Informatics Publishing Limited

Nachiket S. Dighe ¹, Ravindra B. Saudagar ², Ramesh S. Kalkotwar ³, D. A. Jain ⁴

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Loni, MS -413736, IN
2 Department of Pharmaceutical Chemistry, R.G. Sapkal College of Pharmacy, Nashik, M.S, IN
3 Department of Pharmaceutical Chemistry, S.N.D. College of Pharmacy, Yeola, Dist-Nashik, MS, IN
4 Department of Pharmaceutical Sciences and Research, Bhagwant University, Ajmer, Rajasthan, IN

Abstract

Mercaptooxadiazole is a five membered heterocyclic system consists of two nitrogen and one oxygen atoms along with acidic thiol group. As it increases the acidity of the titled compounds. It can be easily synthesized from hydazides using potassium hydroxide in presence of carbon disulphide. Mercaptooxadiazoles posses wide spectrum of biological activities like antibacterial, antifungal, antiviral, anti-inflammatory, anticonvulsant, antidepressant, antihypertensive, analgesic, and hypoglycemic properties. The present review is an attempt made to reveal the therapeutic and synthetic profiles of the mercaptooxadiazole ring.

Keywords

Mercaptooxadiazole, Synthesis, Biological Evaluation.

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Nachiket S. Dighe ¹, Ravindra B. Saudagar ², Ramesh S. Kalkotwar ³, D. A. Jain ⁴

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Loni, MS-413736, IN
2 Department of Pharmaceutical Chemistry, R.G.Sapkal College of Pharmacy, Nashik, M.S., IN
3 Department of pharmaceutical Chemistry, S.N.D. College of Pharmacy, Yeola, Dist-Nashik, MS, IN
4 Department of Pharmaceutical Sciences and Research, Bhagwant University, Ajmer, Rajasthan, IN

Abstract

Triazole is a five membered heterocyclic system consisting of two carbon atoms and three nitrogen atoms shows wide range of biological activities. Triazoles can be synthesized using Einhorn-Brunner reaction or the Pellizzari reaction from acyl hydrazides. Triazoles posses wide spectrum of biological activities like including antibacterial, antifungal, antiviral, anti-inflammatory, anticonvulsant, antidepressant, antihypertensive, analgesic, and hypoglycemic properties. The present reviews attempted to gather the various developments in synthesis and biological activities of triazole derivatives.

Keywords

1, 2, 4-Triazole, Pharmacological Activity, SAR, Total Synthesis.

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Ravindra B. Saudagar ¹, Nachiket S. Dighe ², Deepak S. Musmade ³, Vinayak M. Gaware ⁴, D. A. Jain ⁵

Affiliations
1 Department of Pharmaceutical Chemistry, R.G. Sapkal College of Pharmacy, Nashik, M.S., IN
2 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Loni-413736, MS, IN
3 Department of Pharmaceutical Chemistry, Sanjivani College of Pharmaceutical Education and Research, Kopargaon, MS, IN
4 Department of Pharmaceutical Chemistry, College of Pharmacy, Chincholi, MS, IN
5 Department of Pharmaceutical Sciences and Research, Bhagwant University, Ajmer, Rajasthan, IN

Abstract

Selective estrogen receptor modulators are the class of a chemical compounds acting on a estrogen receptors. These are selectively inhibit or stimulate the estrogen like actions in various tissues. SERMs play a key role in breast cancer chemoprevention. These agents antagonize estrogens in some tissues and mimic their action in others. The mechanism for tissue selectivity appears to be related to differences in their molecular and three-dimensional structures, which affect the transcriptional activity of the activated estrogen receptor. For example, tamoxifen and toremifene act as estrogen antagonists in breast tissue and as estrogen agonists in the endometrium. The present review article is directed towards highlighting the importance of SERMs in treatment of breast cancer.

Keywords

Selective Estrogen Receptor Modulators (SERM’s), Breast Cancer, Hormone Replacement Therapy (HRT).

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