23912-50-7Relevant academic research and scientific papers
Identification of 1,5,7-Triazabicyclododecene and Polystyrene-Supported Superbases as Efficient Hydroxylaminolysis Agents of Sterically Hindered and Epimerizable Esters
Pierre, Romain,Gaigne, Frédéric,El-Bazbouz, Ghizlane,Mouis, Grégoire,Ouvry, Gilles,Tomas, Loic,Harris, Craig S.
supporting information, p. 1102 - 1106 (2018/04/24)
In modern pharmaceutical research, the need for reliable protocols for the preparation of chemical libraries in a controlled manner is quintessential to driving the Design-Make-Test cycle in drug discovery programs. In this letter, we communicate the iden
Amino acid based chiral N-amidothioureas. Acetate anion binding induced chirality transfer
Wang, Fang,He, Wen-Bin,Wang, Jin-He,Yan, Xiao-Sheng,Zhan, Ying,Ma, Ying-Ying,Ye, Li-Cai,Yang, Rui,Cai, Fu,Li, Zhao,Jiang, Yun-Bao
supporting information; experimental part, p. 11784 - 11786 (2011/12/02)
N-Amidothioureas generated from amine-dimethylated natural l-phenylalanine and its d-enantiomer bearing a chiral carbon that is by 2 atoms or 3 chemical bonds away from the anion binding site establish chiral communication upon acetate anion binding to the thiourea moiety.
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents
Dong, Ming-Xin,Zhang, Jian,Peng, Xu-Qing,Lu, Hong,Yun, Liu-Hong,Jiang, Shibo,Dai, Qiu-Yun
experimental part, p. 4096 - 4103 (2010/10/02)
By modifying the chemical structure of anti-orthopoxvirus compound ST-246, we designed and synthesized a series of tricyclononene carboxamide derivatives and tested their anti-HIV-1 activity and cytotoxicity. We found that benzoimidazol-containing compound 7g was highly effective in inhibiting HIV-1 R5 infection with an IC50 value of 0.41 μM and a selectivity index of 292, but it exhibited no significant inhibitory activity on HIV-1 reverse transcriptase, integrase and protease. CoMFA was used to analyze structure-activity relationships with good predictive power (r2 = 0.921; q2 = 0.582). Moreover, the CoMFA model showed that the length of the molecule, the amide, and the amine moieties all played crucial roles in anti-HIV activity. These results suggest that 7g may serve as a lead for the development of novel anti-HIV-1 therapies. A series of tricyclononene carboxamide derivatives based on anti-orthopoxvirus compound ST-246 were synthesized and characterized as novel anti-HIV-1 agents.
STUDIES ON THE KINETICS OF RACEMIZATION OF 2,4-DISUBSTITUTED-5(4H)-OXAZOLONES
Slebioda, Marek,St-Amand, Marc A.,Chen, Francis M. F.,Benoiton, N. Leo
, p. 2540 - 2544 (2007/10/02)
The kinetics of racemization of 2,4-disubstituted-5(4H)-oxazolones obtained from N-acetyl, N-benzoyl, and N-benzyloxycarbonylglycyl-L-leucine, -valine, and -phenylalanine have been studied in several solvents alone and in the presence of tertiary amines.T
