50971-75-0Relevant academic research and scientific papers
Hydrogenated acridine derivative and its application
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Paragraph 0154; 0155; 0156; 0160, (2016/10/08)
The invention relates to the field of chemical synthesis, and particularly relates to a compound with the general formula being Y-L-X and an application of the compound serving as a calcium channel blocking agent or/and an acetylcholinesterase inhibitor. The compound with the general formula being Y-L-X can be used for adjusting calcium homeostasis and treating cardiovascular diseases, stroke or dementia.
Synthesis, biological evaluation and molecular docking study of novel piperidine and piperazine derivatives as multi-targeted agents to treat Alzheimer's disease
Meena, Poonam,Nemaysh, Vishal,Khatri, Manisha,Manral, Apra,Luthra, Pratibha Mehta,Tiwari, Manisha
, p. 1135 - 1148 (2015/03/04)
Development of Multi-Target Directed Ligands (MTDLs) has emerged as a promising approach for targeting complex etiology of Alzheimer's disease (AD). Following this approach, a new series of N′-(4-benzylpiperidin-/piperazin-/benzhydrylpiperazin-1-yl)alkylamine derivatives were designed, synthesized and biologically evaluated as inhibitors of cholinesterases (ChEs), amyloid-beta (Aβ) self aggregation and also for their radical scavenging activity. The in vitro studies showed that the majority of synthesized derivatives strongly inhibited acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values in the low-nanomolar range, and were clearly more potent than the reference compound donepezil in this regard. Among them, inhibitors 5h and 5k, strongly inhibited AChE, with IC50 value of 6.83 nM and 2.13 nM, respectively, and particularly, compound 5k was found to be highly selective for AChE (～38-fold). Moreover, both kinetic analysis of AChE inhibition and the docking study suggested that 5k binds simultaneously to catalytic active site and peripheral anionic site of AChE. Besides, these compounds also exhibited greater ability to inhibit self-induced Aβ1-42 aggregation at 25 μM with percentage inhibition from ～54% to 89% and specially compound 5k provided highest inhibition (88.81%). Also, the derivatives containing methoxy and hydroxy groups showed potent oxygen radical absorbance capacity (ORAC) ranging from 2.2- to 4.4-fold of the Trolox value. Furthermore, results of ADMET studies suggested that all compounds exhibited appropriate drug like properties. Taken together, these results suggest that 5k might be a promising lead compound for further AD drug development.
Cyanoguanidine compounds
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, (2008/06/13)
A cyanoguanidine compound of the following formula: is disclosed. A cyanoguanidine compound of the present invention possess a high specificity for tumor cells. Also disclosed are methods for preparing a cyanoguanidine compound.
Quantitative structure-activity analyses of novel hydroxyphenylurea derivatives as antioxidants
Nakao, Kazuya,Shimizu, Ryo,Kubota, Hitoshi,Yasuhara, Mikiko,Hashimura, Yoshimasa,Suzuki, Toshikazu,Fujita, Toshio,Ohmizu, Hiroshi
, p. 849 - 868 (2007/10/03)
A series of substituted hydroxyphenylureas was synthesized, the chemical structure of which was designed based on structures of natural antioxidants, vitamin E (α-tocopherol) and uric acid. They exhibited high inhibitory activity against lipid peroxidation. In order to gain an insight into the mechanism of the inhibition reaction, we analyzed their structure-activity relationships quantitatively. Electronic and steric effects of substituents on the phenolic hydroxyl group were shown to be of importance in governing the inhibitory potency. An increase in the electron donating property of substituents toward the phenolic hydroxyl group enhanced the antioxidative activity by the stabilization of an electron-deficient radical-type transition state. The steric shielding by ortho-substituents stabilized the phenoxy radicals formed following the transition state. Derivatives having the carboxyl group were only weakly active presumably because of an intermolecular ion-dipole interaction of the phenolic hydroxyl group with the carboxylate anion which could retard the formation of the transition state. Copyright (C) 1998 Elsevier Science Ltd.
Synthesis and histamine H1-receptor antagonist activity of 4-(diphenylmethyl)-1-piperazine derivatives with a terminal heteroaryl or cycloalkyl amide fragment
Orjales,Gil-Sanchez,Alonso-Cires,Labeaga,Mosquera,Berisa,Ucelay,Innerarity,Corcostegui
, p. 813 - 818 (2007/10/03)
New 4-(diphenylmethyl)-1-piperazine derivatives with a terminal heteroaryl or cycloalkyl amide fragment were synthesized and evaluated for their antihistaminic anticholinergic and antiallergic activities. Tested compounds were found to be moderate to potent in vitro (guinea-pig ileum) histamine H1-receptor antagonists. Derivatives with a four methylene chain (1e-1h) were as potent in vivo (capillary permeability in rats) as cetirizine; the heteroaryl derivatives 1e and 1h were found to be the most active agents. These compounds displayed only weak in vitro (guinea-pig ileum) muscarinic M3-receptor antagonist activity. Compounds 1e and 1g were about 100 times more potent than ketotifen in preventing the compound 48/80-induced histamine release from rat peritoneal mast cells. Derivatives 1e, 1f and 1h did not modify the spontaneous motor activity in rats at 100 mg/kg po. Compound 1e has been selected for further studies.
THIAZOLIDINECARBOXYLIC ACID AMIDE DERIVATIVES AND THEIR THERAPEUTIC USES
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, (2008/06/13)
Thiazolidinecarboxylic acid amides having combined antiallergic and antiasthmatic activities with an antagonist activity against platelet Activating Factor and having the following general formula (I) STR1
