170100-60-4Relevant articles and documents
Functionalization of luminescent lanthanide-gallium metallacrowns using copper-catalyzed alkyne-azide cycloaddition and thiol-maleimide Michael addition
Lutter, Jacob C.,Lopez Bermudez, Beatriz A.,Nguyen, Tu N.,Kampf, Jeff W.,Pecoraro, Vincent L.
, p. 119 - 125 (2019)
The synthesis and characterization of {Ln[12-MCGa III N(eshi)-4]}2(iph)4 and {Ln[12-MCGa III N(shi)-4]}2(miph)4 metallacrowns (MCs), where shisu
INHIBITORS OF PROTEIN ARGININE DEIMINASE 1 AND METHODS OF PREPARATION AND USE THEREOF
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Paragraph 00176, (2021/01/23)
The invention provides novel inhibitors or inactivators of protein arginine deiminase 1, pharmaceutical compositions and methods of use thereof. The invention also relates to molecular probes based on such compounds and methods of use thereof.
Halogen Bonding Increases the Potency and Isozyme Selectivity of Protein Arginine Deiminase 1 Inhibitors
Mondal, Santanu,Gong, Xuefeng,Zhang, Xiaoqian,Salinger, Ari J.,Zheng, Li,Sen, Sudeshna,Weerapana, Eranthie,Zhang, Xuesen,Thompson, Paul R.
supporting information, p. 12476 - 12480 (2019/08/07)
Protein arginine deiminases (PADs) hydrolyze the side chain of arginine to form citrulline. Aberrant PAD activity is associated with rheumatoid arthritis, multiple sclerosis, lupus, and certain cancers. These pathologies established the PADs as therapeutic targets and multiple PAD inhibitors are known. Herein, we describe the first highly potent PAD1-selective inhibitors (1 and 19). Detailed structure–activity relationships indicate that their potency and selectivity is due to the formation of a halogen bond with PAD1. Importantly, these inhibitors inhibit histone H3 citrullination in HEK293TPAD1 cells and mouse zygotes with excellent potency. Based on this scaffold, we also developed a PAD1-selective activity-based probe that shows remarkable cellular efficacy and proteome selectivity. Based on their potency and selectivity we expect that 1 and 19 will be widely used chemical tools to understand PAD1 biology.
As neuroprotective agents of pharmaceutical compounds
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Paragraph 0158; 0159; 0160; 0161, (2019/06/26)
The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents
Ding, Shi,Dai, Rui-Yang,Wang, Wen-Ke,Cao, Qiao,Lan, Le-Fu,Zhou, Xian-Li,Yang, Yu-She
, p. 94 - 102 (2017/12/15)
LpxC inhibitors are new-type antibacterial agents developed in the last twenty years, mainly against Gram-negative bacteria infections. To develop novel LpxC inhibitors with good antibacterial activities and biological metabolism, we summarized the basic skeleton of reported LpxC inhibitors, designed and synthesized several series of compounds and tested their antibacterial activities against Escherichial coli and Pseudomonas aeruginosa in vitro. Structure-activity relationships have been discussed in this article. The metabolism stability of YDL-2, YDL-5, YDL-8, YDL-14, YDL-20–YDL-23 have been evaluated in liver microsomes, which indicated that the 2-amino isopropyl group may be a preferred structure than the 2-hydroxy ethyl group in the design of LpxC inhibitors.
Bi-aromatic compounds linked via a heteroethylene radical, and pharmaceutical and cosmetic compositions using them
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, (2008/06/13)
Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.
Bi-aromatic compounds linked via a heteroethylene radical, and pharmaceutical and cosmetic compositions using them
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, (2008/06/13)
Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.
Bi-aromatic compounds bound by a heteroethynylene radical and pharmaceutical and cosmetic compositions containing same
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, (2008/06/13)
Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.
Triaromatic compounds and pharmaceutical/cosmetic compositions comprised thereof
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, (2008/06/13)
Novel pharmaceutically/cosmetically-active triaromatic compounds have the structural formula (I): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
Polyaromatic propynyl compounds and pharmaceutical/cosmetic compositions comprised thereof
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, (2008/06/13)
Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): STR1 in which X is one of the radicals: STR2 and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.