341998-57-0Relevant articles and documents
Discovery of novel indoleaminopyrimidine NIK inhibitors based on molecular docking-based support vector regression (SVR) model
Ye, Qing,Li, Qiu,Gao, Anhui,Ying, Huazhou,Cheng, Gang,Chen, Jing,Che, Jinxin,Li, Jia,Dong, Xiaowu,Zhou, Yubo
, p. 38 - 45 (2019/02/07)
A set of NF-κB-inducing kinase (NIK) inhibitors was used to develop a molecular docking-based QSAR model by using nonlinear regression method. The accuracy of the QSAR model was remarkably improved by integrating the docking scores and key interaction pro
Meridianin D Analogues Display Antibiofilm Activity against MRSA and Increase Colistin Efficacy in Gram-Negative Bacteria
Huggins, William M.,Barker, William T.,Baker, James T.,Hahn, Nicholas A.,Melander, Roberta J.,Melander, Christian
, p. 702 - 707 (2018/06/04)
In the last 30 years, development of new classes of antibiotics has slowed, increasing the necessity for new options to treat multidrug resistant bacterial infections. Development of antibiotic adjuvants that increase the effectiveness of currently available antibiotics is a promising alternative approach to classical antibiotic development. Reports of the ability of the natural product meridianin D to modulate bacterial behavior have been rare. Herein, we describe the ability of meridianin D to inhibit biofilm formation of methicillin-resistant Staphylococcus aureus (MRSA) and to increase the potency of colistin against colistin-resistant and sensitive Gram-negative bacteria. Analogues were identified that are capable of inhibiting and dispersing MRSA biofilms and lowering the colistin MIC to below the CLSI breakpoint against Acinetobacter baumannii, Klebsiella pneumoniae, and Escherichia coli.
Towards the syntheses of N-H and N-alkylated derivatives of meridianins
Simon, Ga?lle,Couthon-Gourves, Hélène,Haelters, Jean-Pierre,Corbel, Bernard,Kervarec, Nelly,Michaud, Fran?ois,Meijer, Laurent
, p. 793 - 801 (2008/03/29)
(Chemical Equation Presented) Novel N-H and N-alkylated derivatives of meridianins have been synthesized as potential antitumor agents by a two-step conversion of N-tosyl-3-acetylindoles or N-alkyl-3-acetylindoles to the corresponding enaminones using DMF-DMA, with or without added pyrrolidine. Further cyclization with guanidine gave the corresponding 2-aminopyrimidines. The structures of the compounds, thus obtained, were proved by 1H and 13C NMR spectroscopy, NOE experiments and X-ray analysis.
Synthesis of the indole alkaloids meridianins from the tunicate Aplidium meridianum
Fresneda, Pilar M,Molina, Pedro,Bleda, Juan A
, p. 2355 - 2363 (2007/10/03)
The marine natural products meridianins A and C-E have been synthesized for the first time starting from the appropriate N-tosyl-3-acetylindole. A facile two-step conversion of N-tosyl-3-acetylindoles to the corresponding meridianins by treatment with dimethylformamide dimethylacetal and further cyclization of the resulting enaminone with aminoguanidine is described. This method has also been applied for the preparation of the 3-[(2-amino)pyrimidin-4-yl]-7-azaindole.
Synthetic studies towards the 2-aminopyrimidine alkaloids variolins and meridianins from marine origin
Fresneda, Pilar M.,Molina, Pedro,Delgado, Santiago,Bleda, Juan A.
, p. 4777 - 4780 (2007/10/03)
A nine-step synthesis of 9-amino-4-methoxypyrido[3',2':4,5]pyrrolo[1,2- c]pyrimidine, a tricyclic ring system present in the marine alkaloids variolins is described. The natural marine products meridianins C-E have been synthesized for the first time starting from N-protected 3-acylindoles. (C) 2000 Elsevier Science Ltd.
