SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NEW QUINOLINE DERIVATIVES | ||||
| Zagazig Journal of Pharmaceutical Sciences | ||||
| Article 3, Volume 21, Issue 2, December 2012, Page 14-21 PDF (1.91 MB) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/zjps.2012.163470 | ||||
 View on SCiNiTO | ||||
| Authors | ||||
Lobna Abdel-Aziz  1; Kamel Metwaly2; El-Sayed Lashine2; Rania Badawy2
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| 1Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazige University, Zagazig, Egypt | ||||
| 2Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt | ||||
| Abstract | ||||
| Two series of novel quinoline derivatives; oxadiazolyl and thiadiazolyl quinolines were prepared and evaluated for their antimicrobial activities. The first series; 5-(2-aryl-6-substituted-4-quinolyl)-1.3,4-oxadiazol-2-amines (Va-g) was synthesized by cyclization of the key intermediate thiosemicarbazides (IV1-7). The second one; 5-(2-aryl-6-substituted-4-quinoly!)-1,3.4- thiadiazol-2-amines (VI a.c.f.g) was synthesized through cyclization of the key intermediate quinoline-4-carboxylic acids (I1-7) or from the synthetically accessible thiosemicarbazides (IV1-7).The target oxadiazole and thiadiazole derivatives were evaluated against Gram positive, Gram negative bacteria and fungi. The obtained results showed that the 1,3,4-thiadiazoles VI 4,8 exhibited the most potent antibacterial activity with MIC values of 4 µg/ml. | ||||
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