SYNTHESIS, IN VITRO ANTIMICROBIAL, ANTI-LIVER CANCER EVALUATION OF SOME NOVEL BIS-CYANOACRYLAMIDE AND BIS-AZOLES DERIVATIVES

Kheder, Nabila and ALTALBAWY, FARAG M. A. (2015) SYNTHESIS, IN VITRO ANTIMICROBIAL, ANTI-LIVER CANCER EVALUATION OF SOME NOVEL BIS-CYANOACRYLAMIDE AND BIS-AZOLES DERIVATIVES. SYNTHESIS, IN VITRO ANTIMICROBIAL, ANTI-LIVER CANCER EVALUATION OF SOME NOVEL BIS-CYANOACRYLAMIDE AND BIS-AZOLES DERIVATIVES. pp. 420-427. ISSN 0975-1491

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Abstract

ABSTRACT Objective: Synthesis of some novel bis [3-(aryl)-2-cyanoacrylamide], bis-pyrazole, bis-thiazole and bis-triazole derivatives starting from N,N'-ethane-1,2-diylbis(2-cyanoacetamide) (1) to evaluate for their in-vitro antibacterial, antifungal and anticancer activities. Methods: Reaction of N, N'-ethane-1,2-diylbis(2-cyanoacetamide) (1) with different aromatic and heteroaromatic aldehydes yielded the corresponding bis[3-(aryl)-2-cyanoacrylamide] derivatives, which reacted with hydrazine hydrate to give N,N'-ethane-1,2-diylbis[3-amino-5-(4-aryl)-1H-pyrazole-4-carboxamide] derivatives. Compound 1 reacted with each of thioglycolic acid, Phenyl isocyanate and elemental sulfur in presence triethylamine to give bis-thiazole derivatives. Diazotization of 1 with the desired diazonium chloride yielded the bis-hydrazone derivatives. The latter compounds refluxed with hydroxylamine hydrochloride and chloro- acetonitrile to give bis-triazole and bis-pyrazole derivatives respectively. Results: The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H NMR, [13]C NMR and mass spectral data. A total fourteen new synthesized compounds were evaluated for their in-vitro antibacterial, antifungal and anticancer activities against human liver cancer cell line (HEPG-2). Conclusion: The results obtained indicated that some of such compounds showed promising activities against Gram-positive, Gram-

Item Type: Article
Subjects: Pharmacy
Divisions: College of Pharmacy > Pharmacy
Depositing User: NABILA MOHAMMED
Date Deposited: 20 Aug 2017 08:42
Last Modified: 20 Aug 2017 08:42
URI: http://eprints.kku.edu.sa/id/eprint/890

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