2. Academic Validation
  3. Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists

Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists

  • ACS Med Chem Lett. 2022 May 25;13(6):943-948. doi: 10.1021/acsmedchemlett.2c00079.
Nicholas R Wurtz 1,  James A Johnson 1,  Andrew Viet 1,  Pravin S Shirude 2,  Vishweshwaraiah Baligar 2,  Sudhakara Madduri 2,  Daniel L Cheney 1,  Hyunsoo Park 1,  John A Lupisella 1,  Mei-Yin Hsu 1,  Mojgan Abousleiman 1,  Michael A Galella 3,  Darpandeep Aulakh 3,  Elizabeth A Dierks 1,  Ricardo A Garcia 1,  Jacek Ostrowski 1,  Ellen K Kick 1,  Ruth R Wexler 1
Affiliations

Affiliations

  • 1 Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543, United States.
  • 2 Biocon Bristol Myers Squibb R&D Center, Bangalore-560099, India.
  • 3 Bristol Myers Squibb Research and Development, New Brunswick, New Jersey 08901, United States.
PMID: 35707160 DOI: 10.1021/acsmedchemlett.2c00079
Abstract

Formyl peptide receptor 2 (FPR2) agonists have shown efficacy in inflammatory-driven animal disease models and have the potential to treat a range of diseases. Many reported synthetic agonists contain a phenylurea, which appears to be necessary for activity in the reported chemotypes. We set out to find isosteres for the phenylurea and focused our efforts on heteroaryl rings. The wide range of potencies with heterocyclic isosteres demonstrates how electronic effects of the heteroatom placement impact molecular recognition. Herein, we report our discovery of benzimidazole and aminophenyloxadiazole FPR2 agonists with low nanomolar activity.

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