- ALKYNE COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS
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Provided are compounds of formula (Ia) and pharmaceutically acceptable salts thereof, wherein A, B, R 1, R 2, m and n are as defined herein, which are active as inhibitors of S-Nitrosoglutathione reductase (GSNOR). These compounds prevent, inhibit, or suppress the action of GSNOR and are therefore useful in the treatment of GSNOR mediated diseases, disorders, syndromes or conditions such as, e.g., pulmonary hypertension, acute respiratory distress syndrome (ARDS), asthma, bronchospasm, cough, pneumonia, pulmonary fibrosis, interstitial lung diseases, cystic fibrosis and chronic obstructive pulmonary disease (COPD).
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Page/Page column 71; 103
(2016/05/02)
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- Triton B-mediated efficient and convenient alkoxylation of activated aryl and heteroaryl halides
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A simple and convenient one-pot synthesis of aryl alkyl ethers by the alkoxylation of aryl halides with alcohol in the presence of Triton B as a base is described. The procedure is applicable for a variety of aryl and heteroaryl halides, and yields are very good. The use of a nonmetallic base and solvent-free conditions are important features of the reaction. Copyright Taylor & Francis Group, LLC.
- Meshram,Goud, P. Ramesh,Reddy, B. Chennakesava,Kumar, D. Aravind
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experimental part
p. 2122 - 2129
(2010/08/13)
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- Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure-activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamides
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A new series of 3-(3-pyridyl)acrylamides 16, 17, 19, and 26, and 5-(3-pyridyl)-2,4-pentadienamides 20-25 were prepared and evaluated for their antiallergic activity. Several of these compounds exhibited more potent inhibitory activities than the parent compounds 1a [(E)-N-[4 [4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamide] against the rat passive cutaneous anaphylaxis (PCA) reaction and the enzyme 5-lipoxygenase. Particularly, 4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3-pyridyl)acrylamide (17p) showed an ED50 value of 3.3 mg/kg po in the rat PCA test, which was one-fifth of ketotifen and oxatomide. As compared with ketotifen and oxatomide, compound 17p (AL-3264) possessed a better balance of antiallergic properties due to inhibition of chemical mediator release, inhibition of 5-lipoxygenase, and antagonism of histamine.
- Nishikawa,Shindo,Ishii,Nakamura,Kon,Uno
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p. 583 - 593
(2007/10/02)
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- Liquid Crystalline Compounds Bearing Pyridine Ring: 3-(4-Alkoxyphenylazoxy)-6-alkoxypyridines
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3-(4-Alkoxyphenylazo)-6-alkoxypyridines (6) with n-alkoxyl (C1-C6) groups were synthesized by the coupling reaction of phenol with 6-alkoxy-3-pyridine diazonium chloride prepared from 2-chloro-5-nitropyridine via 2-alkoxy-5-nitro and 2-alkoxy-5-aminopyridines and subsequent etherification with n-alkyl iodides.Mild oxidation of 6 with hydrogen peroxide in acetic acid provided 3-6-alkoxy-pyridines (7) containing nearly equimolar amounts of ONN (8) and NNO (8') isomers.Centrifugal liquid chromatography satisfactorily separated these two isomers.Mesomorphic behaviors of 8 and 8' are characteristic in that the pyridine ring exerts polar effects and 8 are more balanced in polarity than 8'.Compounds 7 possess rather lower mesomorphic ranges than 8 and 8'.Some of compounds 6 indicate mesomorphic ranges but generally azo compounds are inferior to azoxy ones.
- Kamogawa, Hiroyoshi,Kasai, Tsuneharu
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