Khanage Shantaram Gajanan, Raju S Appala, Mohite Popat Baban, Pandhare Ramdas Bhanudas
Research scholar, Department of Pharmacy,Vinayaka Missions University, Salem, Sankari main road, NH-47,Tamilnadu, India.
Adv Pharm Bull. 2012;2(2):213-22. doi: 10.5681/apb.2012.033. Epub 2012 Aug 15.
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.
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(-5) M.
Compound 4b, 4c, 4d, 4i and 4j were exhibited significant antimicrobial potential against tested strains at 50μg/ml and 100μg/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).
Ten noveldihydropyrimidine analogues has been synthesized, characterized and found to bepromising antibacterial, anticonvulsant and antitumor agents.
已描述了一种高效合成6 -（取代芳基）-4 -（3,5 - 二苯基-1H - 1,2,4 - 三唑-1 - 基）-1,6 - 二氢嘧啶-2 - 硫醇的方法，该化合物是一种有益的抗菌、抗惊厥和抗癌剂。
通过三步合成标题化合物的查耳酮，随后这些查耳酮在乙醇中KOH存在下与硫脲进一步反应，生成二氢嘧啶衍生物（4a - j）。通过琼脂孔法筛选化合物4a - j的体外抗菌活性，并通过MES模型筛选其抗惊厥活性。在美国马里兰州国立癌症研究所对两种新合成的杂环化合物以10⁻⁵ M的单剂量针对60种不同人类肿瘤细胞系评估其抗癌活性。
化合物4b、4c、4d、4i和4j在50μg/ml和100μg/ml浓度下对测试菌株表现出显著的抗菌潜力。在所研究的十种化合物中，4a、4b、4c、4h和4j在0.5小时后显示出与苯妥英和卡马西平相当的MES活性。4小时后，测试化合物的效力未显示比标准药物更强。发现化合物4a和4d对非小细胞肺癌（HOP - 92）有活性。
已合成、表征了十种新型二氢嘧啶类似物，发现它们是有前景的抗菌、抗惊厥和抗肿瘤剂。
