مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

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Information Journal Paper

Title

SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF SOME NEW PYRIMIDINE DERIVATIVES CONTAINING 1,2,4-TRIAZOLE

Pages

  213-222

Abstract

 Purpose: An efficient method has been described for synthesis of 6- (substituted aryl) -4- (3, 5-diphenyl-1H-1, 2, 4-triazol-1-yl) -1, 6-dihydropyrimidine-2-thiol, as a beneficial antimicrobial, anticonvulsant and anticancer agents.Methods: The clalcones of title compounds were synthesized in three steps and subsequently these CHALCONES were further reacted with thiourea in the presence of KOH in ethanol, which led to the formation of DIHYDROPYRIMIDINE derivatives (4a-j). Compounds 4a-j were screened for their in vitro ANTIMICROBIAL ACTIVITY by agar well method and their anticonvulsant activity by the MES model. Anticancer activity of two newly synthesized heterocycles were evaluated at National Cancer Institute (NCI) Maryland, USA against 60 cell lines of different human tumor at a single dose of 10-5M.Results: Compound 4b, 4c, 4d, 4i and 4j were exhibited significant antimicrobial potential against tested strains at 50 mg/ml and 100 mg/ml concentrations. Out of the ten compounds studied 4a, 4b, 4c, 4h and 4j showed comparable MES ACTIVITY to Phenytoin and Carbamazepine after 0.5h. Tested compounds did not showed to be more potent than standard drugs after 4h. Compound 4a and 4d were found active on Non-Small Cell Lung Cancer (HOP-92).Conclusion: Ten noveldihydropyrimidine analogues has been synthesized, characterized and found to bepromising antibacterial, anticonvulsant and ANTITUMOR AGENTs.

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    • Cite

    APA: Copy

    GAJANAN KHANAGE, SHANTARAM, APPALA RAJU, S., BABAN MOHITE, POPAT, & BHANUDAS PANDHARE, RAMDAS. (2012). SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF SOME NEW PYRIMIDINE DERIVATIVES CONTAINING 1,2,4-TRIAZOLE. ADVANCED PHARMACEUTICAL BULLETIN, 2(2), 213-222. SID. https://sid.ir/paper/331656/en

    Vancouver: Copy

    GAJANAN KHANAGE SHANTARAM, APPALA RAJU S., BABAN MOHITE POPAT, BHANUDAS PANDHARE RAMDAS. SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF SOME NEW PYRIMIDINE DERIVATIVES CONTAINING 1,2,4-TRIAZOLE. ADVANCED PHARMACEUTICAL BULLETIN[Internet]. 2012;2(2):213-222. Available from: https://sid.ir/paper/331656/en

    IEEE: Copy

    SHANTARAM GAJANAN KHANAGE, S. APPALA RAJU, POPAT BABAN MOHITE, and RAMDAS BHANUDAS PANDHARE, “SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF SOME NEW PYRIMIDINE DERIVATIVES CONTAINING 1,2,4-TRIAZOLE,” ADVANCED PHARMACEUTICAL BULLETIN, vol. 2, no. 2, pp. 213–222, 2012, [Online]. Available: https://sid.ir/paper/331656/en

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