- Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence.
Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence.
Bioorganic & medicinal chemistry letters (2011-05-03)
Klaus Urbahns, Takeshi Yura, Muneto Mogi, Masaomi Tajimi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki, Timothy B Lowinger, Heinrich Meier, Fiona Chan, David Madge, Jang B Gupta
PMID21531136
RESUMEN
We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration.