80563-89-9Relevant academic research and scientific papers
Synthesis and insecticidal activity in vitro and vivo of novel benzenesulfonyl derivatives based on potent target subunit H of V-ATPase
Yang, Chaofu,Li, Xiaoting,Wei, Jielu,Zhu, Feng,Gang, Fangli,Wei, Shaopeng,Zhao, Yunlong,Zhang, Jiwen,Wu, Wenjun
, p. 3164 - 3167 (2018/09/11)
Two lead compounds with benzenesulfonamide were found through virtual screening based on the 3D structure of the subunit H of V-ATPase in previous study. 74 benzenesulfonyl derivatives were synthesized and their insecticidal activities were evaluated. The derivatives with propargyl substituents exhibit excellent insecticidal activities against Mythimna separata Walker. The LD50 values of compounds A5.7 (28.0 μg·g?1) and B5.7 (36.4 μg·g?1) were significantly less than that of Celangulin V (344.0 μg·g?1). Furthermore, Isothermal Titration Calorimetry (ITC) data indicate there is a strong binding affinity between A5.7 and V-ATPase Subunit H. These results demonstrate that it is a practical way to develop pesticides targeting at H subunit of V-ATPase.
Insecticidal Methods Using 3-Amino-1,2-Benzisothiazole Derivatives
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Page/Page column 32, (2009/04/24)
The invention relates to insecticidal methods using 3-amino-1,2-benzoisothiazole compounds of the formula (I) wherein the variables n and R1 to R6 are as defined in the description. The invention relates to methods of combating or co
Biphenylsulfonamide endothelin antagonists: Structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N-(3,4- dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1,1'-biphenyl]-2-sulfonamide (BMS- 187308)
Murugesan, Natesan,Gu, Zhengxiang,Stein, Philip D.,Bisaha, Sharon,Spergel, Steve,Girotra, Ravi,Lee, Ving G.,Lloyd, John,Misra, Raj N.,Schmidt, Joan,Mathur, Arvind,Stratton, Leslie,Kelly, Yolanda F.,Bird, Eileen,Waldron, Tom,Liu, Eddie C.-K.,Zhang, Rongan,Lee, Helen,Serafino, Randy,Abboa-Offei, Benoni,Mathers, Parker,Giancarli, Mary,Seymour, Andrea Ann,Webb, Maria L.,Moreland, Suzanne,Barrish, Joel C.,Hunt, John T.
, p. 5198 - 5218 (2007/10/03)
Substitution at the ortho position of N-(3,4-dimethyl-5-isoxazolyl) benzenesulfonamide led to the identification of the biphenylsulfonamides as a novel series of endothelin-A (ETA) selective antagonists. Appropriate substitutions on the pendant phenyl ring led to improved binding as well as functional activity. A hydrophobic group such as isobutyl or isopropoxyl was found to be optimal at the 4'-position. Introduction of an amino group at the 2'-position also led to improved analogues. Combination of the optimal 4'- isobutyl substituent with the 2'-amino function afforded an analogue (20, BMS-187308) with improved ET(A) binding affinity and functional activity. Compound 20 also has good oral activity in inhibiting the pressor effect caused by an ET-1 infusion in rats. Doses of 10 and 30 μmol/kg iv 20 attenuated the pressor responses due to the administration of exogenous ET-1 to conscious monkeys, indicating that the compound inhibits the in vivo activity of endothelin-1 in nonhuman primates.
4-Hydroxy-1,2-Benzisothiazol-3(2H)-one-1,1-dioxides and salts thereof
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, (2008/06/13)
Compounds of the formula STR1 wherein R1 is hydrogen or hydroxyl, and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as sweetening agents.
