Synthesis and biological evaluation of certain 2H-pyran-2-ones and some derived 1H-pyridin-2-one analogs as antimicrobial agents

Pyran-2-one and pyridine-2-one analogs are known to be biological versatile compounds possessing variety of pharmacological activities. Some 4-[4-nitrophenyl]-5,6-diphenyl-pyran-2-ones and their 1H-pyridin-2-one analogs were synthesized and evaluated for their in vitro antimicrobial activities. The chemistry of the reactions employed for the synthesis of the intermediates and target compounds was discussed. The results revealed that some compounds exhibited promising antibacterial and antifungal activities. Compound 8; 1-hydroxy-4-[4-nitrophenyl]-5,6-diphenyl-1H-pyridin-2-one; showed the most potent broad spectrum antimicrobial activity. 1-Methyl-4-[4-nitrophenyl]-5,6-diphenyl-1H-pyridin-2-thione 12; was able to exert weak growth inhibitory effect against the Mycobacterium tuberculosis

In vitro antitumour screening of some polysubstituted pyrazole analogs

Certain 1-[4-chlorophenyl]-4-hydroxy-1H-pyrazole-3-carboxylic acid hydrazide derivatives, carrying various substituents at position 3- such as 1,2,4-triazolyl and 1,2,4-oxadiazolyl moieties have been previously synthesized and preliminarily evaluated for their antitumor activity at the National Cancer Institute's [NCI] in vitro disease-oriented antitumor screen unit. In the primary 60 cell line assay, three compounds [1-3] revealed potential broad spectrum antitumor activity against a wide range of different human cell lines of nine tumor subpanels. These compounds were further selected by the NCI for carrying out confirmatory screening procedures in order to assess their exact in vitro antitumor potentialities. A detailed discussion of the best in vitro antitumor results of these active analogs obtained from the three consecutive NCI procedures is reported in this paper. The active three compounds at the GI50 level exhibited TGI and LC50 levels with nearly the same order of activity; 3> 2> 1