title: Synthesis and biological evaluation of novel series of aminopyrimidine derivatives as urease inhibitors and antimicrobial agents.
abstract: A novel series of carbazole substituted aminopyrimidines (5a-p) were synthesized and screened for their in vitro urease inhibition and antimicrobial activity. Among the compounds, 4-(2,4-dichlorophenyl)-6-(9-methyl-9H-carbazol-3-yl)-pyrimidin-2-amine (5i) was found to be the most potent showing urease inhibitory activity with an IC50 value 19.4 ± 0.43 µM. Compounds 5c, 5g, 5j and 5o showed good activity against all selected bacterial strains and compounds 5b, 5c, 5m and 5o showed good activity against selected fungal strains. All the compounds were subjected for ADME predictions by computational method.
authors.affiliation: Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University , Solapur, Maharashtra , India.
authors.forename: Laxman K
authors.initials: LK
authors.lastname: Adsul
authors.forename: Babasaheb P
authors.initials: BP
authors.lastname: Bandgar
authors.forename: Hemant V
authors.initials: HV
authors.lastname: Chavan
authors.forename: Shivkumar S
authors.initials: SS
authors.lastname: Jalde
authors.forename: Valmik D
authors.initials: VD
authors.lastname: Dhakane
authors.forename: Amol L
authors.initials: AL
authors.lastname: Shirfule
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D032449:Canavalia / Q000201:enzymology; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005658:Fungi / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014510:Urease / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D004791:Enzyme Inhibitors; D011743:Pyrimidines; D014510:Urease