P.A. Patil, R.P. Bhole, R.V. Chikhale, K.P. Bhusari, Amol Chandekar
P.A. Patil1*, R.P. Bhole1, R.V. Chikhale1, K.P. Bhusari1 and Amol Chandekar2
1Sharad Pawar College of Pharmacy, Nagpur-441 110, (MS) India
2RKDF College of Pharmacy, Bhopal (MP)
Volume - 3,
Issue - 3,
Year - 2010
Six new 3,4-Dihydro-1H-pyrimidine-5-carbohydrazide Derivatives (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 (1a-f) 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 activity was carried out by carrageenan induced rat-paw oedema method. 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 direct method. 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.
DOCA-salt hypertension; Non-invasive tail-cuff method; Carotid artery cannulation; Antihypertensive activity; Anti-inflammatory activity; Ulcerogenic activity, nifedipine, Schiff base.
Cite this article:
P.A. Patil, R.P. Bhole, R.V. Chikhale, K.P. Bhusari, Amol Chandekar. Synthesis of 3, 4-Dihydro-1H-Pyrimidine-5-Carbohydrazide Derivatives and their Pharmacological Screening. Asian J. Research Chem. 3(3): July- Sept. 2010; Page 531-538.