Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA2 Receptor | Zendy

Renukadevi Patil | Zendy; James I. Fells | Zendy; Erzsébet Szabó | Zendy; Keng G. Lim | Zendy; Derek D. Norman | Zendy; Andrea Balogh | Zendy; Shivaputra A. Patil | Zendy; Jur Strobos | Zendy; Duane D. Miller | Zendy; Gábor Tigyi | Zendy

Open Access

Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA₂ Receptor

Author(s) -

Renukadevi Patil,

James I. Fells,

Erzsébet Szabó,

Keng G. Lim,

Derek D. Norman,

Andrea Balogh,

Shivaputra A. Patil,

Jur Strobos,

Duane D. Miller,

Gábor Tigyi

Publication year - 2014

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm5007116

Subject(s) - chemistry , lysophosphatidic acid , g protein coupled receptor , agonist , benzoic acid , docking (animal) , stereochemistry , receptor , ligand (biochemistry) , mediator , biochemistry , pharmacology , microbiology and biotechnology , biology , medicine , nursing

Lysophosphatidic acid (LPA) is a growth factor-like mediator and a ligand for multiple GPCR. The LPA2 GPCR mediates antiapoptotic and mucosal barrier-protective effects in the gut. We synthesized sulfamoyl benzoic acid (SBA) analogues that are the first specific agonists of LPA2, some with subnanomolar activity. We developed an experimental SAR that is supported and rationalized by computational docking analysis of the SBA compounds into the LPA2 ligand-binding pocket.

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