In:
Archiv der Pharmazie, Wiley, Vol. 348, No. 6 ( 2015-06), p. 399-407
Abstract:
The optimization of a series of fused β‐homophenylalanine inhibitors of dipeptidyl peptidase‐4 (DPP‐4) is described. Modification on the P2‐binding moiety of 6 (IC 50 = 10 nM) led to the discovery of β‐homophenylalanine derivatives containing pyrrolidin‐2‐ylmethyl amides. The introduction of a sulfamine in the meta position of the phenyl ring improved the potency against DPP‐4 (6–12‐fold increase). Compound 14k showed DPP‐4 inhibitory activity with an IC 50 value of 0.87 nM. Meanwhile, in vivo experiments exhibited that 14h had an efficiency comparable to sitagliptin at the dose of 10 mg/kg.
Type of Medium:
Online Resource
ISSN:
0365-6233
,
1521-4184
DOI:
10.1002/ardp.201500082
Language:
English
Publisher:
Wiley
Publication Date:
2015
detail.hit.zdb_id:
1496815-0
SSG:
15,3
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