title: Convenient synthesis of novel 4-substitutedamino-5-trifluoromethyl-2,7-disubstituted pyrido[2,3-d] pyrimidines and their antibacterial activity.
abstract: Novel pyrido[2,3-d]pyrimidines 4 have been synthesised starting from 2-amino-4-trifluoromethyl-6-substituted nicotinonitriles 1 via imine formation, selective amination followed by Dimroth rearrangement. Compounds 4 were screened against Gram +ve and -ve bacteria in vitro. Compounds 4h and 4d showed significant activity against all species of Gram positive bacteria and moderate activity against Gram negative bacteria. N-2,4 difluorophenyl compounds 4l and 4m were the least active among all the compounds. All the compounds were inactive against Pseudomonas aeruginosa at the maximum concentration of 200 microg ml(-1).
authors.affiliation: Fluoroorganics Division, Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: S
authors.initials: S
authors.lastname: Ravi Kantha
authors.forename: G
authors.initials: G
authors.lastname: Venkat Reddy
authors.forename: K
authors.initials: K
authors.lastname: Hara Kishore
authors.forename: P
authors.initials: P
authors.lastname: Shanthan Rao
authors.forename: B
authors.initials: B
authors.lastname: Narsaiaha
authors.forename: U
authors.initials: U
authors.lastname: Surya Narayana Murthy
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared
chemical_list: D000900:Anti-Bacterial Agents; D011743:Pyrimidines