Journal of Enzyme Inhibition and Medicinal Chemistry 2015-04-01

Implication of novel thiazolo-thiophene derivative (MCD-KV-10) for management of asthma.

Dhiraj Patil, Ranjeet Prasad Dash, Sandeep Kumar Thakur, Amit N Pandya, P Venkatesh, Kamala K Vasu, Manish Nivsarkar

文献索引：J. Enzyme Inhib. Med. Chem. 30(2) , 229-39, (2015)

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摘要

Asthma is multifaceted disease where many targets contribute towards its development and progression. Among these, adenosine receptor subtypes play a major role.MCD-KV-10, a novel thiazolo-thiophene was designed and evaluated pre-clinically for its implication in management of asthma.This compound showed good affinity and selectivity towards A(2A)/A3 adenosine receptor (AR) subtypes. Furthermore, MCD-KV-10 was evaluated for in vitro lipoxygenase inhibition activity; in vivo mast cell stabilization potential and in vivo anti-asthmatic activity was done in ovalbumin-induced airway inflammation model in guinea pigs.The compound showed good (>57%) inhibition of lipoxygenase enzyme and also effectively protected mast cell degranulation (>63%). The compound showed good anti-asthmatic activity as inferred from the in vivo studies.These results indicate that MCD-KV-10 has an inhibitory effect on airway inflammation.Though, we have identified a potential candidate for management of asthma, further mechanistic studies are needed.