title: Synthesis and anti-HIV-1 integrase activity of cyano pyrimidinones.
abstract: A series of 2-phenethyl/benzylthio-6-oxo-4-phenyl-1,6-dihydropyrimidine-5-carbonitrile were synthesized and tested against recombinant HIV-1 integrase in an enzyme assay. 2-(Phenethylthio)-4-(4-chlorophenyl)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile 4m and 2-(phenethylthio)-4-(3-chlorophenyl)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile 4o showed significant inhibition against integrase in the assay (strand transfer: IC(50) values of 16 and 17 microM, respectively).
authors.affiliation: Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan, The M.S. University of Baroda, Vadodara, India.
authors.forename: R
authors.initials: R
authors.lastname: Ramajayam
authors.forename: Nilesh B
authors.initials: NB
authors.lastname: Mahera
authors.forename: Nouri
authors.initials: N
authors.lastname: Neamati
authors.forename: Mange Ram
authors.initials: MR
authors.lastname: Yadav
authors.forename: Rajani
authors.initials: R
authors.lastname: Giridhar
mesh_terms: D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D015394:Molecular Structure; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D019428:HIV Integrase Inhibitors; D011744:Pyrimidinones