Synthesis of Some Nefopam Analogues as Potential Analgesics

2002 ◽  
Vol 55 (9) ◽  
pp. 577 ◽  
Author(s):  
A. E. Rosamilia ◽  
P. A. Mayes ◽  
R. Papadopoulos ◽  
E. M. Campi ◽  
W. R. Jackson ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Narcotic Analgesic ◽  
Noradrenaline Uptake ◽  
Antagonist Activity ◽  
Ester Derivative ◽  
Uptake Of Noradrenaline ◽  
Derivatives Of

Some derivatives of the non-narcotic analgesic nefopam containing amidine and guanidine substituents have been prepared and their analgesic activity assessed by their ability to block the uptake of noradrenaline. The compounds have been shown to inhibit noradrenaline uptake but they also display possible α1 antagonist activity at higher concentration. An ester derivative was also active and was more selective as it did not exhibit α1 adrenoreceptor antagonism.

Synthesis and Analgesic Activity of 3,7-dimethylpurine-2,6-dion-1-yl Derivatives of Acetic and Butanoic Acid

2014 ◽  
Vol 11 (10) ◽  
pp. 1204-1213 ◽  
Author(s):  
Mal.gorzata Zygmunt ◽  
Pawe.l Zmudzki ◽  
Graz.yna Chl.on.-Rzepa ◽  
Jacek Sapa ◽  
Maciej Pawl.owski
Keyword(s):  
Analgesic Activity ◽  
Butanoic Acid ◽  
Derivatives Of

The Through-Bond Interaction of a Sulfur Lone Pair with Oxygenated Substituents in the Thiacyclohexane Framework

2005 ◽  
Vol 58 (7) ◽  
pp. 531
Author(s):  
Laura Andrau ◽  
Jonathan M. White
Keyword(s):  
Low Temperature ◽  
Crystal Structures ◽  
Bond Distance ◽  
Lone Pair ◽  
X Ray ◽  
Ester Derivative ◽  
Bond Interaction ◽  
Derivatives Of ◽  
Electron Demand

Low-temperature X-ray crystal structures were determined on a range of derivatives of 4-thiacyclohexanol 5a of varying electron demand with a view to finding evidence for a through-bond interaction between the sulfur lone pair and the oxygenated substituent. In contrast to earlier suggestions, plots of C–OR bond distance versus pKa (ROH) showed that any interaction between the sulfur and the OR group is unlikely to be of a through-bond origin. Furthermore, unimolecular solvolysis rate measurements on the nosylate ester derivative 5g showed that the sulfur actually retards the reaction slightly in comparison with the corresponding sulfur-free analogue 6.

Novel, Potent, and Orally Active Substance P Antagonists: Synthesis and Antagonist Activity of N-Benzylcarboxamide Derivatives of Pyrido[3,4-b]pyridine

1995 ◽  
Vol 38 (16) ◽  
pp. 3106-3120 ◽  
Author(s):  
Hideaki Natsugari ◽  
Yoshinori Ikeura ◽  
Yutaka Kiyota ◽  
Yuji Ishichi ◽  
Takenori Ishimaru ◽  
...  
Keyword(s):  
Substance P ◽  
Active Substance ◽  
Antagonist Activity ◽  
Substance P Antagonists ◽  
Orally Active ◽  
Derivatives Of

ChemInform Abstract: Synthesis and Analgesic Activity of Nitrogen-Heterocyclic Derivatives of Embelin.

ChemInform ◽  
1990 ◽  
Vol 21 (4) ◽  
Author(s):  
S. M. JAIN ◽  
R. KANT ◽  
A. N. SARIN ◽  
S. K. DHAR ◽  
K. L. DHAR
Keyword(s):  
Analgesic Activity ◽  
Heterocyclic Derivatives ◽  
Derivatives Of ◽  
Nitrogen Heterocyclic

scholarly journals Syntheses of N-Acyl Derivatives of α-Methyl-3, 4-methylenedioxyphenethylamine and their Analgesic Activity.

1963 ◽  
Vol 11 (5) ◽  
pp. 654-657 ◽  
Author(s):  
Keijiro Takagi ◽  
Yutaka Kasuya ◽  
Kyo Fujie ◽  
Minoru Watanabe ◽  
Setsuko Kayaoka
Keyword(s):  
Analgesic Activity ◽  
Derivatives Of ◽  
Acyl Derivatives

Synthesis and Analgesic Activity of Some Deaza Derivatives of Anpirtoline

1999 ◽  
Vol 332 (1) ◽  
pp. 13-18 ◽  
Author(s):  
Stanislav Rádl ◽  
Petr Hezky ◽  
Jan Proška ◽  
Ivan Krejcí
Keyword(s):  
Analgesic Activity ◽  
Derivatives Of

Synthesis, cytotoxicity and calcium antagonist activity of novel imidazolyl derivatives of 1,8-acridinediones

2011 ◽  
Vol 8 (4) ◽  
pp. 983-991 ◽  
Author(s):  
A. Jamalian ◽  
R. Miri ◽  
O. Firuzi ◽  
M. Amini ◽  
A. A. Moosavi-Movahedi ◽  
...  
Keyword(s):  
Calcium Antagonist ◽  
Antagonist Activity ◽  
Derivatives Of

Synthesis and α1-antagonist activity of derivatives of 4-chloro-5-{4-[2-(2-methoxyphenoxy)-ethyl]-1-piperazinyl}-3(2H)-pyridazinone

2000 ◽  
Vol 35 (7-8) ◽  
pp. 773-779 ◽  
Author(s):  
Giovannella Strappaghetti ◽  
Roberta Barbaro ◽  
Gabrielle Marucci
Keyword(s):  
Antagonist Activity ◽  
Derivatives Of

Structure-based design and synthesis of conformationally constrained derivatives of methyl-piperidinopyrazole (MPP) with estrogen receptor (ER) antagonist activity

2021 ◽  
pp. 105554
Author(s):  
Mahmoud A. Ragab ◽  
Mohamed Elagawany ◽  
Hoda Daabees ◽  
Al-Shaimaa F. Ahmed ◽  
Eman M. Awad ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Antagonist Activity ◽  
Conformationally Constrained ◽  
Design And Synthesis ◽  
Derivatives Of
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