jct
Open Access
ISSN: 2161-0495
ISSN: 2161-0495
Department of on Communicable Diseases, Translational Health Science and Technology Institute, Faridabad, Haryana, India
Research Article
Developing Selective FPR2 Agonists can be a Potential Approach to Treat Moderate to Severe Asthma?
Author(s): Senthil A Visaga, Harikesh Kalonia, Vinay Verma, Sandeep Sinha, Shashi Kant Singh, Swati Upadhyay, Sudhir Sahdev, Amita Pansari, Rajesh Kumar, Mahadev Bandgar, Narayan Karanjule, Raj Kumar Shirumalla, Kaoru Morishita and Ruchi Tandon*
Formyl Peptide Receptors (FPRs) play an important role in the modulation of inflammation. There has however been a lot of ambiguity in the past with regard to the pro and anti-inflammatory profiles of FPR family members. A few FPR2/FPR1 dual agonists are reported in the public domain for their anti-inflammatory properties along with associated toxicities. Targeting FPR1 alone on the other hand has been shown to result into both positive and negative outcomes. We, therefore, aimed to develop FPR2 agonists which were selective against FPR1 followed by evaluating their potential in mitigating the non-resolving inflammation in asthma. Extensive Structure-Activity-Relationship (SAR) studies were conducted on the imidazole and benzimidazole chemotypes and a few molecules were shortlisted based on their in vitro profile and Absorption, Distribution, Metabolism and Excretion (ADME) p.. View More»
DOI:
10.35248/2161-0495.22.12.510