Discovery of Novel Indole Derivatives as Fructose-1,6-bisphosphatase Inhibitors and X-ray Cocrystal Structures Analysis

Author(s):  
Xiaoyu Wang ◽  
Rui Zhao ◽  
Wenming Ji ◽  
Jie Zhou ◽  
Quan Liu ◽  
...  
2021 ◽  
Vol 66 ◽  
pp. 61-71
Author(s):  
Tahereh Heidarzadeh ◽  
Navabeh Nami ◽  
Daryoush Zareyee

The principal aim of this research is using biosynthesized ZnO-CaO nanoparticles (NPs) for preparation of indole derivatives. ZnO-CaO NPs have been prepared using Zn(CH3COO)2 and eggshell waste powder in solvent-free conditions. Morphology and structure of NPs were determined by FT-IR, X-ray diffraction (XRD), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and energy dispersive spectra (EDS). It was used as a highly efficient catalyst for the synthesis of indole derivatives. Some indole derivatives were synthesized by the reaction of indole, formaldehyde, aromatic and aliphatic amines in the presence of ZnO-CaO NPs (5 mol%) in ethanol under reflux conditions. The assigned structure was further established by CHN analyses, NMR, and FT-IR spectra. Because of excellent capacity, the exceedingly simple workup and good yield, eco-friendly catalyst ZnO-CaO NPs were proved to be a good catalyst for this reaction.


Synthesis ◽  
2019 ◽  
Vol 52 (08) ◽  
pp. 1215-1222
Author(s):  
Robert Connon ◽  
Laura Carroll ◽  
Patrick J. Guiry

Herein, we report a base-promoted Zn(II)–bis(oxazoline)-catalyzed one-pot Friedel–Crafts alkylation/Michael addition of 3-(indol-4-yl)acrylonitrile derivatives with trans-β-nitrostyrenes to yield the tricyclic core of the ergoline skeleton in up to 71% yield and 85% ee. During the purification of 3-(indol-4-yl)acrylonitrile, the key substrate for catalytic studies, a novel trans-cis-trans-cyclobutane derivative, thought to be formed via a [2+2] light-promoted cycloaddition, was identified by X-ray crystallographic analysis. Finally, a novel class of 4-substituted bis(indole)methane derivatives were serendipitously prepared in excellent yield by reacting 4-substituted indole derivatives with 4-nitrobenzaldehyde. One bis(indole)methane was characterized by X-ray crystallographic analysis.


1984 ◽  
Vol 259 (14) ◽  
pp. 8915-8916
Author(s):  
B A Seaton ◽  
R L Campbell ◽  
G A Petsko ◽  
D R Rose ◽  
I Edelstein ◽  
...  

2017 ◽  
Vol 13 ◽  
pp. 2304-2309 ◽  
Author(s):  
Mio Matsumura ◽  
Mizuki Yamada ◽  
Atsuya Muranaka ◽  
Misae Kanai ◽  
Naoki Kakusawa ◽  
...  

The parent benzophospholo[3,2-b]indole was prepared by the reaction of dichlorophenylphosphine with a dilithium intermediate, which was prepared in two steps from 2-ethynyl-N,N-dimethylaniline. Using the obtained benzophosphole-fused indole as a common starting material, simple modifications were carried out at the phosphorus center of the phosphole, synthesizing various functionalized analogs. The X-ray structure analysis of trivalent phosphole and phosphine oxide showed that the fused tetracyclic moieties are planar. The benzophosphole-fused indoles, such as phosphine oxide, phospholium salt, and borane complex, exhibited strong photoluminescence in dichloromethane (Φ = 67–75%).


2017 ◽  
Vol 41 (7) ◽  
pp. 427-429
Author(s):  
Demin Ren ◽  
Guoqiang Kuang ◽  
Xiaolian Hu ◽  
Xiaofang Li

The 1,3-dipolar cycloaddition of azomethine ylide, generated in situ from isatin and sarcosine, to 5-arylmethylidene-1-phenyl-6,7-dihydro-1 H-indazol-4(5 H)-ones afforded novel 1′-methyl-4′-aryl-1-phenyl-6,7-dihydrodispiro[indazole-5,3′-pyrrolidine-2′,3″-indole]-2″,4(1 H,1″ H)-diones in moderate yields. The structures of all the products were characterised thoroughly by NMR, IR, HRMS, together with X-ray crystallographic analysis.


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