Hirst DJ

References (1)

Title : Investigation of a Bicyclo[1.1.1]pentane as a Phenyl Replacement within an LpPLA2 Inhibitor - Measom_2017_ACS.Med.Chem.Lett_8_43
Author(s) : Measom ND , Down KD , Hirst DJ , Jamieson C , Manas ES , Patel VK , Somers DO
Ref : ACS Med Chem Lett , 8 :43 , 2017
Abstract : We describe the incorporation of a bicyclo[1.1.1]pentane moiety within two known LpPLA2 inhibitors to act as bioisosteric phenyl replacements. An efficient synthesis to the target compounds was enabled with a dichlorocarbene insertion into a bicyclo[1.1.0]butane system being the key transformation. Potency, physicochemical, and X-ray crystallographic data were obtained to compare the known inhibitors to their bioisosteric counterparts, which showed the isostere was well tolerated and positively impacted on the physicochemical profile.
ESTHER : Measom_2017_ACS.Med.Chem.Lett_8_43
PubMedSearch : Measom_2017_ACS.Med.Chem.Lett_8_43
PubMedID: 28105273
Gene_locus related to this paper: human-PLA2G7