title: Synthesis and in vitro anti-leishmanial activity of 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]- and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines.
abstract: The synthesis and anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds including 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines were described. Most of the synthesized compounds exhibited potent anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major at non-cytotoxic concentrations. In general, 5-nitrofuran derivatives were more active than the corresponding 5-nitrothiophene analogues.
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy & Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.
authors.forename: Mina
authors.initials: M
authors.lastname: Behrouzi-Fardmoghadam
authors.forename: Fatemeh
authors.initials: F
authors.lastname: Poorrajab
authors.forename: Sussan Kaboudanian
authors.initials: SK
authors.lastname: Ardestani
authors.forename: Saeed
authors.initials: S
authors.lastname: Emami
authors.forename: Abbas
authors.initials: A
authors.lastname: Shafiee
authors.forename: Alireza
authors.initials: A
authors.lastname: Foroumadi
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D005663:Furans / Q000737:chemistry; D018320:Leishmania major / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D017672:Nitrogen Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry*
chemical_list: D000981:Antiprotozoal Agents; D005663:Furans; D017672:Nitrogen Compounds; D010879:Piperazines; D013844:Thiazoles; D000077489:Piperazine; C039281:furan