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Updated: Sep 23, 2026

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
Novel selective hindlimb vasodilators: synthesis and biological activity of 1-acyl-4-aminopiperidine derivatives
Shuji Teramoto1, Michinori Tanaka, Hiroshi Shimizu
1Medicinal Chemistry Research Institute, Otsuka Pharmaceutical Co, Ltd, 463-10 Kagasuno Kawauchi-cho, Tokushima 771-0192, Japan. stera@research.otsuka.co.jp
Abstract:
A series of 6-(4-amino-1-piperidinyl)carbonyl-2(1H)-quinolinones, and their open form derivatives, were synthesized and evaluated for their ability to stimulate femoral artery blood flow (FBF) in the canine hindlimb. All members of this series stimulated FBF, and subsequent experiments revealed that selected members of this series produced minimal changes in coronary blood flow or systemic blood pressure. Compound 25 was the most promising agent in this respect, and clinical trials are now ongoing to evaluate the effectiveness of this drug as a novel treatment for intermittent claudication and Raynaud's phenomenon.
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