- 2-(1,2,4-triazolyl)benzoyl arylamine active compound for inhibiting pathogens causing take-all disease of wheat
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The invention discloses a 2-(1,2,4-triazolyl)benzoyl arylamine active compound for inhibiting pathogens causing the take-all disease of wheat. The active compound is characterized in that the active compound has a structure shown as a formula I which is d
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Paragraph 0019; 0021
(2020/06/09)
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- Preparation of highly potent and selective non-peptide antagonists of the arginine vasopressin V1A receptor by introduction of a 2-ethyl-1H-1-imidazolyl group
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To find a new series of arginine vasopressin (AVP) V1A receptor antagonists, the influence of the 2-phenyl group of 2-phenyl-4′-[(2,3,4,5- tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide (7) was investigated. Replacement of the 2-phenyl group by a 2-ethyl-1H-imidazol-1-yl group was effective in yielding a V1A-selective compound. Moreover, this imidazolyl group was introduced in the same position in YM-35471 (6), and further studies of these compounds were performed. Consequently, we found that the (Z)-4′-({4,4-difluoro-5-[(N-cyclo-propylcarbamoyl) methylene]-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl}carbonyl)-2-(2-ethyl-1H-1- imidazol-1-yl)benzanilide (9f) exhibited highly potent affinity and selectivity, and was the most potent antagonist for the V1A receptor among our compounds. The synthesis and pharmacological evaluation of these compounds are described in this paper
- Shimada, Yoshiaki,Akane, Hiroaki,Taniguchi, Nobuaki,Matsuhisa, Akira,Kawano, Noriyuki,Kikuchi, Kazumi,Yatsu, Takeyuki,Tahara, Atsuo,Tomura, Yuichi,Kusayama, Toshiyuki,Wada, Koh-Ichi,Tsukada, Junko,Tsunoda, Takashi,Tanaka, Akihiro
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p. 764 - 769
(2007/10/03)
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- Cyclization Reactions in Azole Chemistry: The Reaction of Some Azoles with o-Fluoroacetophenone, o-Fluorobenzaldehyde and o-Fluorobenzophenone
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The reactions of some azoles with o-fluoro-acetophenone, -benzaldehyde and -benzophenone in dimethyl sulfoxide solution in the presence of anhydrous potassium carbonate have been investigated.In addition to the expected substitution products, cyclization
- Rosevear, Judi,Wilshire, John F. K.
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p. 1097 - 1114
(2007/10/02)
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