77290-31-4Relevant academic research and scientific papers
Design, synthesis and biological evaluation of marine phidianidine-inspired derivatives against oxidized LDL-induced endothelial injury by activating Nrf2 anti-oxidation pathway
Xie, Hong-Xu,Wang, Yan-Hong,Zhang, Jin-He,Zhang, Juan,Zhong, Ying-Nan,Ge, Yong-Xi,Cheng, Zhi-Qiang,Jiang, Cheng-Shi,Meng, Ning
, (2022/01/20)
Inhibition of oxidized low-density lipoprotein (oxLDL)-induced vascular endothelial cell (VEC) injury is one of the effective strategies for treating atherosclerosis. In the present study, a series of novel marine phidianidine-inspired indole-1,2,4-oxadiazoles was designed, synthesized, and evaluated for their effects against oxLDL-induced injury in VECs. Among them, compound D-6, displaying the most effective protective activity, was found to inhibit oxLDL-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Mechanistic studies showed that D-6 could trigger Nrf2 nuclear translocation, subsequently resulting in increased expression of Nrf2 target gene HO-1. Meanwhile, D-6 suppressed the increase of ROS level and nuclear translocation of NF-κB induced by oxLDL. Importantly, Nrf2 knockdown attenuated the inhibition effects of D-6 on oxLDL-induced apoptosis, ROS production and NF-κB nuclear translocation. Collectively, our studies demonstrated that compound D-6 protected against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway.
Synthesis and application of indole oxadiazole derivative with aryl piperazine structure
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Paragraph 0022-0023, (2021/08/06)
The invention relates to the field of medicinal chemistry, in particular to an indole-1, 2, 4 oxadiazole derivative with an aryl piperazine structure which has a protective effect on oxLDL-induced endothelial dysfunction cells. The structural general formula of the derivative is shown in the specification. A preliminary activity test proves that the compound has a protective effect on the oxLDL-induced endothelial dysfunction cells. The compound provided by the invention is simple in structure, has a strong protection effect on oxLDL-induced endothelial dysfunction cells, and provides guidance for research and development of novel anti-atherosclerosis drugs.
Preparation and application of indole oxadiazole derivative with acylated piperazine structure
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Paragraph 0022-0023, (2021/08/07)
The invention relates to the field of medicinal chemistry, in particular to an indole-1, 2, 4 oxadiazole derivative containing an acylated piperazine structure, which has a protective effect on oxLDL-induced endothelial dysfunction cells, the structural general formula of the indole-1, 2, 4 oxadiazole derivative is shown in the specification, and a preliminary activity test proves that the compound has the protective effect on the oxLDL-induced endothelial dysfunction cells. The compound provided by the invention is simple in structure, has a strong protection effect on oxLDL-induced endothelial dysfunction cells, and provides guidance for research and development of novel anti-atherosclerosis drugs.
AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF CONDITIONS RELATED TO THE MODULATION OF IL-12, IL-23 AND/OR IFN-ALPHA
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Page/Page column 93, (2020/05/29)
Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-2
Design, synthesis, and evaluation of the anticancer properties of a novel series of carboxamides, sulfonamides, ureas, and thioureas derived from 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl substituted with pyrazolo[1,5-a]pyrimidine derivatives
Ajeesh Kumar,Nair, Kanya B.,Bodke, Yadav D.,Sambasivam, Ganesh,Bhat, Kishore G.
, p. 2221 - 2234 (2016/11/17)
Abstract: A series of novel carboxamides, sulfonamides, ureas, and thioureas derived from 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl substituted with pyrazolo[1,5-a]pyrimidine analog were designed and synthesized. The newly synthesized compounds were characterized by 1H NMR, 13C NMR, ESI–MS, and IR and were tested for their in vitro antiproliferative activity by MTT assay. Out of these twenty derivatives, five compounds showed good anticancer activity against HeLa cell line. These are superior with less than 10?μg/cm3 of IC50 when compared to the marketed anticancer drug paclitaxel with 30?μg/cm3 of IC50 against Hela cell line. Graphical abstract: [Figure not available: see fulltext.]
NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS
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Page/Page column 58, (2012/02/05)
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor. (I).
Isoindolone formation via intramolecular Diels-Alder reaction
Ball, Matthew,Boyd, Alistair,Churchill, Gwydion,Cuthbert, Murray,Drew, Mark,Fielding, Mark,Ford, Gair,Frodsham, Lianne,Golden, Michael,Leslie, Kevin,Lyons, Sarah,McKeever-Abbas, Ben,Stark, Andrew,Tomlin, Paula,Gottschling, Stephen,Hajar, Abraham,Jiang, Ji-Long,Lo, Josephine,Suchozak, Bob
experimental part, p. 741 - 747 (2012/07/31)
The intramolecular Diels-Alder reaction provides a useful synthetic methodology to build biologically active and synthetically useful isoindolone ring systems. An application of this methodology, providing an efficient manufacturing route to an mGluR2 positive allosteric modulator via a 1,5,7-substituted isoindolone, is reported herein.
DIKETO-PIPERAZINE AND PIPERIDINE DERIVATIVES AS ANTIVIRAL AGENTS
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Page/Page column 132, (2008/06/13)
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K
Setti, Eduardo L.,Venkatraman, Shankar,Palmer, James T.,Xie, Xiaoming,Cheung, Harry,Yu, Walter,Wesolowski, Gregg,Robichaud, Joel
, p. 4296 - 4299 (2008/02/03)
The synthesis and biological profile of a novel series of potent and selective inhibitors of cysteine protease cathepsin K (Cat K) are described. Pharmacokinetic evaluation of 12 indicated that some members of this series could be suitable candidates to develop new orally active therapeutic agents for the treatment of osteoporosis.
Quinazoline derivatives with anti-tumour activity
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, (2008/06/13)
The invention concerns quinazoline derivatives of Formula I wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
