메뉴 건너뛰기




Volumn 18, Issue 13, 2008, Pages 3706-3710

Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design

Author keywords

Diabetes; DPP 4 inhibitors; Fluorine H bond

Indexed keywords

AMIDE; ASPARTIC ACID; BETA ALANINE; CARBONIC ACID; CARBONYL DERIVATIVE; CESIUM; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; DIPYRONE; FLUORINE; FLUOROPYRROLIDINE AMIDE; GLYCINE; METHYL GROUP; NITRILE; NITROGEN; OXADIAZOLE DERIVATIVE; OXYGEN; PHENYLACETIC ACID; SITAGLIPTIN; VALEROLACTAM;

EID: 44849112519     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.05.061     Document Type: Article
Times cited : (26)

References (30)
  • 8
    • 33845489598 scopus 로고    scopus 로고
    • Raz I., et al. Diabetologia 49 (2006) 2564
    • (2006) Diabetologia , vol.49 , pp. 2564
    • Raz, I.1
  • 17
    • 44849137891 scopus 로고    scopus 로고
    • note
    • 1H NMR and LC-MS prior to submission for biological evaluation.
  • 24
    • 44849107140 scopus 로고    scopus 로고
    • note
    • At the time of this study, the stereochemistry of neither 7 nor 12 could be unambiguously assigned, and 'anti configuration was assumed for both series. Later, X-ray structural analysis showed that 12c is indeed 'anti, but 7c is actually 'syn. However, X-structures also showed that the backbones of both compounds fit in the enzyme active site the same way regardless of the orientation of the chiral methyl groups.
  • 29
    • 44849102769 scopus 로고    scopus 로고
    • note
    • max, peak plasma concentration after indicated oral dosing; F%, oral bioavailability.
  • 30
    • 44849138213 scopus 로고    scopus 로고
    • note
    • The coordinates for the structure of DPP-4 in complex with 24d were deposited with the Protein Data Bank, Accession code 3D4L.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.