Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole
Journal Title: Advanced Pharmaceutical Bulletin - Year 2012, Vol 2, Issue 2
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 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). Conclusion: Ten noveldihydropyrimidine analogues has been synthesized, characterized and found to bepromising antibacterial, anticonvulsant and antitumor agents.
Authors and Affiliations
Shantaram Gajanan Khanage, S. Appala Raju, Popat Baban Mohite, Ramdas Bhanudas Pandhare
Keywords
Related Articles
- EP ID EP119949
- DOI 10.5681/apb.2012.033
- Views 94
- Downloads 0
Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole
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 ag...
Dose-Dependent Effect of Flouxetine on 6-OHDA-Induced Catalepsy in Male Rats: A Possible Involvement of 5-HT1A Receptors
Purpose: Progressive loss of dopaminergic neurons of the substantia nigra pars compacta (SNc) in Parkinson’s disease (PD) leads to impairment of motor skills. Several evidences show that the role of serotonergic system i...
Resistance to Reperfusion Injury Following Short Term Postischemic Administration of Natural Honey in Globally Ischemic Isolated Rat Heart
Purpose: Results of our previous study revealed that preischemic perfusion of honey before zero flow global ischemia had cardioprotective effects in rat. The present study investigated potential resistance to reperfusion...
Protective Effect against Hydroxyl-induced DNA Damage and Antioxidant Activity of Radix Glycyrrhizae (Liquorice Root)
Purpose: As a typical Chinese herbal medicine, Radix Glycyrrhizae (RG) possesses various pharmacological effects involved in antioxidant ability. However, its antioxidant has not been explored so far. The aim of the stud...
Lactose Engineering for Better Performance in Dry Powder Inhalers
Dry powder inhaler (DPI) is generally formulated as a powder mixture of coarse carrier particles and micronized drug with aerodynamic diameters of 1-5 μm. Carrier particles are used to improve drug particle flowability,...