From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor
Futatsugi, K; Mascitti, V; Guimarães, CR; Morishita, N; Cai, C; Deninno, MP; Gao, H; Hamilton, MD; Hank, R; Harris, AR; Kung, DW; Lavergne, SY; Lefker, BA; Lopaze, MG; Mcclure, KF; Munchhof, MJ; Preville, C; Robinson, RP; Wright, SW; Bonin, PD; Cornelius, P; Chen, Y; Kalgutkar, AS
| HERO ID | 1834879 |
|---|---|
| In Press | No |
| Year | 2013 |
| Title | From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor |
| Authors | Futatsugi, K; Mascitti, V; Guimarães, CR; Morishita, N; Cai, C; Deninno, MP; Gao, H; Hamilton, MD; Hank, R; Harris, AR; Kung, DW; Lavergne, SY; Lefker, BA; Lopaze, MG; Mcclure, KF; Munchhof, MJ; Preville, C; Robinson, RP; Wright, SW; Bonin, PD; Cornelius, P; Chen, Y; Kalgutkar, AS |
| Journal | Bioorganic & Medicinal Chemistry Letters |
| Volume | 23 |
| Issue | 1 |
| Page Numbers | 194-197 |
| Abstract | A novel GPR119 agonist based on the 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole scaffold was designed through lead optimization starting from pyrazole-based GPR119 agonist 1. The design is centered on the conformational restriction of the core scaffold, while minimizing the change in spatial relationships of two key pharmacophoric elements (piperidine-carbamate and aryl sulfone). |
| Doi | 10.1016/j.bmcl.2012.10.119 |
| Pmid | 23177788 |
| Wosid | WOS:000312267700033 |
| Is Certified Translation | No |
| Dupe Override | No |
| Comments | Journal: Bioorganic & medicinal chemistry letters ISSN: 1464-3405Scopus URL: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84871013771&doi=10.1016%2fj.bmcl.2012.10.119&partnerID=40&md5=e2bb17831527b71452c2bb846330d23c |
| Is Public | Yes |
| Language Text | English |
| Keyword | GPR119; Intrinsic activity; Conformational restriction |