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1.
Acta Pol Pharm ; 69(3): 433-8, 2012.
Article in English | MEDLINE | ID: mdl-22594257

ABSTRACT

In the present study, a series of (Z)-N-(1-[2-{3-[(dimethylamino)methyl)]-2-methoxyphenyl}-5-(pyridin-4-yl)-1,3,4-oxadiazol-3(2H)-yl]ethylidene)benzenamine derivatives have been synthesized and characterized by IR, 1H NMR and 13C NMR spectra. All the synthesized compounds were evaluated for their antifungal activity and were compared with the standard drug, clotrimazole. The compounds demonstrated excellent to weak antifungal activity. Among the synthesized derivatives, 4f and 4h showed significant activity and 4c exhibited moderate activity against Candida albicans, Candida tropicalis and Aspergillus niger as compared with the standard antifungal agent - clotrimazole. The minimum inhibitory concentration of the compounds was in the range of 1.62-25 microg/mL against fungi. Furthermore, the substitution of chloro, nitro and methoxy groups at para position of benzene moiety play an important role in enhancing the antifungal activity of this class of compounds.


Subject(s)
Amines/chemical synthesis , Amines/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/pharmacology , Benzene Derivatives/chemical synthesis , Benzene Derivatives/pharmacology , Fungi/drug effects , Amines/chemistry , Antifungal Agents/chemistry , Benzene Derivatives/chemistry , Microbial Sensitivity Tests/methods , Oxadiazoles/chemical synthesis , Oxadiazoles/chemistry , Oxadiazoles/pharmacology
2.
Acta Pol Pharm ; 69(2): 363-8, 2012.
Article in English | MEDLINE | ID: mdl-22568053

ABSTRACT

Seventeen analogues of benzylidene were synthesized and evaluated for in vitro hydrogen peroxide scavenging activity. The structure of the newly synthesized compounds were confirmed by elemental and spectral (IR, 1H-NMR, 13C-NMR) studies. The antioxidant activity of the titled compounds was evaluated. Compounds: 4h--N'-[2-amino-3-(morpholinomethyl)benzylidene]isonicotinohydrazide, 4p 7-(4-(2-amino-3-[(2-isonicotinoylhydrazono)methyl]benzyl}piperazin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquino- line-3-carboxylic acid and 4q 7-(4-{2-amino-3-[(2 isonicotinoylhydrazono)methyl]benzyl} piperazin-1-yl)-1-ethyl-6,8-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid were the most active compounds with significant hydrogen peroxide scavenging activity.


Subject(s)
Antioxidants/chemical synthesis , Benzylidene Compounds/chemical synthesis , Antioxidants/chemistry , Antioxidants/pharmacology , Benzylidene Compounds/chemistry , Benzylidene Compounds/pharmacology , Magnetic Resonance Spectroscopy
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