title: One pot synthesis and biological activity evaluation of novel Schiff bases derived from 2-hydrazinyl-1,3,4-thiadiazole.
abstract: Considering the structural features of a group of known potent inhibitors of human platelet aggregation containing hydrazone structural backbone, a series of novel hydrazone derivatives of 2-hydrazinyl-1,3,4-thiadiazole were synthesized using a one-pot process and tested for their inhibitory activity against platelet aggregation induced by arachidonic acid and ADP. Among the derivatives, compounds 3l, 3o and 3p exhibited the highest antiplatelet aggregation activity. The derivatives were also screened for their potential antimycobacterial activity and compounds 3g, 3k, 3p and 3q were among the most active compounds.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Vali Asr Ave. Niayesh Junction, Tehran P.O. Box 14155-6153, Iran.
authors.forename: Kamaleddin
authors.initials: K
authors.lastname: Haj Mohammad Ebrahim Tehrani
authors.forename: Soroush
authors.initials: S
authors.lastname: Sardari
authors.forename: Vida
authors.initials: V
authors.lastname: Mashayekhi
authors.forename: Marjan
authors.initials: M
authors.lastname: Esfahani Zadeh
authors.forename: Parisa
authors.initials: P
authors.lastname: Azerang
authors.forename: Farzad
authors.initials: F
authors.lastname: Kobarfard
mesh_terms: D000244:Adenosine Diphosphate / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D016718:Arachidonic Acid / Q000037:antagonists & inhibitors / Q000494:pharmacology; D006801:Humans; D006835:Hydrazones / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D009163:Mycobacterium bovis / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012545:Schiff Bases / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013830:Thiadiazoles / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D006835:Hydrazones; D010975:Platelet Aggregation Inhibitors; D012545:Schiff Bases; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate