| Title : Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification - Boyle_2002_Bioorg.Med.Chem.Lett_12_3479 |
| Author(s) : Boyle CD , Vice SF , Campion J , Chackalamannil S , Lankin CM , McCombie SW , Billard W , Binch H, 3rd , Crosby G , Williams MC , Coffin VL , Cox KA , Grotz DE , Duffy RA , Ruperto V , Lachowicz JE |
| Ref : Bioorganic & Medicinal Chemistry Lett , 12 :3479 , 2002 |
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Abstract :
We previously reported the initial discovery of a novel class of stabilized benzylidene ketal M(2) receptor antagonists. This paper discusses new analogues consisting of benzamide modifications which not only improved M(2) receptor affinity and selectivity, but also enhanced the pharmacokinetic properties of the series. These changes led to the discovery of a highly potent and selective M(2) antagonist, which demonstrated in vivo efficacy and had good bioavailability in multiple species. |
| PubMedSearch : Boyle_2002_Bioorg.Med.Chem.Lett_12_3479 |
| PubMedID: 12419388 |
Boyle CD, Vice SF, Campion J, Chackalamannil S, Lankin CM, McCombie SW, Billard W, Binch H, 3rd, Crosby G, Williams MC, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE (2002)
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification
Bioorganic & Medicinal Chemistry Lett
12 :3479
Boyle CD, Vice SF, Campion J, Chackalamannil S, Lankin CM, McCombie SW, Billard W, Binch H, 3rd, Crosby G, Williams MC, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE (2002)
Bioorganic & Medicinal Chemistry Lett
12 :3479