title: Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
abstract: A series of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines (8-21) were synthesized in good yields by alkylation of 5-methyl-6-phenyl-2-thioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid ethyl esters (2-7) with different alkyl or aralkyl halides in the presence of a combination of anhydrous K(2)CO(3) and catalytic amount of tetrabutyl ammonium bromide. The title compounds were evaluated for their antifilarial activity against adult parasites of human lymphatic filarial parasite Brugia malayi (sub-periodic strain) in vitro and in vivo at various concentrations. One of the compounds (18) showed promising antifilarial activity.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, Uttar Pradesh, India.
authors.forename: B K
authors.initials: BK
authors.lastname: Singh
authors.forename: Mridul
authors.initials: M
authors.lastname: Mishra
authors.forename: Nisha
authors.initials: N
authors.lastname: Saxena
authors.forename: G P
authors.initials: GP
authors.lastname: Yadav
authors.forename: P R
authors.initials: PR
authors.lastname: Maulik
authors.forename: M K
authors.initials: MK
authors.lastname: Sahoo
authors.forename: R L
authors.initials: RL
authors.lastname: Gaur
authors.forename: P K
authors.initials: PK
authors.lastname: Murthy
authors.forename: R P
authors.initials: RP
authors.lastname: Tripathi
mesh_terms: D000478:Alkylation; D000818:Animals; D017178:Brugia malayi / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D005369:Filaricides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013237:Stereoisomerism
chemical_list: D005369:Filaricides; D011743:Pyrimidines