622372-77-4Relevant academic research and scientific papers
Design, synthesis, biological evaluation and molecular docking study of novel pyridoxine-triazoles as anti-Alzheimer's agents
Bhimaneni, Saipriyanka,Flora, S. J. S.,Pal, Tiyas,Sharma, Abha
, p. 26006 - 26021 (2020)
A series of multi-target natural product-pyridoxine based derivatives were designed, synthesized, characterized and evaluated as anti-Alzheimer agents. In vitro testing revealed the multi-functional properties of compounds such as inhibition of acetylcholinesterase (AChE), antioxidant and metal chelation. Among the series, 5i derivative was found most potent AChE inhibitor, possess antioxidant potential and chelating metal ions. Further binding interaction of 5i with AChE was studied using molecular docking, showed interaction with both PAS and CAS site of AChE. In silico predictions were also performed to predict toxicity and ADME properties of the molecule 5i and found within drug likeness range. Therefore, 5i could be a promising multi-functional compound that can be used for further development of novel drug for Alzheimer disease.
P-benzoquinone diazide core skeleton derivative as well as preparation method and application thereof
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Paragraph 0046; 0136-0140, (2020/03/17)
The invention relates to a p-benzoquinone diazide core skeleton derivative and a preparation method and application, thereof, belongs to. the field of organic chemistry, and can effectively treat-ovarian-ovarian cancer-carcinoma STAT3-ovarian, cancer-ATG4
Naphthoquinone-fused triazole core skeleton derivative compound, preparation method and application thereof
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Paragraph 0043; 0093-0097; 0182-0186; 0296-0300, (2019/10/01)
The invention relates to a naphthoquinone-fused triazole core skeleton derivative compound, relates to a preparation method and application of the naphthoquinone-triazole core skeleton derivative compound, and belongs to the field of organic chemistry. Th
Synthesis of novel pyrazoline-based bis(1,2,3-triazole) scaffolds via click chemistry
Kiran, Kothuri,Ashok, Dongamanti,Rao, Boddu Ananda,Sarasija, Madderla,Rao, Alapati Srinivas
, p. 241 - 251 (2017/05/09)
A series of novel bis(1,2,3-triazoles) derivatives 7a-m were synthesized by the 1,3-dipolar cycloaddition (click-reaction) of 1-methyl-3,5-bis(2-(prop-2-yn-1-yloxy)phenyl)-4,5-dihydro-1H-pyrazole (5) with various aralkyl azides 6a-m in the presence of sod
Synthesis of New P-substituted Iminophosphoranes Via Staudinger Raction and Antimicrobial Activity Evaluation
Madhava,Subramanyam,Thaslim Basha,Jawahar Babu,Naga Raju
, p. 16 - 21 (2016/01/25)
A class of two series of new P-substituted iminophosphoranes, N-(1,3-benzothiazol-2-ylmethyl)-N-(alkyl subtituted-λ5-phosphanylidene)amine 5(a-e) and N-(alkyl substituted-λ5-phosphanylidene)-(3,5-difluorophenyl)methanamine 9(a-e) was
O-(triazolyl)methyl carbamates as a novel and potent class of Fatty Acid Amide Hydrolase (FAAH) inhibitors
Colombano, Giampiero,Albani, Clara,Ottonello, Giuliana,Ribeiro, Alison,Scarpelli, Rita,Tarozzo, Glauco,Daglian, Jennifer,Jung, Kwang-Mook,Piomelli, Daniele,Bandiera, Tiziano
supporting information, p. 380 - 395 (2015/02/05)
Inhibition of fatty acid amide hydrolase (FAAH) activity is under investigation as a valuable strategy for the treatment of several disorders, including pain and drug addiction. A number of potent FAAH inhibitors belonging to different chemical classes have been disclosed to date; O-aryl carbamates are one of the most representative families. In the search for novel FAAH inhibitors, a series of O-(1,2,3-triazol-4-yl)methyl carbamate derivatives were designed and synthesized exploiting a coppercatalyzed [3+2] cycloaddition reaction between azides and alkynes (click chemistry). Exploration of the structure-activity relationships within this new class of compounds identified potent inhibitors of both rat and human FAAH with IC50 values in the single-digit nanomolar range. In addition, these derivatives showed improved stability in rat plasma and kinetic solubility in buffer with respect to the lead compound. Based on the results of the study, the novel analogues identified can be considered to be promising starting point for the development of new FAAH inhibitors with improved drug-like properties.
