41964-65-2Relevant academic research and scientific papers
Novel monoacylglycerol lipase inhibitor as well as preparation method and application thereof
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Paragraph 0264-0266, (2021/02/10)
The invention discloses a novel monoacylglycerol lipase inhibitor as well as a preparation method and application thereof. Specifically, the invention provides a compound shown as a formula I, or a pharmaceutically acceptable salt, a stereoisomer, or a deuterated derivative thereof. Experimental results show that the compound provided by the invention can effectively inhibit MAGL activity, can beused for preparing an MAGL inhibitor and preparing medicines for preventing and/or treating diseases (including endometrial cancer, colorectal cancer, liver cancer, breast cancer, ovarian cancer, neurodegenerative diseases and the like) related to abnormal MAGL activity, and has a wide application prospect.
Synthesis and Antifungal Activity of New N-Aryl-2-(2-hydroxyphenylamino)ethylenediamine Derivatives
Gao, Han,Wan, Yichao,Tan, Yuhuan,Luo, Xi,Li, Lin
, p. 122 - 127 (2021/02/21)
Abstract: In this study, a series of new N-aryl-2-(2-hydroxyphenylamino)ethylenediamine derivatives has beendesigned, synthesized and evaluated for antifungal activity against six selectedspecies of phytopathogenic fungi. Among the products, the most potent compoundhave demonstrated 97.7% inhibitory activity against S.sclerotiorum at the concentration of 50 μg/mL, which is higherthan that of the positive control chlorothalonil.
Synthesis and Cytotoxic Evaluation of Some New 1,2,3-Triazole Linked 2-Imino-4-(Trifuoromethyl)-Thiazolidin-4-ol Derivatives
Appalanaidu, K.,Dadmal, Tulshiram L.,Kumbhare, Ravindra M.,Pamanji, R.,Rao, J. Venkateswara,Reddy, Prathyusha J.,Velatooru, L. R.
, p. 81 - 89 (2021/08/12)
A new series of 1,2,3-triazole tagged 2-imino-4-(trifluoromethyl)thiazolidinol derivatives was synthesized through click chemistry under Sharpless conditions and evaluated for anticancer activity against human monocytic leukemia (U937), human breast adeno
Design, synthesis of novel (Z)-2-(3-(4-((3-benzyl-2,4-dioxothiazolidin-5-ylidene)methyl)-1-phenyl-1H-pyrazol-3-yl)phenoxy)-N-arylacetamide derivatives: Evaluation of cytotoxic activity and molecular docking studies
Kolluri, Prashanth Kumar,Gurrapu, Nirmala,Subhashini,Putta, Shravani,Singh, Surya Sathyanarayana,Vani, Tamalapakula,Manga, Vijjulatha
, (2019/11/26)
In an attempt to discover potential cytotoxic agents, a series of novel (Z)-2-(3-(4-((3-benzyl-2,4-dioxothiazolidin-5-ylidene)methyl)-1-phenyl-1H-pyrazol-3-yl) phenoxy)-N-arylacetamide derivatives 11a-n were synthesized in varied steps with acceptable reaction procedures with good yields and characterized by 1H NMR, 13C NMR, IR and ESI-MS spectra. All the novel synthesized derivatives were assessed for their cytotoxic activity against human breast cell line (MCF-7) with different concentration of 0.625 μM, 1.25 μM, 2.5 μM, 5 μM and 10 μM respectively. Biological evaluation assay results were displayed in terms of percentage of cell viability reduction and IC50 values. Most of the screened derivatives demonstrated moderate to promising cytotoxic activity. Some of the derivatives, particularly compound 11d and 11n have shown promising cytotoxic activity with IC50 values 0.604 μM and 0.665 μM compared to standard drug cisplatin and compounds 11a, 11e and 11g also have shown considerable cytotoxic activity and the rest of the derivatives have shown moderate activity. Furthermore, molecular docking calculations and ADME properties of the synthesized molecules are in effective compliance with the cytotoxic evaluation results.
Synthesis, anticancer, and computational studies of 1, 3, 4-oxadiazole-purine derivatives
Faisal, Shahla,Kamal, Shagufta,Parveen, Bushra,Rasool, Nasir,Rasul, Azhar,Raza, Zohaib,Shahzadi, Irum,Zahid, Faisal M.,Zahoor, Ameer F.,Zia-ur-Rehman, Muhammad
, p. 2782 - 2794 (2020/04/16)
Theophylline-7-acetic acid (acefylline) (3) and its derivatives are pharmacologically active compounds and generally recognized as bronchodilators for the treatment of respiratory diseases like acute asthma for over 70 years. In this article, synthesis of
N-heterocycles scaffolds as quorum sensing inhibitors. Design, synthesis, biological and docking studies
Fuentes-Gutiérrez, Alfredo,Curiel-Quesada, Everardo,Correa-Basurto, José,Martínez-Mu?oz, Alberto,Reyes-Arellano, Alicia
, p. 1 - 26 (2020/12/22)
Quorum sensing is a communication system among bacteria to sense the proper time to express their virulence factors. Quorum sensing inhibition is a therapeutic strategy to block bacterial mechanisms of virulence. The aim of this study was to synthesize and evaluate new bioisosteres of N-acyl homoserine lactones as Quorum sensing inhibitors in Chromobacterium violaceum CV026 by quantifying the specific production of violacein. Five series of compounds with different heterocyclic scaffolds were synthesized in good yields: thiazoles, 16a–c, thiazolines 17a–c, benzimidazoles 18a–c, pyridines 19a–c and imidazolines 32a–c. All 15 compounds showed activity as Quorum sensing inhibitors except 16a. Compounds 16b, 17a–c, 18a, 18c, 19c and 32b exhibited activity at concentrations of 10 μM and 100 μM, highlighting the activity of benzimidazole 18a (IC50 = 36.67 μM) and 32b (IC50 = 85.03 μM). Pyridine 19c displayed the best quorum sensing inhibition activity (IC50 = 9.66 μM). Molecular docking simulations were conducted for all test compounds on the Chromobacterium violaceum CviR protein to gain insight into the process of quorum sensing inhibition. The in-silico data reveal that all 15 the compounds have higher affinity for the protein than the native AHL ligand (1). A strong correlation was found between the theoretical and experimental results.
1,3,4,9-TETRAHYDRO-2H-PYRIDO[3,4-B]INDOLE DERIVATIVE COMPOUNDS AND USES THEREOF
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Paragraph 0134-0315; 0137, (2020/03/05)
The present invention relates to 1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indole derivative compounds and uses thereof. In particular, compounds of the invention have antibacterial activity and/or are capable of re-sensitizing methicillin-resistant Staphylococcus aureus to a P-lactam antibiotic or a combination of a P-lactam antibiotic and a P-lactamase inhibitor. The present invention also relates to a method for producing and using said compounds.
Substituted Pyridazin-3(2 H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists
Deora, Girdhar Singh,Qin, Cheng Xue,Vecchio, Elizabeth A.,Debono, Aaron J.,Priebbenow, Daniel L.,Brady, Ryan M.,Beveridge, Julia,Teguh, Silvia C.,Deo, Minh,May, Lauren T.,Krippner, Guy,Ritchie, Rebecca H.,Baell, Jonathan B.
supporting information, p. 5242 - 5248 (2019/05/28)
Herein we describe the development of a focused series of functionalized pyridazin-3(2H)-one-based formyl peptide receptor (FPR) agonists that demonstrate high potency and biased agonism. The compounds described demonstrated biased activation of prosurvival signaling, ERK1/2 phosphorylation, through diminution of the detrimental FPR1/2-mediated intracellular calcium (Cai2+) mobilization. Compound 50 showed an EC50 of 0.083 μM for phosphorylation of ERK1/2 and an approximate 20-fold bias away from Cai2+ mobilization at the hFPR1.
Design, Synthesis, Antimicrobial Evaluation, and Laccase Catalysis Effect of Novel Benzofuran–Oxadiazole and Benzofuran–Triazole Hybrids
Faiz, Sadia,Zahoor, Ameer Fawad,Ajmal, Muhammad,Kamal, Shagufta,Ahmad, Sajjad,Abdelgawad, Abdelrahman M.,Elnaggar, Mehrez E.
, p. 2839 - 2852 (2019/11/03)
Novel structural hybrids of benzofuran–oxadiazole and benzofuran–triazole have been synthesized and evaluated for their potential against Staphylococcus aureus, Bacillus subtilis, and Escherichia coli. The excellent antibiotic activity was shown by compou
3-Aminomethyl pyridine chalcone derivatives: Design, synthesis, DNA binding and cytotoxic studies
Durgapal, Sunil Dutt,Soni, Rina,Umar, Shweta,Suresh, Balakrishnan,Soman, Shubhangi S.
, p. 1279 - 1287 (2018/06/29)
Herein we report design, synthesis, and anticancer activity of compounds 6a–h and 11a–j. Compounds 6a–f were designed based on 3-aminomethyl pyridine attached to different acetamide derivatives and in compounds 6g–h it was attached to coumarin moiety. Coumarin containing compounds 6g–h showed very poor anticancer activity against both A549 (Lungs cancer cell line), and MCF-7 (Breast cancer cell line) cell lines in MTT assay. Compounds 11a–j were designed as derivatives of 3-aminomethyl pyridine and 4-amino chalcones. A series of chalcone derivatives of 3-aminomethyl pyridine 11a–j have been synthesized and screened for their in vitro anticancer activity and DNA binding affinity. Most of the compounds showed very good antimitotic activity against A549 cell line as compared to fluorouracil. Compounds 11g and 11i were selected for DNA-binding studies as they showed excellent activity against cancer cell lines in MTT assay. CT-DNA binding affinity of compounds 11g and 11i have been investigated by UV based DNA titration and fluorescence emission study against DNA-EtBr complex. Interestingly, compound 11i has displayed excellent antiproliferative activity, with IC50 0.0067?±?0.0002?μm, against MCF-7 cell line. Compound 11i has been studied for its cytotoxicity using MTT, LDH, as well as EtBr/AO assay and was found to induce apoptosis in the cancerous cell line.
