Chemistry, like all the natural sciences, begins with the direct observation of nature¡ª in this case, of matter.139755-85-4, Name is 5-(2-Ethoxy-5-((4-(2-hydroxyethyl)piperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one, SMILES is O=C1C(N(C)N=C2CCC)=C2N=C(C3=CC(S(=O)(N4CCN(CCO)CC4)=O)=CC=C3OCC)N1, belongs to piperazines compound. In a document, author is Jankowska, Agnieszka, introduce the new discover, Product Details of 139755-85-4.
Novel anilide and benzylamide derivatives of arylpiperazinylalkanoic acids as 5-HT1A/5-HT7 receptor antagonists and phosphodiesterase 4/7 inhibitors with procognitive and antidepressant activity
A library of novel anilide and benzylamide derivatives of omega-(4-(2-methoxyphenyl)piperazin-1-yl)alkanoic acids as combined 5-HT1A/5-HT7 receptor ligands and phosphodiesterase PDE4B/PDE7A inhibitors was designed using a structure-based drug design approach. The in vitro studies of 33 newly synthesized compounds (7-39) allowed us to identify 22 as the most promising multifunctional 5-HT1A/5-HT7 receptor antagonist (5-HT1AKi= 8 nM, K-b = 0.04 nM; 5-HT7 K-1 = 451 nM, K-b = 460 nM) with PDE4B/PDE7A inhibitory activity (PDE4B IC50 = 80.4 mu M; PDE7A IC50 = 151.3 mu M). Compound 22 exerted a very good ability to passively penetrate through biological membranes and a high metabolic stability in vitro. Moreover, the pharmacological evaluation of 22 showed its procognitive and antidepressant properties in rat behavioral tests. Compound 22 at a dose of 3 mg/kg (i.p.) significantly reversed MK-801-induced episodic memory deficits in the novel object recognition test, while at a dose of 10 mg/kg (i.p.) reduced the immobility time of animals (by about 34%) in the forced swimming test. The antidepressant-like effect produced by compound 22 was stronger than that of escitalopram used as a reference drug. This study opens a new perspective in the search for efficacious drugs for the treatment of cognitive and depressive disorders. (C) 2020 Elsevier Masson SAS. All rights reserved.
The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 139755-85-4 is helpful to your research. Product Details of 139755-85-4.
Reference:
Piperazine – Wikipedia,
,Piperazines – an overview | ScienceDirect Topics