58351-20-5Relevant academic research and scientific papers
Affinity of 10-(4-Methylpiperazino)dibenzoxepins for Clozapine and Spiroperidol Binding Sites in Rat Brain
Harris, Terry W.,Smith, Howard E.,Mobley, Philip L.,Manier, D. Hal,Sulser, Fridolin
, p. 855 - 858 (1982)
10-(4-Methylpiperazino)dibenzoxepins were prepared and evaluated as potential antipsychotic agents using specific clozapine diazepine> binding sites in rat forebrain that are noncholinergic and nondopaminergic in nature and from which clozapine is displaced by known antipsychotic agents. Clozapine binding in the presence of atropine represents nonmuscarinic binding, while binding in the absence of atropine represents muscarinic (cholinergic) plus nonmuscarinic binding.The relative affinity for dopamine binding sites was determined by displacement of spiroperidol from binding sites in rat caudate nuclei.Thus, clozapine, its 2-chloro isomer, its dechloro analogue, and their 5H-dibenzocycloheptene and dibenzoxepin analogues have about the same relative affinity for the nonmuscarinic clozapine binding sites.At the spiroperidol (dopaminergic) sites, both the nature of the tricyclic system and the presence of chlorine atom on the tricyclic system have a substantial effect on the binding affinity.Within each series, shift of a chlorine atom from the position distal to the piperazino group to the proximal position increases the binding affinity by a factor of about nine, but removal of the chlorine atom substantially decreases the binding affinity.Nevertheless, 10-(4-methylpiperazino)dibenzoxepin has a threefold greater affinity for the dopaminergic binding sites than does clozapine itself.
AZOLE DERIVATIVE, INTERMEDIATE COMPOUND, METHOD FOR PRODUCING AZOLE DERIVATIVE, AGRICULTURAL OR HORTICULTURAL CHEMICAL AGENT, AND PROTECTIVE AGENT FOR INDUSTRIAL MATERIAL
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Paragraph 0416-0417, (2020/12/14)
It is provided a plant disease controlling agent having low toxicity to human and animals and excellent handling safety, and showing excellent controlling effects on various plant diseases and high antibiotic action to plant disease germs. A compound repr
Transition-metal-free intramolecular carbene aromatic substitution/Büchner reaction: Synthesis of fluorenes and [6,5,7]benzo-fused rings
Liu, Zhenxing,Tan, Haocheng,Wang, Long,Fu, Tianren,Xia, Ying,Zhang, Yan,Wang, Jianbo
supporting information, p. 3056 - 3060 (2015/03/30)
Intramolecular aromatic substitution and Büchner reaction have been established as powerful methods for the construction of polycyclic compounds. These reactions are traditionally catalyzed by RhII catalysts with a-diazocarbonyl compounds as the substrates. Herein a transition-metal-free intramolecular aromatic substitution/Büchner reaction is presented. These reactions use readily available N-tosylhydrazones as the diazo compound precursors and show wide substrate scope.
(Aryloxy)aryl semicarbazones and related compounds: A novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen
Dimmock, Jonathan R.,Puthucode, Ramanan N.,Smith, Jennifer M.,Hetherington, Mark,Quail, J. Wilson,Pugazhenthi, Uma,Lechler, Terry,Stables, James P.
, p. 3984 - 3997 (2007/10/03)
A number of (aryloxy)aryl semicarbazones and related compounds were synthesized and evaluated far anticonvulsant activities. After intraperitoneal injection to mice, the semicarbazones were examined in the maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ), and neurotoxicity (NT) screens. The results indicated that greater protection was obtained in the MES test than the scPTZ screen. Quantitation of approximately one-third of the compounds revealed an average protection index (PI, i.e. TD50/ED50) of approximately 9. After oral administration to rats, a number of compounds displayed significant potencies in the MES screen (ED50 of 1-5 mg/kg) accompanied by very high protection indices. In fact over half the compounds had PI figures of greater than 100, and two were in excess of 300. The compounds were essentially inactive in the scPTZ and NT screens after oral administration to rats. Various compounds displayed greater potencies and PI figures in the mouse intraperitoneal and rat oral screens than three reference clinically used drugs. The data generated supported a binding site hypothesis. Quantitative structure-activity relationships indicated a number of physicochemical parameters which contributed to activity in the MES screen. X-ray crystallography of five compounds suggested the importance of certain interatomic distances and bond angles for activity in the mouse and rat MES screens.
Dichloroacyl diphenyl ether mite ovacides
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, (2008/06/13)
Compounds having the formula STR1 wherein one of X or Y is chloro and the other is trifluoromethyl or wherein X is hydrogen and Y is chloro and methods of preparing said compounds. The compounds can be prepared by the reaction of the corresponding 1-acety
