186650-78-2Relevant academic research and scientific papers
USE OF DISUBSTITUTED BENZENES TO CONTROL INSECTICIDE-RESISTANT PESTS
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, (2018/11/26)
The invention is in the technical field of insect control and relates to the use of a disubstituted benzenes for controlling insecticide-resistant pests such as mosquitoes and cockroaches.
NICOTINIC ACETYLCHOLINE RECEPTOR SILENT AGONISTS
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Page/Page column 35; 36, (2017/05/02)
Derivatives of N,N-diethyl-N'- phenyl-piperazine, a silent agonist of the mammalian α7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.
Dissection of N,N-diethyl-N′-phenylpiperazines as α7 nicotinic receptor silent agonists This manuscript is dedicated to Professor Koji Nakanishi on the occasion of his 90th birthday
Quadri, Marta,Papke, Roger L.,Horenstein, Nicole A.
supporting information, p. 286 - 293 (2015/12/31)
The α7 nicotinic acetylcholine receptor (nAChR) is a target for control of inflammation-related phenomena via compounds that are able to selectively induce desensitized states of the receptor. Compounds that selectively desensitize, without facilitating s
1,4-Disubstituted benzenes as insecticides
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, (2008/06/13)
Compounds of formula I: wherein A, B, D, and R are as defined herein and their agriculturally acceptable salts are disclosed as effective insecticides. In addition, compositions comprising an insecticidally effective amount of a compound of Formula I in admixture with at least one agriculturally acceptable extender or adjuvant and methods of controlling insects comprising applying said compositions to locus on crops where control is desired are disclosed. It is emphasized that his abstract is provided to comply with the rules requiring an abstract that will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the claims (see 37 C.F.R. 1.72(b)).
An efficient, palladium-catalysed, amination of aryl bromides
Guari, Yannick,Van Es, Daan S.,Reek, Joost N.H.,Kamer, Paul C.J.,Van Leeuwen, Piet W.N.M.
, p. 3789 - 3790 (2007/10/03)
Aryl bromides are coupled to primary aliphatic amines, anilines and cyclic secondary amines in an efficient and selective procedure using catalytic amounts of Pd(OAc)2 and the chelating ligand 9,9-dimethyl- 4,6bis(diphenylphosphino)xanthene (Xa
Synthesis of novel succinamide derivatives having a 5,11-dihydro-6h- pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton as potent and selective M2 muscarinic receptor antagonists. II
Watanabe, Toshihiro,Kakefuda, Akio,Kinoyama, Isao,Takizawa, Kenji,Hirano, Seiko,Shibata, Hiroshi,Yanagisawa, Isao
, p. 1458 - 1469 (2007/10/03)
A series of succinamide derivatives containing the 5,11-dihydro-6H- pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton (6a-z) was prepared and evaluated for binding affinity to muscarinic receptors in vitro and for antagonism of bradycardia and salivation in vivo in comparison with AF-DX 116 (1a). Structure-activity relationships (SAR) studies in vitro indicated that the 4-(4-alkyl-1-piperazinyl)benzylamino moiety plays a crucial role in enhancing the infinity for M2 muscarinic receptors. Compound 6y, containing a 4-(4-isopropyl-1-piperazinyl)benzylmethylamino moiety, exhibited the highest affinity for M2 muscarinic receptors (pK(i) = 9.2), being 200 times as potent as 1a, and compound 6u, containing a 4-(4-ethyl-1- piperazinyl)benzylethylamino moiety, showed the highest selectivity for M2 over M3 muscarinic receptors (M3/M2 ratio=320). Both 6y and 6u antagonized the oxotremorine-induced bradycardia in rats after intravenous or oral administration. Oral evaluation in conscious dogs showed that the efficacy for increasing the heart rate was at least 3-fold greater than that of 1a.
