Abstract
Synthesis and biological evaluation of new heterocyclic moiety N-(2-furylmethyleneamino)-3,4-dihydro-1H-pyrimidine-5- carboxamide derivatives
Author(s): P.A.Patil, K.P.Bhusari, R.P.Bhole, S.S.ChitlangeSix new3,4-Dihydro-1H-pyrimidine-5-carbohydrazideDerivatives (3a-f) have been synthesized in a three step reaction. In first step 5-(Ethoxycarbonyl)- 6-methyl-4-substitutedaryl-3,4-dihydropyrimidin-2(1H)-ones obtained (1af) and in second step 4-Substitutedaryl-6-methyl-2-pyrimidinone-5- Carbohydrazides (2a-f). Third step involves synthesis of 4-Substitutedaryl- 6-methyl-2-pyrimidinone-5-(N-p-tosyl) Carbohydrazides (3a-f). Their structures are confirmed by IR, 1H- NMR, C13NMR and Mass. The compounds were tested for antihypertensive activity by non-invasive tail-cuff, and evaluated by carotid artery cannulation method for determining the diastolic blood pressure. Hypertension was induced by DOCA-salt.Anti-inflammatory activitywas carried out by carrageenan induced rat-pawoedemamethod. Test compounds c1-8 exerted comparative anti-hypertensive activity at 10 mg/kg dose level compared to nifedipine. Compounds 3c, 3e, 3f and 2 b, 2c, 2f showed excellent results on evaluation by directmethod. Test compounds 3c, 3e and 2f exerted moderate to comparative anti-inflammatory activity at the 100 mg/kg dose level compared to indomethacin. Their further investigation for analgesic activity and acute ulcerogenesis was carried out, compounds 3b, 3c and 3e showed low ulcerogenic activity.
