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Determination of Melting Point of Novel Pyrazolyl Tetrazoles As Selective COX-2 Inhibitors by Open Capillary Method (CAT#: STEM-PPA-0106-YJL)

Introduction

Currently marketed non steroidal anti-inflammatory drugs (NSAIDs) have been associated with several side effects like gastrointestinal mucosal damage, bleeding, intolerance, renal toxicity, and hepatotoxicity. The pharmacological effects of NSAIDs occur due to inhibition of the membrane enzyme called cyclooxygenase (COX-1 and COX-2), which is involved in prostaglandin biosynthesis. <br />Pyrazole template is considered as an important chemical entity of various physiological significances and pharmaceutical utility. Pyrazoles have drawn a greater attention due to their wide range of therapeutic activities including anticonvulsant, antidepressant, antitumor, antimicrobial, ACE inhibitor, antiviral, anti-inflammatory, etc. The well known selective COX-2 inhibitor, Celecoxib, and non steroidal antiphlogistic drug. Lonazolac, are good examples of pyrazoles containing anti-inflammatory drugs. According to literature, tetrazole and its derivatives are known to possess antibacterial, anti-inflammatory, antifungal, cyclo-oxygenase inhibitor, hypoglycemic, and anticancer activities.




Principle

Melting point is a characteristic property of solid crystalline substance. It is the temperature at which the solid phase changes to the liquid phase. This phenomenon occurs when the substance is heated.
In all major pharmacopoeias the open capillary method is described to determine the melting point (slip point) for fats, fatty acids, paraffin, and waxes. In a glass capillary tube open at both ends (1), 10 mm of sample is introduced (2), chilled to a given temperature and immersed into a water bath (3/4). The melting point with open capillary, also known as slip point or slip melting point, is the temperature at which the substance begins to rise in the capillary due to the effect of the increasing temperature and buoyancy.

Applications

Chemical industry; Cosmetic/pharmaceutical industry

Procedure

1. Prepare the substance.
2. Affix one of the capillaries to a thermometer.
3. Place the thermometer with an affixed capillary into a glass.
4. Increase the temperature.

Materials

• Sample Type: crystalline compounds