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Abstract
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 A2A/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.
Acknowledgements
The authors wish to acknowledge NIPER – Ahmedabad for providing all the facilities to carry out this work and Dr. Sonja Kachler and Dr. Karl-Norbert Klotz from Institut für Pharmakologie und Toxikologie, Julius-Maximilians-Universität, Germany for their assistance in in vitro studies. The authors are also grateful to Torrent Pharmaceuticals (Ahmedabad, India) for providing ketotifen fumarate as a gift sample.
Declaration of interest
The authors declare that there are no conflicts of interest.
Supplementary material available online
Notes
* NIPER-Ahmedabad Submission No – NIPERA250213.