182919-58-0Relevant articles and documents
Synthesis, bioactivity and molecular modeling studies on potential anti-Alzheimer piperidinehydrazide-hydrazones
Parlar, Sulunay,Sayar, Gozde,Tarikogullari, Ayse Hande,Karadagli, Sumru Sozer,Alptuzun, Vildan,Erciyas, Ercin,Holzgrabe, Ulrike
, p. 888 - 900 (2019)
A group of N-benzylpiperidine-3/4-carbohydrazide-hydrazones were designed, synthesized and evaluated for acetylcholinesterase (AChE), butyrylcholinesterase (BuChE)activities, Aβ42 self-aggregation inhibitory potentials, and antioxidant capacities, in vitro. All of the compounds displayed eeAChE and huAChE inhibitory activity in a range of IC50 = 5.68–11.35 μM and IC50 = 8.80–74.40 μM, respectively and most of the compounds exhibited good to moderate inhibitory activity on BuChE enzyme. Kinetic analysis and molecular modeling studies were also performed for the most potent compounds (1g and 1j). Not only the molecular modeling studies but also the kinetic analysis suggested that these compounds might be able to interact with the catalytic active site (CAS)and the peripheral anionic site (PAS)of the enzymes. In the light of the results, compound 1g and compound 1j may be suggested as lead compounds for multifunctional therapy of AD.
Synthesis, biological evaluation, docking study and ulcerogenicity profiling of some novel quinoline-2-carboxamides as dual COXs/LOX inhibitors endowed with anti-inflammatory activity
Abdelrahman, Mostafa H.,Youssif, Bahaa G.M.,abdelgawad, Mohamed A.,Abdelazeem, Ahmed H.,Ibrahim, Hussein M.,Moustafa, Abd El Ghany A.,Treamblu, Laurent,Bukhari, Syed Nasir Abbas
, p. 972 - 985 (2017)
A series of novel quinoline-2-carboxamides 15–28 was synthesized and evaluated in?vitro as dual COXs/LOX inhibitors. Compounds 19 and 27 exhibited the highest potency and selectivity for COX-2 inhibitory activity (IC50?=?1.21 and 1.13?μM, respe
Novel 1,5-diaryl pyrazole-3-carboxamides as selective COX-2/sEH inhibitors with analgesic, anti-inflammatory, and lower cardiotoxicity effects
Hendawy,Gomaa, Hesham A.M.,Alzarea, Sami I.,Alshammari, Mutariah S.,Mohamed, Fatma A.M.,Mostafa, Yaser A.,Abdelazeem, Ahmed H.,Abdelrahman, Mostafa H.,Trembleau, Laurent,Youssif, Bahaa G.M.
, (2021/09/01)
COX-2 selective drugs have been withdrawn from the market due to cardiovascular side effects, just a few years after their discovery. As a result, a new series of 1,5-diaryl pyrazole carboxamides 19–31 was synthesized as selective COX-2/sEH inhibitors wit
SUBSTITUTED CYCLOHEXYL DERIVATIVES AS NK-3 RECEPTOR ANTAGONISTS
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Page/Page column 35, (2010/11/25)
The present invention relates to the compounds of formula (I): wherein A,B, n, X, Y, Z, R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them and their use in treating diseases mediated by neurokinin-3 (NK-3) receptors. These compounds can thus be used in methods of treatment to suppress and treat such disorders.
A convenient route to 1-benzyl 3-aminopyrrolidine and 3-aminopiperidine
Jean, Ludovic,Baglin, Isabelle,Rouden, Jacques,Maddaluno, Jacques,Lasne, Marie-Claire
, p. 5645 - 5649 (2007/10/03)
1-Benzyl 3-aminopyrrolidine 1 and 1-benzyl 3-aminopiperidine 2 were prepared rapidly mainly in aqueous conditions in 55 and 75% yields, respectively, on a multi-gram scale starting from inexpensive and commercially available starting materials. The key step involved the Curtius rearrangement mediated by sodium nitrite and trifluoroacetic acid of the appropriate acylhydrazides. All the reactions (except LAH reductions) were performed in water.