Search Results - "Saku, Osamu"
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K-685, a TRPV1 Antagonist, Blocks PKC-Sensitized TRPV1 Activation and Improves the Inflammatory Pain in a Rat Complete Freund’s Adjuvant Model
Published in Journal of Pharmacological Sciences (2013)“…Transient receptor potential vanilloid 1 (TRPV1) is a Ca2+-permeable non-selective cation channel that transmits pain signals. TRPV1 is activated by multiple…”
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Synthesis of 1-Azaazulenes from Cycloheptatrienylmethyl Ketone O-Pentafluorobenzoyloximes by Palladium-Catalyzed Cyclization and Oxidation
Published in Bulletin of the Chemical Society of Japan (2004)“…Various 1-azaazulenes are synthesized from cycloheptatrienylmethyl ketone O-pentafluorobenzoyloximes by treatment with a catalytic amount of Pd(dba)2–t-Bu3P…”
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3
Palladium-Catalyzed Synthesis of 1-Azaazulenes from Cycloheptatrienylmethyl Ketone O-Pentafluorobenzoyl Oximes
Published in Chemistry letters (01-06-2002)“…Substituted 1-azaazulenes are synthesized from cycloheptatrienylmethyl ketone O-pentafluorobenzoyloximes by the intramolecular Heck-type amination catalyzed by…”
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Synthetic studies on selective adenosine A2A receptor antagonists: Synthesis and structure-activity relationships of novel benzofuran derivatives
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…A series of benzofuran derivatives were prepared to study their antagonistic activities to the A(2A) receptor. Replacement of the ester group of the lead…”
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Discovery of Novel 5,5-Diarylpentadienamides as Orally Available Transient Receptor Potential Vanilloid 1 (TRPV1) Antagonists
Published in Journal of medicinal chemistry (12-04-2012)“…We have developed a novel and potent chemical series of 5,5-diphenylpentadienamides for targeting TRPV1 in vitro and in vivo. In this investigation, we…”
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Synthetic studies on selective adenosine A2A receptor antagonists. Part II: Synthesis and structure–activity relationships of novel benzofuran derivatives
Published in Bioorganic & medicinal chemistry letters (15-06-2010)“…The discovery of a novel series of A2A antagonists is described. A selected compound was shown to be able to induce anti-parkinsonian effects in MPTP-treated…”
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Synthetic study of VLA-4/VCAM-1 inhibitors: Synthesis and structure–activity relationship of piperazinylphenylalanine derivatives
Published in Bioorganic & medicinal chemistry (01-02-2008)“…To improve poor pharmacokinetic characters of the preceding VLA-4 inhibitors, novel piperazinylphenylalanine derivatives were designed and optimized for oral…”
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Synthetic studies on selective adenosine A sub(2A) receptor antagonists: Synthesis and structure-activity relationships of novel benzofuran derivatives
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…A series of benzofuran derivatives were prepared to study their antagonistic activities to the A sub(2A) receptor. Replacement of the ester group of the lead…”
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Synthetic studies on selective adenosine A 2A receptor antagonists: Synthesis and structure–activity relationships of novel benzofuran derivatives
Published in Bioorganic & medicinal chemistry letters (2010)“…Novel benzofuran derivatives as potent and selective adenosine A 2A inhibitors were synthesized and evaluated. A series of benzofuran derivatives were prepared…”
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Synthesis of indole and indolenine derivatives starting from indoline-2-thiones
Published in Journal of heterocyclic chemistry (01-01-2001)“…Indoline‐2‐thiones 1a‐b,d,f,h, which have at least one hydrogen at the 3‐position reacted with α‐halo ester 2a‐d, α‐halo ketones 2e‐f, and a‐bromoacetonitrile…”
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