Synthesis of new 2-substituted pyrido[2,3-d]pyrimidin-4(1H)-ones and their antibacterial activity☆

European Journal of Medicinal Chemistry
2009.0

Abstract

2-Substituted-5,7-dimethyl pyrido[2,3-d]pyrimidin-4(1H)-ones (8) were synthesized by oxidation of 2-substituted-5,7-dimethyl dihydropyrido[2,3-d]pyrimidin-4(1H)-ones (7) which were in turn prepared from 2-amino-4,6-dimethyl nicotinamide (5) and substituted aryl aldehydes (6). 2-Amino-4,6-dimethyl nicotinamide (5) was prepared from ethyl cyanoacetate (1) via malonamamidine hydrochloride (3). The compounds were characterized by IR, NMR, MS and elemental analyses. Compounds 7 and 8 were screened for antibacterial activity against gram positive and gram negative bacteria. Dehydrogenated compounds (8) showed less antibacterial activity than the compounds 7. Among all the test compounds screened for antibacterial activity 7c (1.25 microg/ml) showed greater activity. All the synthesized compounds were found inactive when screened for antifungal activity at the concentration of 200 microg/ml.

Knowledge Graph

Similar Paper

Synthesis of new 2-substituted pyrido[2,3-d]pyrimidin-4(1H)-ones and their antibacterial activity☆
European Journal of Medicinal Chemistry 2009.0
Synthesis and anti-microbial activity of some 1- substituted amino-4,6-dimethyl-2-oxo-pyridine-3-carbonitrile derivatives
European Journal of Medicinal Chemistry 2011.0
Synthesis and antimicrobial activity of novel pyrazolo[3,4-d]pyrimidin derivatives
European Journal of Medicinal Chemistry 2010.0
Synthesis of pyrazole encompassing 2-pyridone derivatives as antibacterial agents
Bioorganic & Medicinal Chemistry Letters 2013.0
Synthesis, characterization, crystal structure determination and biological screening of novel N-1 and C5 alkyl substituted scaffolds of pyrimidine
European Journal of Medicinal Chemistry 2015.0
A search of novel antimicrobial based on benzimidazole and 2-pyridone heterocycles
Medicinal Chemistry Research 2012.0
Organoiodine (III)-mediated synthesis of 3-aryl/heteroaryl-5,7-dimethyl-1,2,4-triazolo[4,3-c]pyrimidines as antibacterial agents
European Journal of Medicinal Chemistry 2009.0
Synthesis and antimicrobial activity of new pyridine derivatives-I
Medicinal Chemistry Research 2011.0
Further derivatives of 4-benzoyl-1,5-diphenyl-1H-pyrazole-3-carboxylic acid and their antibacterial activities
Medicinal Chemistry Research 2007.0
Synthesis of new series of pyrazolo[4,3-d]pyrimidin-7-ones and pyrido[2,3-d]pyrimidin-4-ones for their bacterial and cyclin-dependent kinases (CDKs) inhibitory activities
Medicinal Chemistry Research 2011.0