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Bhole, R. P.
- Synthesis of 3,4-Dihydro-1H-Pyrimidine-5-Carbohydrazide Derivatives and Their Pharmacological Screening
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Affiliations
1 Sharad Pawar College of Pharmacy, Nagpur-441110, (MS), IN
2 RKDF College of Pharmacy, Bhopal (MP), IN
1 Sharad Pawar College of Pharmacy, Nagpur-441110, (MS), IN
2 RKDF College of Pharmacy, Bhopal (MP), IN
Source
Asian Journal of Research in Chemistry, Vol 3, No 3 (2010), Pagination: 531-538Abstract
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 2b, 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.Keywords
DOCA-Salt Hypertension, Non-Invasive Tail-Cuff Method, Carotid Artery Cannulation, Antihypertensive Activity, Anti-Inflammatory Activity, Ulcerogenic Activity, Nifedipine, Schiff Base.
- Design and Screening of PPAR-γ Agonist based Isatin Derivatives and its Remarkable Activity as Anti-Cancer and Anti-Diabetic
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Authors
Affiliations
1 Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, IN
1 Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, IN
Source
Research Journal of Pharmacy and Technology, Vol 12, No 4 (2019), Pagination: 2017-2026Abstract
Isatin are flexible compound, where it can be used for the preparation of a large number of substituted heterocyclic compounds, such as pyrazole, benzofuran, pyridazinone and sulphonamides. Sulphonamides is important class such as carbonic anhydrase inhibitors, antibacterial, antitumor, diuretic, hypo-glycemic, antidiabetic and anti-thyroid. In the past few decades, research has reached to the mark with an increased interest in capturing novel methodologies and targets that forcefully worked for the preparation isatin based sulphonamides derivatives. This review covers updated information of most of the active isatin based sulphonamides derivatives that have been shown considerable novel synthetic schemes as well as pharmacological and biological actions by targeting them on PPAR-γ agonist. From these considerations, ideas for future molecular modifications by different synthetic scheme leading to preparation of compounds with greater favorable pharmacological and biological properties may be derived.Keywords
Isatin Based Sulphonamides, PPAR-γ, Antitumor, Antidiabetic.References
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