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.
Keywords: Adenosine; asthma; cytokines; lipoxygenase; thiazolo-thiophene.