Design, synthesis and in vitro evaluation of antitubercular and antimicrobial activity of some novel pyranopyrimidines

The clinical significance of pyran and pyrimidine condensed systems and the raise in problem of multidrug resistant bacterial pathogens has directed us to synthesize pyranopyrimidine derivatives via the reactions of the versatile, 2-amino-4-(4-methoxyphenyl)-4 H-substitutedchromene-3-carbonitrile wi...

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Bibliographic Details
Published in:	European journal of medicinal chemistry Vol. 45; no. 11; pp. 5056 - 5063
Main Authors:	Kamdar, Nimesh R., Haveliwala, Dhaval D., Mistry, Prashant T., Patel, Saurabh K.
Format:	Journal Article
Language:	English
Published:	Kidlington Elsevier Masson SAS 01-11-2010 Elsevier
Subjects:	Anti-Infective Agents - chemistry Anti-Infective Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Antimicrobial activity Antitubercular activity Aspergillus niger - drug effects Bacteria - drug effects Biological and medical sciences Drug Design Drug Evaluation, Preclinical General aspects Magnetic Resonance Spectroscopy Medical sciences Microbial Sensitivity Tests Pharmacology. Drug treatments Pyranopyrimidine Pyrimidine thiones Pyrimidines - chemistry Pyrimidines - pharmacology Pyrimidone Pyrimidone Antimicrobial activity Pyranopyrimidine Antitubercular activity Pyrimidine thiones Lactam Thiolactam Tricyclic compound Thioureas In vitro Antimicrobial agent Antifungal agent Structure activity relation Antituberculous agent Aromatic compound Antibacterial agent Chemical synthesis Oxygen nitrogen heterocycle
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Summary:	The clinical significance of pyran and pyrimidine condensed systems and the raise in problem of multidrug resistant bacterial pathogens has directed us to synthesize pyranopyrimidine derivatives via the reactions of the versatile, 2-amino-4-(4-methoxyphenyl)-4 H-substitutedchromene-3-carbonitrile with the appropriate reagents. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, Mass spectra and Elemental analysis. The compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H 37 Rv [ATCC-27294] and antibacterial activity against Staphylococcus aureus [ATCC-25923] and Streptococcus pyogenes [MTCC-443] as Gram-positive, Escherichia coli [ATCC-25922] and Pseudomonas aeruginosa [MTCC-441] as Gram-negative bacterial strains and antifungal activity against Aspergillus niger [MTCC-282]. Several derivatives exhibited pronounced antitubercular and antimicrobial activities. [Display omitted]
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0223-5234 1768-3254
DOI:	10.1016/j.ejmech.2010.08.014