| Novel selective hindlimb vasodilators: synthesis and biological activity of 1-acyl-4-aminopiperidine derivatives. | |
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MedLine Citation:
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PMID: 12825942 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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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Authors:
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Shuji Teramoto; Michinori Tanaka; Hiroshi Shimizu; Takafumi Fujioka; Fujio Tabusa; Takashi Imaizumi; Kenji Yoshida; Hiroyuki Fujiki; Toyoki Mori; Takumi Sumida; Michiaki Tominaga |
Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 46 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 2003 Jul |
Date Detail:
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Created Date: 2003-06-26 Completed Date: 2003-08-07 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 3033-44 Citation Subset: IM |
Affiliation:
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Medicinal Chemistry Research Institute, Otsuka Pharmaceutical Co, Ltd, 463-10 Kagasuno Kawauchi-cho, Tokushima 771-0192, Japan. stera@research.otsuka.co.jp |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Arteries Blood Pressure / drug effects Coronary Circulation / drug effects Dogs Femur / blood supply Hindlimb / blood supply* Piperidines / chemical synthesis*, chemistry, pharmacology Quinolones / chemical synthesis, chemistry, pharmacology Regional Blood Flow / drug effects Structure-Activity Relationship Vasodilator Agents / chemical synthesis*, chemistry, pharmacology |
| Chemical | |
Reg. No./Substance:
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0/1-(3,5-dimethyl-4-propionylamino)benzoyl-4-(N-methyl-2-phenylethyl)aminopiperidine; 0/Piperidines; 0/Quinolones; 0/Vasodilator Agents |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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