Isopropyl Amide Derivatives of Potent and Selective Muscarinic M2 Receptor Antagonists.

ChemInform ◽  
2004 ◽  
Vol 35 (34) ◽  
Author(s):  
Anandan Palani ◽  
Sundeep Dugar ◽  
John W. Clader ◽  
William J. Greenlee ◽  
Vilma Ruperto ◽  
...  
2004 ◽  
Vol 14 (7) ◽  
pp. 1791-1794 ◽  
Author(s):  
Anandan Palani ◽  
Sundeep Dugar ◽  
John W. Clader ◽  
William J. Greenlee ◽  
Vilma Ruperto ◽  
...  

Author(s):  
Agnieszka Jankowska ◽  
Grzegorz Satała ◽  
Artur Świerczek ◽  
Krzysztof Pociecha ◽  
Anna Partyka ◽  
...  

Aims: 5-HT1A receptor antagonists constitute a potential group of drugs in the treatment of CNS diseases. The aim of this study was to search for new procognitive and antidepressant drugs among amide derivatives of aminoalkanoic acids with 5-HT1A receptor antagonistic properties. Materials & methods: Thirty-three amides were designed and evaluated in silico for their drug-likeness. The synthesized compounds were tested in vitro for their 5-HT1A receptor affinity and functional profile. Moreover, their selectivity over 5-HT7, 5-HT2A and D2 receptors and ability to inhibit phosphodiesterases were evaluated. Results: A selected 5-HT1A receptor antagonist 20 ( Ki = 35 nM, Kb = 4.9 nM) showed procognitive and antidepressant activity in vivo. Conclusion: Novel 5-HT1A receptor antagonists were discovered and shown as potential psychotropic drugs.


2013 ◽  
Vol 9 (7) ◽  
pp. 920-925 ◽  
Author(s):  
Yi Bi ◽  
Jinyi Xu ◽  
Fei Sun ◽  
Xiaoming Wu ◽  
Wencai Ye ◽  
...  

Author(s):  
Vasil Tsanov ◽  
Hristo Tsanov

Background:: This article concentrates on the processes occurring in the medium around the cancer cell and the transfer of glycoside amides through their cell membrane. They are obtained by modification of natural glycoside-nitriles (cyano-glycosides). Hydrolysis of starting materials in the blood medium and associated volume around physiologically active healthy and cancer cells, based on quantum-chemical semi-empirical methods, is considered. Objective:: Based on the fact that the cancer cell feeds primarily on carbohydrates, it is likely that organisms have adapted to take food containing nitrile glycosides and / or modified forms to counteract "external" bioactive activity. Cancers, for their part, have evolved to create conditions around their cells that eliminate their active apoptotic forms. This is far more appropriate for them than changing their entire enzyme regulation to counteract it. In this way, it protects itself and the gene sets and develops according to its instructions. Methods:: Derived pedestal that closely defines the processes of hydrolysis in the blood, the transfer of a specific molecular hydrolytic form to the cancer cell membrane and with the help of time-dependent density-functional quantum- chemical methods, its passage and the processes of re-hydrolysis within the cell itself, to forms causing chemical apoptosis of the cell - independent of its non-genetic set, which seeks to counteract the process. Results:: Used in oncology it could turn a cancer from a lethal to a chronic disease (such as diabetes). The causative agent and conditions for the development of the disease are not eliminated, but the amount of cancer cells could be kept low for a long time (even a lifetime). Conclusion:: The amide derivatives of nitrile glycosides exhibit anti-cancer activity, the cancer cell probably seeks to displace hydrolysis of these derivatives in a direction that would not pass through its cell membrane and the amide- carboxyl derivatives of nitrile glycosides could deliver extremely toxic compounds within the cancer cell itself and thus block and / or permanently damage its normal physiology.


ACS Omega ◽  
2021 ◽  
Author(s):  
Qiang Shang ◽  
Xiaobo Zhou ◽  
Ming-Rong Yang ◽  
Jing-Guang Lu ◽  
Yu Pan ◽  
...  

ChemInform ◽  
2010 ◽  
Vol 31 (8) ◽  
pp. no-no
Author(s):  
Matthew J. Tozer ◽  
Ildiko M. Buck ◽  
Tracey Cooke ◽  
S. Barret Kalindjian ◽  
Iain M. McDonald ◽  
...  

MedChemComm ◽  
2018 ◽  
Vol 9 (6) ◽  
pp. 1069-1075 ◽  
Author(s):  
Moustafa T. Gabr ◽  
Mohammed S. Abdel-Raziq

A biphenyl amide–tryptamine hybrid as a selective 5-HT2B antagonist.


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