1126635-79-7Relevant academic research and scientific papers
[HDBU][HSO4]-catalyzed facile synthesis of new 1,2,3-triazole-tethered 2,3-dihydroquinazolin-4[1H]-one derivatives and their DPPH radical scavenging activity
Akolkar, Satish V.,Khedkar, Vijay M.,Nagargoje, Amol A.,Pisal, Parshuram M.,Sangshetti, Jaiprakash N.,Shingate, Bapurao B.,Siddiqui, Madiha M.
, (2022/01/19)
A simple and efficient protocol has been developed for the synthesis of new1,2,3-triazole-2,3-dihydroquinazolin-4[1H]-one (DHQ) conjugates(6a?j) via ultrasound-assisted, solvent-free ionic liquid [HDBU][HSO4]-catalyzed reaction in good to excellent yields. This non-conventional, ultrasound-assisted route has taken the reactions over the conventional reflux method to provide good to excellent yields of the corresponding products (6a?j) in a very short time. In addition, mild reaction conditions, tolerance to functionalized substrates, ease of product isolation, prevention of its over oxidation and reusability of catalyst [HDBU][HSO4] are some key striking features of the methodology. The newly synthesized derivatives (6a?j) were screened for antioxidant activity using 1,1-diphenyl-2-picryl hydrazyl (DPPH) assay and are found to be a potent scavenger. The compounds 6b, 6c, 6d, 6e and 6i showed significant antioxidant activity. Molecular docking studies showed significant binding affinity in the active site of myeloperoxidase (MPO) enzyme and hence scavenged by inhibition of MPO. In silico ADMET and pharmacokinetic studies of the conjugates are very promising; a cumulative body of evidence suggests their medicinal value as a potential orally active drug candidate. Graphical abstract: [Figure not available: see fulltext.]
Design, synthesis and antibacterial evaluation of novel 15-membered 11a-azahomoclarithromycin derivatives with the 1, 2, 3-triazole side chain
Qin, Yinhui,Teng, Yuetai,Ma, Ruixin,Bi, Fangchao,Liu, Zhiyang,Zhang, Panpan,Ma, Shutao
, p. 321 - 339 (2019/07/18)
Macrolides are widely prescribed in clinic to treat various respiratory tract infections. However, due to their inappropriate use, the prevalence of macrolide-resistant strains among clinical isolates has become a concern for public health. Therefore, nov
New 1,2,3-triazole-linked tetrahydrobenzo[b]pyran derivatives: Facile synthesis, biological evaluation and molecular docking study
Khare, Smita P.,Deshmukh, Tejshri R.,Akolkar, Satish V.,Sangshetti, Jaiprakash N.,Khedkar, Vijay M.,Shingate, Bapurao B.
, p. 5159 - 5182 (2019/07/04)
Abstract: An efficient ultrasound-promoted one-pot three-component synthesis of a series of new 1,2,3-triazole-linked tetrahydrobenzo[b]pyran derivatives as antifungal and antioxidant agents using NaHCO3 has been described for the first time. T
Ultrasound assisted rapid synthesis, biological evaluation, and molecular docking study of new 1,2,3-triazolyl pyrano[2,3-c]pyrazoles as antifungal and antioxidant agent
Khare, Smita P.,Deshmukh, Tejshri R.,Sangshetti, Jaiprakash N.,Khedkar, Vijay M.,Shingate, Bapurao B.
, p. 2521 - 2537 (2019/07/15)
In search of new generation of triazole based antifungal agents, synthesis of series of new 1,2,3-triazolyl pyrano[2,3-c]pyrazoles under ultrasonic irradiation using NaHCO3 has been reported. The bioevaluation results indicate that, the compoun
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia
Xu, Qiaoling,Dai, Baozhu,Li, Zhiwei,Xu, Le,Yang, Di,Gong, Ping,Hou, Yunlei,Liu, Yajing
, (2019/08/27)
FMS-like tyrosine kinase 3 (FLT3) was an important therapeutic target in acute myeloid leukemia (AML). We synthesized two series of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives possessing the semicarbazide moiety and 2,2,2-trifluoro-N,N′-dimeth
Small Molecule Inhibition of MicroRNA miR-21 Rescues Chemosensitivity of Renal-Cell Carcinoma to Topotecan
Naro, Yuta,Ankenbruck, Nicholas,Thomas, Meryl,Tivon, Yaniv,Connelly, Colleen M.,Gardner, Laura,Deiters, Alexander
, p. 5900 - 5909 (2018/08/04)
Chemical probes of microRNA (miRNA) function are potential tools for understanding miRNA biology that also provide new approaches for discovering therapeutics for miRNA-associated diseases. MicroRNA-21 (miR-21) is an oncogenic miRNA that is overexpressed in most cancers and has been strongly associated with driving chemoresistance in cancers such as renal cell carcinoma (RCC). Using a cell-based luciferase reporter assay to screen small molecules, we identified a novel inhibitor of miR-21 function. Following structure-activity relationship studies, an optimized lead compound demonstrated cytotoxicity in several cancer cell lines. In a chemoresistant-RCC cell line, inhibition of miR-21 via small molecule treatment rescued the expression of tumor-suppressor proteins and sensitized cells to topotecan-induced apoptosis. This resulted in a >10-fold improvement in topotecan activity in cell viability and clonogenic assays. Overall, this work reports a novel small molecule inhibitor for perturbing miR-21 function and demonstrates an approach to enhancing the potency of chemotherapeutics specifically for cancers derived from oncomir addiction.
Design and synthesis of novel dehydroepiandrosterone analogues as potent antiproliferative agents
Huang, Xing,Shen, Qing-Kun,Zhang, Hong-Jian,Li, Jia-Li,Tian, Yu-Shun,Quan, Zhe-Shan
, (2018/09/12)
The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C16 position on human cancer cells. The cancer cells used in the present study were A549, Hel
Synthesis of novel 1-substituted triazole linked 1,2-benzothiazine 1,1-dioxido propenone derivatives as potent anti-inflammatory agents and inhibitors of monocyte-to-macrophage differentiation
Gannarapu, Malla Reddy,Vasamsetti, Sathish Babu,Punna, Nagender,Kotamraju, Srigiridhar,Banda, Narsaiah
, p. 1494 - 1500 (2015/08/18)
A series of novel 1-substituted-triazole linked 1,2-benzothiazine 1,1-dioxido propenone derivatives 8a-s & 12a-l were prepared from 1-substituted 1,2,3-triazol-4-aldehydes 6 & 11 with N-methyl-3-acetyl-4-hydroxybenzothiazine-1,1-dioxide 7 by condensation.
Novel 1,2,3-triazole derivatives for use against mycobacterium tuberculosis H37Rv (ATCC 27294) strain
Boechat, Nubia,Ferreira, Vitor F.,Ferreira, Sabrina B.,Ferreira, Maria De Lourdes G.,Da Silva, Fernando De C.,Bastos, Monica M.,Costa, Marilia Dos S.,Louren?o, Maria Cristina S.,Pinto, Angelo C.,Krettli, Antoniana U.,Aguiar, Anna Caroline,Teixeira, Brunno M.,Da Silva, Nathalia V.,Martins, Priscila R. C.,Bezerra, Flavio Augusto F. M.,Camilo, Ane Louise S.,Da Silva, Gerson P.,Costa, Carolina C. P.
, p. 5988 - 5999 (2011/10/09)
The purpose of this study was to prepare various 4-substituted N-phenyl-1,2,3-triazole derivatives using click chemistry. The derivatives were screened in vitro for antimicrobial activity against Mycobacterium tuberculosis strain H37Rv (ATCC 27294) using
