16357-33-8Relevant academic research and scientific papers
Design, Synthesis, and Structure-Activity Relationship of Economical Triazole Sulfonamide Aryl Derivatives with High Fungicidal Activity
Hao, Ge-Fei,Li, Yi-Tao,Lin, Jian,Xu, Jun-Xing,Yao, Wen-Qiang,Zhou, Si
, p. 6792 - 6801 (2020/07/08)
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.
NOVEL COMPOUNDS AS INHIBITORS OF RENIN
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Page/Page column 10, (2012/05/20)
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
NOVEL COMPOUNDS AS INHIBITORS OF RENIN
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Page/Page column 20, (2010/11/05)
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
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors
Bezen?on, Olivier,Bur, Daniel,Weller, Thomas,Richard-Bildstein, Sylvia,Remeň, Lubo?,Sifferlen, Thierry,Corminboeuf, Olivier,Grisostomi, Corinna,Boss, Christoph,Prade, Lars,Delahaye, Stéphane,Treiber, Alexander,Strickner, Panja,Binkert, Christoph,Hess, Patrick,Steiner, Beat,Fischli, Walter
supporting information; experimental part, p. 3689 - 3702 (2010/04/02)
Starting from known piperidine renin inhibitors, a new series of 3,9-diazabicyclo[3.3.1]nonene derivatives was rationally designed and prepared. Optimization of the positions 3, 6, and 7 of the diazabicyclonene template led to potent renin inhibitors. The substituents attached at the positions 6 and 7 were essential for the binding affinity of these compounds for renin. The introduction of a substituent attached at the position 3 did not modify the binding affinity but allowed the modulation of the ADME properties. Our efforts led to the discovery of compound (+)-26g that inhibits renin with an IC 50 of 0.20 nM in buffer and 19 nM in plasma. The pharmacokinetics properties of this and other similar compounds are discussed. Compound (+)-26g is well absorbed in rats and efficacious at 10 mg/kg in vivo.
ORGANIC COMPOUNDS
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Page/Page column 29; 30, (2010/02/11)
Novel piperazine derivatives of the general formulae (I) and (II), with the substituent definitions as illustrated in detail in the description are described. The compounds are suitable especially as renin inhibitors and have high potency.
TACHYKININ RECEPTOR ANTAGONISTS
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Page 30, (2010/02/10)
The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
NOVEL 3,4-DISUBSTITUTED 1,2,3,6-TETRAHYDROPYRIDINE DERIVATIVES
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Page 24, (2010/02/09)
The invention relates to novel 3,4-disubstituted 1,2,3,6-tetrahydropyridine derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including proc
