title: Synthesis and antitrypanosomal activity of new 6,6,7-trisubstituted thiopyrano[2,3-d][1,3]thiazoles.
abstract: А series of novel 6,6,7-trisubstituted thiopyrano[2,3-d][1,3]thiazoles-based molecules have been synthesized and evaluated as potential antitrypanosomal agents. The most active analogue 3b inhibited Trypanosoma brucei brucei and Trypanosoma brucei gambiense with an IC(50) of 0.26 and 0.42 μМ, respectively. They could be considered as potent hits for further antitrypanosomal drug discovery efforts.
authors.affiliation: Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, 69 Pekarska, Lviv 79010, Ukraine.
authors.forename: Nataliya
authors.initials: N
authors.lastname: Zelisko
authors.forename: Dmytro
authors.initials: D
authors.lastname: Atamanyuk
authors.forename: Olexandr
authors.initials: O
authors.lastname: Vasylenko
authors.forename: Philippe
authors.initials: P
authors.lastname: Grellier
authors.forename: Roman
authors.initials: R
authors.lastname: Lesyk
mesh_terms: D006801:Humans; D011714:Pyrans / Q000737:chemistry*; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013438:Sulfhydryl Compounds / Q000737:chemistry*; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014347:Trypanosoma brucei gambiense / Q000187:drug effects
chemical_list: D011714:Pyrans; D011759:Pyrrolidines; D013438:Sulfhydryl Compounds; D013844:Thiazoles; D014344:Trypanocidal Agents; C579644:rel-(6'R,7'R)-7'-(3,4-dimethoxyphenyl)-1-(4-chlorophenyl)-3',7'-dihydro-2H,2'H,5H-spiro(pyrolidin-3,6'-thiopyrano(2,3-d)thiazol)-2,2',5-trione; C522033:thiopyran