COMPARATIVE SAR OF SYNTHETIC COUMARIN DERIVATIVES FOR THEIR ANTI-INFLAMMATORY ACTIVITYAbstract
Coumarin (2H-1-benzopyran-2-one) nucleus and it’s natural, as well as synthetic derivatives, has been a field of interest due to its unique tendency to adopt varying categories of substitutions which provides the basis for modifying this nucleus for multidisciplinary actions. The extensive literature review reflects that coumarin derivatives have been synthesized by several structural modifications and exhibit numerous activities like anti-inflammatory, anti-tumor, anti-HIV, anticoagulant, antimicrobial, antioxidant, anti-hepatitis, hepatoprotective, anti-pyretic, analgesics, anti-thrombotic, vasodilatory, anti-mutagenic, antioxidant, anti-fungal, anti-viral, anti-hypertensive, anti-tubercular, anti-convulsant, anti-adipogenic and anti-hyperglycemic. They also inhibit lipooxygenase, cyclooxygenase, MAO-A, MAO-B, and TNF-alpha enzymes. The purpose of this study is to review the anti-inflammatory potentials of coumarins and to generate a comparative SAR that may support to improve their anti-inflammatory activity by newer and potent diverse structural modifications of the coumarin nucleus. The review shows that wide varieties of coumarin derivatives have been synthesized and have shown anti-inflammatory potentials. These derivatives can be further modified with the help of SAR generated in the present work to improve the anti-inflammatory potentials of the versatile coumarin nucleus.
G. Kayal *, K. Jain, S. Malviya and A. Kharia
Modern Institute of Pharmaceutical Sciences, Alwasa, Behind Rewti Range, Indore, Madhya Pradesh, India.
10 March 2014
08 May 2014
26 May 2014
01 September 2014