| Title : Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors - Shen_2011_Bioorg.Med.Chem.Lett_21_1299 |
| Author(s) : Shen HC , Ding FX , Zhou C , Xiong Y , Verras A , Chabin RM , Xu S , Tong X , Xie D , Lassman ME , Bhatt UR , Garcia-Calvo MM , Geissler W , Shen Z , Chen D , SinhaRoy R , Hale JJ , Tata JR , Pinto S , Shen DM , Colletti SL |
| Ref : Bioorganic & Medicinal Chemistry Lett , 21 :1299 , 2011 |
|
Abstract :
A series of benzimidazole pyrrolidinyl amides containing a piperidinyl group were discovered as novel prolylcarboxypeptidase (PrCP) inhibitors. Low-nanomolar IC(50)'s were achieved for several analogs, of which compound 9b displayed modest ex vivo target engagement in eDIO mouse plasma. Compound 9b was also studied in vivo for its effect on weight loss and food intake in an eDIO mouse model and the results will be discussed. |
| PubMedSearch : Shen_2011_Bioorg.Med.Chem.Lett_21_1299 |
| PubMedID: 21315588 |
| Gene_locus related to this paper: human-PRCP |
| Inhibitor | CHEMBL1684295 |
| Gene_locus | human-PRCP |
Shen HC, Ding FX, Zhou C, Xiong Y, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen D, SinhaRoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL (2011)
Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors
Bioorganic & Medicinal Chemistry Lett
21 :1299
Shen HC, Ding FX, Zhou C, Xiong Y, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen D, SinhaRoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL (2011)
Bioorganic & Medicinal Chemistry Lett
21 :1299