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Potent 11β-hydroxylase inhibitors with inverse metabolic stability in human plasma and hepatic S9 fractions to promote wound healing.

Authors :
Zhu W
Hu Q
Hanke N
van Koppen CJ
Hartmann RW
Source :
Journal of medicinal chemistry [J Med Chem] 2014 Sep 25; Vol. 57 (18), pp. 7811-7. Date of Electronic Publication: 2014 Sep 08.
Publication Year :
2014

Abstract

Topical application of CYP11B1 inhibitors to reduce cutaneous cortisol is a novel strategy to promote healing of chronic wounds. Pyridyl substituted arylsulfonyltetrahydroquinolines were designed and synthesized resulting in a strong inhibitor 34 (IC50 = 5 nM). It showed no inhibition of CYP17 and CYP19 and no mutagenic effects. It exhibited inverse metabolic stability in plasma (t1/2 ≫ 150 min), which is similar to wound fluid in composition, and in liver S9 fractions (t1/2 = 16 min).

Details

Language :
English
ISSN :
1520-4804
Volume :
57
Issue :
18
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
25176013
Full Text :
https://doi.org/10.1021/jm501004t