125330-80-5Relevant academic research and scientific papers
Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective κ opioid receptor antagonists
He, Guangchao,Peng, Kewen,Song, Qiao,Wang, Junwei,Xu, Anhua,Xu, Yungen,Zhu, Qihua
, (2020/05/19)
Aminobenzyloxyarylamide derivatives 1a-i and 2a-t were designed and synthesized as novel selective κ opioid receptor (KOR) antagonists. The benzoyl amide moiety of LY2456302 was changed into N-hydroxybenzamide and benzisoxazole-3(2H)-one to investigate whether it could increase the binding affinity or selectivity for KOR. All target compounds were evaluated in radioligand binding assays for opioid receptor binding affinity. These efforts led to the identification of compound 1c (κ Ki = 179.9 nM), which exhibited high affinity for KOR. Moreover, the selectivity of KOR over MOR and DOR increased nearly 2-fold and 7-fold, respectively, compared with (±)LY2456302.
Broad assessment of bioactivity of a collection of spiroindane pyrrolidines through “cell painting”
Boskovic, Zarko,Douglas, Justin,Garza, Nathan,Pearson, Zachary,Singh, Manvendra
supporting information, (2020/05/25)
A collection of small molecules has been synthesized by composing photo-cycloaddition, C–H functionalization, and N-capping strategies. Multidimensional biological fingerprints of molecules comprising this collection have been recorded as changes in cell
Synthesis and the keto-enol equilibrium of 2-acyl lactams
Nenajdenko,Gololobov,Zakurdaev,Balenkova
, p. 2473 - 2482 (2007/10/03)
Condensation of N-substituted lactams with carboxylic acid esters was studied. A wide range of substituted 2-acyl lactams with different ring sizes were synthesized. The structure of 2-acyl lactams (primarily, the ring size) was found to influence the ket
A PRACTICAL PREPARATION OF Δ1-2-SUBSTITUTED AND Δ1-2,3-DISUBSTITUTED PYRROLINES
Haslego, Mark L.,Maryanoff, Cynthia A.,Scott, Lorraine,Sorgi, Kirk L.
, p. 643 - 647 (2007/10/02)
Addition of N-vinylpyrrolidinone and an ester to NaH in THF effects acylation and affords keto lactams (1) in high yields.Hydrolysis of 1 in strong acid generates Δ1-2-substituted pyrrolines (2) in good yield.Keto lactams (1) can be further alkylated and hydrolyzed to produce Δ1-2,3-disubstituted pyrrolines (4) in good isolated yield.
