13523-93-8Relevant academic research and scientific papers
Catalytic Aerobic Dehydrogenatin of N-Heterocycles by N-Hydoxyphthalimide
Chen, Weidong,Tang, Hao,Wang, Weilin,Fu, Qiang,Luo, Junfei
supporting information, p. 3905 - 3911 (2020/08/10)
Catalytic methods for the aerobic dehydrogenation of N-heterocycles are reported. In most cases, indoles are accessed efficiently from indolines using catalytic N-hydroxyphthalimide (NHPI) as the sole additive under air. Further studies revealed an improved catalytic system of NHPI and copper for the preparation of other heteroaromatics, for example quinolines. (Figure presented.).
Method for preparing indole compound through air oxidation catalyzed by N-hydroxyphthalimide
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Paragraph 0062-0064, (2020/11/23)
The invention discloses a method for preparing an indole compound through non-transition metal catalyzed air oxidation. According to the method, the low-cost N-hydroxyphthalimide is used as a catalystand air is used as an oxidizing agent, wherein indoline compounds are oxidized in an organic solvent, and synthesis of the indoline compounds is achieved. The method has the advantages of simple reaction operation, low reaction cost, high yield, mild conditions, no heavy metal pollution and the like.
Substituted aromatic four ring anti-fungal compound and its preparation method and application
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Paragraph 0132; 0133, (2016/10/08)
The invention relates to the technical field of pharmaceuticals, and provides a substituted aryl tetracyclic antifungal compound and pharmaceutically acceptable salts. The substituted aryl tetracyclic antifungal compound is as shown in a structural formula of the description. The invention further provides a preparation method of the compound and an application of the compound in preparing antifungal medicaments.
Scaffold hopping of sampangine: Discovery of potent antifungal lead compound against Aspergillus fumigatus and Cryptococcus neoformans
Jiang, Zhigan,Liu, Na,Dong, Guoqiang,Jiang, Yan,Liu, Yang,He, Xiaomeng,Huang, Yahui,He, Shipeng,Chen, Wei,Li, Zhengang,Yao, Jianzhong,Miao, Zhenyuan,Zhang, Wannian,Sheng, Chunquan
, p. 4090 - 4094 (2014/09/17)
Discovery of novel antifungal agents against Aspergillus fumigatus and Cryptococcus neoformans remains a significant challenge in current antifungal therapy. Herein the antifungal natural product sampangine was used as the lead compound for novel antifungal drug discovery. A series of D-ring scaffold hopping derivatives were designed and synthesized to improve antifungal activity and water solubility. Among them, the thiophene derivative S2 showed broad-spectrum antifungal activity, particularly for Aspergillus fumigatus and Cryptococcus neoformans. Moreover, compound S2 also revealed better water solubility than sampangine, which represents a promising antifungal lead compound for further structural optimization.
5-PYRIDIN-3-YL-1,3-DIHYDRO-INDOL-2-ON DERIVATIVES AND THEIR USE AS MODULATORS OF ALDOSTERONE SYNTHASE AND/OR CYP11B1
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Page/Page column 103, (2010/12/17)
The present invention provides a compound a formula (I); or a pharmaceutically acceptable salt thereof, wherein: X is CH2, O, S or-NR1; each R1 are independently C1-7alkyl or C3-8cycloalkyl; each of R
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions
Kemnitzer, William,Drewe, John,Jiang, Songchun,Zhang, Hong,Crogan-Grundy, Candace,Labreque, Denis,Bubenick, Monica,Attardo, Giorgio,Denis, Real,Lamothe, Serge,Gourdeau, Henriette,Tseng, Ben,Kasibhatla, Shailaja,Sui, Xiong Cai
, p. 417 - 423 (2008/09/20)
In our continuing effort to discover and develop apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, we explored the structure-activity relationship (SAR) of alkyl substituted pyrrole fused at the 7,8-positions. A methyl group substituted a
Substituted 4-aryl-4h-pyrrolo[2,3-h]chromenes and analogs as activators of caspases and inducers of apoptosis and the use thereof
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Page/Page column 20, (2008/06/13)
The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the Formula (I): wherein R1, R3-R5, A, D, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
