2′ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling

Brian Budzik, Vincenzo Garzya, Dongchuan Shi, Graham Walker, Yann Lauchart, Adam J. Lucas, Ralph A. Rivero, Christopher J. Langmead, Jeannette M Watson, Zining Wu, Ian T Forbes, JIan Jin

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Abstract

Further optimization of the biaryl amide series via extensively exploring structure-activity relationships resulted in potent and subtype selective M 1 agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure-activity relationships, subtype selectivity for M1 over M2-5, and DMPK properties of these novel compounds are described.

Original languageEnglish
Pages (from-to)3545-3549
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number12
DOIs
Publication statusPublished - 2010
Externally publishedYes

Keywords

  • 2′ biaryl amides
  • CNS-penetrant and orally bioavailable M1 agonist
  • Subtype selective M1 agonist
  • Subtype selective M1 muscarinic acetylcholine receptor agonist

Cite this

Budzik, B., Garzya, V., Shi, D., Walker, G., Lauchart, Y., Lucas, A. J., Rivero, R. A., Langmead, C. J., Watson, J. M., Wu, Z., Forbes, I. T., & Jin, JI. (2010). 2′ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling. Bioorganic and Medicinal Chemistry Letters, 20(12), 3545-3549. https://doi.org/10.1016/j.bmcl.2010.04.127