4483-00-5Relevant academic research and scientific papers
Synthesis, biological activity screening and molecular modeling study of acylaminoacetamide derivatives
Coban, Gunes,Kose, Fadime Aydin,Kirmizibayrak, Petek Ballar,Pabuccuoglu, Varol
, p. 3710 - 3729 (2015/09/07)
In this study, non-rigid analogs of thalidomide have been designed in order to develop potentially active, more effective and safer lead molecules for disorders caused or contributed by inflammation. Five different series of acylaminoacetamide compounds were synthesized, and the biological inhibitory potency of the title compounds has been determined by evaluating their effects on COX-2 isoenzyme expression and PGE2 production in A549 (human lung adenocarcinoma) cell lines. Among the studied series, N-[2-(isopropylamino)-2-oxoethyl]isonicotinamide is the most active inhibitory compound on COX-2 isoenzyme expression, and N-[2-oxo-2-(pyrolydine-1-yl)etyl]isonicotinamide is the most active inhibitory compound on the biosynthesis of PGE2. Molecular docking studies and molecular dynamics simulations were also applied to investigate non-covalent interactions of the most active compounds inside the active side of the crystal structure of murine cyclooxygenase 2 (mCOX-2) isoenzyme.
An efficient synthesis of N,N-disubstituted 5-aminooxazoles
Mazurkiewicz
, p. 941 - 943 (2007/10/02)
N,N-Disubstituted 5-aminooxazoles including 4-unsubstituted derivatives, were prepared from the corresponding α-acylamino amides by treatment with dibromotriphenylphosphorane and triethylamine in refluxing dichloromethane in a novel, convenient and effici
PARTICIPATION D'UN GROUPE AMIDE A LA FORMATION DE SELS DE DIOXOLANNE-1,3 YLIUM-2; MODELE BIOMIMETIQUE DE REACTION DE PEPTIDATION
Mestdagh, Helene,Pancrazi, Ange
, p. 3399 - 3414 (2007/10/02)
An amide group is shown to be capable of intramolecular participation in the formation of an 1,3-dioxolan 2-ylium cation giving a tricyclic organic cation of a new type 5a,b.This cation may be considered as a model of an electrophilic intermediate which m
