Activities of Novel Heterocycles Bearing Imidazole-oxadiazole Based Hybrid Pharmacophores.
abstract: A facile synthesis of 2-substituted-5-amino-oxadiazole derivatives has been achieved by refluxing/sonicating a mixture of semicarbazide with various aromatic acids in conc. sulphuric acid alone. The isolated products were further condensed withp-dimethylaminobenzaldehyde/p-hydroxybenzaldehyde to obtain respective imino derivatives. Finally, some potentially biologically active imidazole analogues were obtained by reacting ammonium acetate and 5-bromoisatin with the synthesized imino products. All the newly synthesized compounds were thoroughly characterized by standard analytical techniques. These imidazole-oxadiazole hybrid compounds were also evaluated for their antimicrobial and antimalarial activities. The compounds all exhibited moderate to significant antimicrobial activity (6-10 mm, zone of inhibition) and promising antimalarial activity (IC500.037-0.100 µM). This report entails a detailed synthetic procedure, spectroscopic elucidation and activities of the synthesized compounds.
authors.affiliation: Department of Chemistry, GIS, GITAM University, Visakhapatnam, India.
authors.forename: K
authors.initials: K
authors.lastname: Balaji
authors.affiliation: Department of Chemistry, GIS, GITAM University, Visakhapatnam, India.
authors.forename: P
authors.initials: P
authors.lastname: Bhatt
authors.affiliation: Department of Chemistry, GIS, GITAM University, Visakhapatnam, India.
authors.forename: A
authors.initials: A
authors.lastname: Jha
mesh_terms: D000085:Acetates / Q000737:chemistry; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology; D007510:Isatin / Q000031:analogs & derivatives / Q000737:chemistry; D010069:Oxadiazoles / Q000737:chemistry* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000085:Acetates; D000890:Anti-Infective Agents; D000962:Antimalarials; D006571:Heterocyclic Compounds; D007093:Imidazoles; D010069:Oxadiazoles; C029899:imidazole; D007510:Isatin; C044414:5-bromoisatin; C018824:ammonium acetate