title: Synthesis and pharmacological evaluation of some new pyrimidine derivatives containing 1,2,4-triazole.
abstract: OBJECTIVE
  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(-5) M.
  
  
  RESULTS
  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).
  
  
  CONCLUSIONS
  Ten noveldihydropyrimidine analogues has been synthesized, characterized and found to bepromising antibacterial, anticonvulsant and antitumor agents.
authors: Research scholar, Department of Pharmacy,Vinayaka Missions University, Salem, Sankari main road, NH-47,Tamilnadu, India.
authors: Shantaram Gajanan
authors: SG
authors: Khanage
authors: S Appala
authors: SA
authors: Raju
authors: Popat Baban
authors: PB
authors: Mohite
authors: Ramdas Bhanudas
authors: RB
authors: Pandhare
keywords: Antimicrobial activity; Antitumor agent; Chalcones; Condensation; Dihydropyrimidine; MES activity