- Discovery of potent transient receptor potential vanilloid 1 antagonists: Design and synthesis of phenoxyacetamide derivatives
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We aimed to discover a novel type of transient receptor potential vanilloid 1 (TRPV1) antagonist because such antagonists are possible drug candidates for treating various disorders. We modified the structure of hit compound 7 (human TRPV1 IC50 = 411 nM) and converted its pyrrolidino group to a (hydroxyethyl)methylamino group, which substantially improved inhibitory activity (15d; human TRPV1 IC50 = 33 nM). In addition, 15d ameliorated bladder overactivity in rats in vivo.
- Takahashi, Eiki,Hirano, Noriyuki,Nagahara, Takashi,Yoshikawa, Satoru,Momen, Shinobu,Yokokawa, Hiroshi,Hayashi, Ryoji
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p. 3154 - 3156
(2013/06/26)
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- COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES
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There are provided according to the invention, novel compounds of formula (I)wherein R, R, R, R, Rand Rare as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
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- Solvent-free synthesis of substituted phenoxyacetic acids under microwave irradiation
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A comparison of microwave-activated vs. classical organic synthesis is presented for a variety of growth-regulator compounds with a phenoxyacetic acid structure. Microwave-assisted nucleophilic substitutions are safely and conveniently carried out in an open vessel, without any solvent. Yields are very good, and reaction times are extremely short.
- Nagy, Gabriela,Filip, Sorin V.,Surducan, Emanoil,Surducan, Vasile
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p. 3729 - 3736
(2007/10/03)
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