title: Synthesis, characterization and biological evaluation of novel 2,4,6-trisubstituted bis-pyrimidine derivatives.
abstract: A new series of 2,4,6-trisubstituted bis-pyrimidines were synthesized and evaluated for in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. Out of 16 compounds 8 compounds have shown IC(50) values in the range of 0.10-1.86 μM. Bis-pyrimidine having methyl-, methoxy-, thiomethyl- and dimehyl-phenyl substituents, exhibited higher antiamoebic activity than the reference drug metronidazole (IC(50) = 1.9 μM). The toxicological studies of active compounds on PC12-rat pheochoromocytoma cell line showed that all compounds were non-toxic at a concentration of 100 μM. 4-4'-Benzene-1,3-diylbis[6-(4-methylphenyl-2-(piperidin-1-yl)pyrimidine] (4c) was found most active (IC(50) = 0.10 μM) and least toxic among all the compounds.
authors.affiliation: Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India. humaira_chem@yahoo.co.in
authors.forename: Humaira
authors.initials: H
authors.lastname: Parveen
authors.forename: Faisal
authors.initials: F
authors.lastname: Hayat
authors.forename: Sayeed
authors.initials: S
authors.lastname: Mukhtar
authors.forename: Attar
authors.initials: A
authors.lastname: Salahuddin
authors.forename: Andleeb
authors.initials: A
authors.lastname: Khan
authors.forename: Fakhrul
authors.initials: F
authors.lastname: Islam
authors.forename: Amir
authors.initials: A
authors.lastname: Azam
mesh_terms: D000818:Animals; D004748:Entamoeba histolytica / Q000187:drug effects; D020128:Inhibitory Concentration 50; D016716:PC12 Cells; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013057:Spectrum Analysis
chemical_list: D011743:Pyrimidines