216443-97-9Relevant articles and documents
Selectivity in the Intermolecular Diels–Alder Reaction of Conjugated Trienes: Experimental and Theoretical Approaches
Remeur, Camille,Desrat, Sandy,Gandon, Vincent,Roussi, Fanny
, p. 5869 - 5877 (2018)
Eleven analogs of the natural product meiogynin A, an inhibitor of proteins of the Bcl-2 family, have been elaborated by an intermolecular Diels–Alder (DA) reaction of various conjugated chloro-trienes, in order to determine the influence of the modification of the south part of meiogynin A on its biological activity. The chloro-trienes were obtained in two to five steps from commercial compounds through a selective hydrochlorination of bromoalkyne intermediates to (Z)-1,2-dihalogenated alkenes followed by a chemoselective Suzuki–Miyaura cross-coupling. The intermolecular DA reaction of these trienes with two α,β-unsaturated carboxylic acids as dienophiles occurred with a perfect regioselectivity and good to excellent diastereoselectivities. These selectivities could be rationalized by DFT calculations.
INDOLE DERIVATIVES AS ALPHA-1 -ANTITRYPSIN MODULATORS FOR TREATING ALPHA-1 -ANTITRYPSIN DEFICIENCY (AATD)
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Paragraph 00227; 00234; 00316; 00740, (2021/10/11)
Indole derivatives as alpha-l-antitrypsin modulators for treating alpha-l-antitrypsin deficiency (AATD).
As neuroprotective agents of pharmaceutical compounds
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Paragraph 0158; 0159; 0162; 0163, (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.
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 (2019/01/15)
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
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.