- Design, Synthesis, and Structure-Activity Relationship of Economical Triazole Sulfonamide Aryl Derivatives with High Fungicidal Activity
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Plant fungal diseases have caused great decreases in crop quality and yield. As one of the considerable agricultural diseases, cucumber downy mildew (CDM) caused by pseudoperonospora cubensis seriously influences the production of cucumber. Amisulbrom is a commercial agricultural fungicide developed by Nissan Chemical, Ltd., for the control of oomycetes diseases that is highly effective against CDM. However, the synthesis of amisulbrom has a high cost because of the introduction of the bromoindole ring. In addition, the continuous use of amisulbrom might increase the risk of resistance development. Hence, there is an imperative to develop active fungicides with new scaffolds but low cost against CDM. In this study, a series of 1,2,4-triazole-1,3-disulfonamide derivatives were designed, synthesized, and screened. Compound 1j showed a comparable fungicidal activity with amisulbrom, but it was low cost and ecofriendly. It has the potential to be developed as a new fungicide candidate against CDM. Further investigations of structure-activity relationship exhibited the structural requirements of 1,2,4-triazole-1,3-disulfonamide and appropriate modification in N-alkyl benzylamine groups with high fungicidal activity. This research will provide powerful guidance for the design of highly active lead compounds with a novel skeleton and low cost.
- Hao, Ge-Fei,Li, Yi-Tao,Lin, Jian,Xu, Jun-Xing,Yao, Wen-Qiang,Zhou, Si
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p. 6792 - 6801
(2020/07/08)
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- NOVEL COMPOUNDS AS INHIBITORS OF RENIN
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The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to
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Page/Page column 10
(2012/05/20)
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- NOVEL COMPOUNDS AS INHIBITORS OF RENIN
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The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to
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Page/Page column 21
(2010/11/05)
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- NOVEL HEXAHYDRO- OR OCTAHYDRO-CYCLOPENTA[C]PYRROLE DERIVATIVES
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The invention relates to novel hexahydro- or octahydro-cyclopenta[c]pyrrole derivatives of the formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including process
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Page/Page column 24-25; 53
(2010/11/27)
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