Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators

Scott D Kuduk; Robert M DiPardo; Douglas C Beshore; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau

doi:10.1016/j.bmcl.2010.02.095

Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2538-41. doi: 10.1016/j.bmcl.2010.02.095. Epub 2010 Mar 10.

Authors

Scott D Kuduk¹, Robert M DiPardo, Douglas C Beshore, William J Ray, Lei Ma, Marion Wittmann, Matthew A Seager, Kenneth A Koeplinger, Charles D Thompson, George D Hartman, Mark T Bilodeau

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, West Point, PA 19486, USA. [email protected]

PMID: 20346667
DOI: 10.1016/j.bmcl.2010.02.095

Abstract

Incorporation of hydroxycycloalkyl fused pyridone carboxylic acids in lieu of quinolone carboxylic acids enhance free fraction without increased susceptibility to P-glycoprotein transport.

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
Allosteric Regulation
Animals
Carboxylic Acids / chemistry
Carboxylic Acids / pharmacology*
Mice
Protein Transport
Pyridones / chemistry*
Rats

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
Carboxylic Acids
Pyridones