183609-18-9Relevant academic research and scientific papers
Triazole compound and application thereof in agriculture (by machine translation)
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Paragraph 0240-0242; 0244-0246, (2020/02/10)
More specifically, the present invention relates to a; method for, preparing a triazole compound (I) represented by formula (I) or a salt (I) thereof, a salt thereof, and a method, for producing a, triazole compound, a salt thereof, and a method for controlling a, disease by using these compounds, and or compositions in the form of a fungicide and a; fungicide ,R composition thereof. 1 , R2 , Y, n, X, R3 , R4 The, m invention has Het .the meanings as described in the present invention. (by machine translation)
Design, Synthesis, and Biological Activity of Novel Triazole Sulfonamide Derivatives Containing a Benzylamine Moiety
Li, Yitao,Yao, Wenqiang,Lin, Jian,Li, Falin,Wu, Yang,Xu, Junxing
, p. 2170 - 2178 (2019/07/09)
The triazole sulfonamide played a very important role in the field of research of new agrochemical compounds as a novel heterocyclic compound with lack of reported resistance. For the research on the innovative triazole sulfonamide fungicide effective against cucumber downy mildew (CDM), the present article designed an array of 1,2,4-triazole-1,3-disulfonamide derivatives. The derivatives were synthesized via coupling multiple benzylamine with triazole sulfonamide groups. 1H-NMR, 13C-NMR, and LC–MS spectrometry were used to characterize these synthesized compounds. Most of these derivatives exhibited better fungicidal activities than that of the commercial cyanosole using bioassays. In particular, compounds 6g and 6h showed the best fungicidal activity against CDM (EC50?=?6.91 and 10.62?mg/L). Comparative experiments demonstrated that the fungicidal activity of 6g and 6h was better than the commercial pesticides amisulbrom and cyanosole. According to the study, the compound 6g had a giant application potential on fungicide against CDM.
Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries
Londregan, Allyn T.,Piotrowski, David W.,Futatsugi, Kentaro,Warmus, Joseph S.,Boehm, Markus,Carpino, Philip A.,Chin, Janice E.,Janssen, Ann M.,Roush, Nicole S.,Buxton, Joanne,Hinchey, Terri
, p. 1407 - 1411 (2013/03/14)
Optimization of a high-throughput screening hit led to the discovery of a new series of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as highly potent agonists of TGR5. This novel chemotype was rapidly developed through iterative combinatorial library synthesis. It was determined that in vitro agonist potency correlated with functional activity data from human peripheral blood monocytes.
RENIN INHIBITORS
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Page/Page column 55, (2008/06/13)
The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.
Synthesis of C-aryl-N-cyclopropylnitrones
Vukics, Krisztina,Tarkanyi, Gabor,Dravecz, Ferenc,Fischer, Janos
, p. 3419 - 3425 (2007/10/03)
Synthesis of C-aryl-N-cyclopropylnitrones is described. Preparations were performed either by condensation of the appropriate aldehyde with N-cyclopropyl-hydroxylamine, or oxidation of N-substituted N-cyclopropylamines with sodium tungstate/hydrogen perox
Pyrrolidine-modified and 6-substituted analogs of nicotine: a structure-affinity investigation
Dukat, M.,Fiedler, W.,Dumas, D.,Damaj, I.,Martin, B. R.,et al.
, p. 875 - 888 (2007/10/03)
Because the structural requirements for the binding of nicotine to central nicotine receptors remain largely uninvestigated, we undertook a systematic investigation of pyrrolidine ring-opened analogs.This led to a subsequent investigation of related conformationally restricted derivatives of these analogs.The results are reported relative to the binding of several well-known and widely used nicotine receptor ligands.Although none of the ring-opened analogs binds with higher affinity than (-)-nicotine (Ki = 2.3 nM), 3-(N-methyl-N-ethylaminomethyl)pyridine (12a; Ki = 28 nM) binds with significant affinity.A conformationally restricted analog of 12a, N-methyl naphthyridine 30b (Ki = 18 nM), binds with similar affinity. 6-Substitution of 12a and racemic nicotine seems to be tolerated when the substituent is halogen or methyl.In functional studies (hypolocomotion and antinociception in mice; stimulus generalization in nicotine-trained rats) 30b retains nicotine-like properties.Several of the 6-substituted compounds were 2 to 20 times more potent than (+/-)nicotine.Although the intact pyrrolidine ring of nicotine appears important for optimal affinity, its presence is not an absolute requirement for activity, and 6-position substitution of the pyridine nucleus can influence both binding and functional activity. - Keywords: nicotine; nicotine receptor; drug discrimination; antinociception.
Substituted pyridines useful as modulators of acetylcholine receptors
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, (2008/06/13)
In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds
