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

摘要

Context: Asthma is multifaceted disease where many targets contribute towards its development and progression. Among these, adenosine receptor subtypes play a major role.Objective: MCD-KV-10, a novel thiazolo-thiophene was designed and evaluated pre-clinically for its implication in management of asthma.Materials and methods: 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.Results: 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.Discussion: These results indicate that MCD-KV-10 has an inhibitory effect on airway inflammation.Conclusion: Though, we have identified a potential candidate for management of asthma, further mechanistic studies are needed.