5378-29-0Relevant academic research and scientific papers
Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents
Bi, Fangchao,Ji, Shengli,Venter, Henrietta,Liu, Jingru,Semple, Susan J.,Ma, Shutao
supporting information, p. 884 - 891 (2018/02/15)
3-Methoxybenzamide (3-MBA) derivatives have been identified as novel class of potent antibacterial agents targeting the bacterial cell division protein FtsZ. As one of isosteres for the amide group, 1,2,3-triazole can mimic the topological and electronic features of the amide, which has gained increasing attention in drug discovery. Based on these considerations, we prepared a series of 1H-1,2,3-triazole-containing 3-MBA analogues via isosteric replacement of the terminal amide with triazole, which had increased antibacterial activity. This study demonstrated the possibility of developing the 1H-1,2,3-triazole group as a terminal amide-mimetic element which was capable of both keeping and modulating amide-related bioactivity. Surprisingly, a different action mode of these new 1H-1,2,3-triazole-containing analogues was observed, which could open new opportunities for the development of antibacterial agents.
Four-gear ring metal platinum (II) complex phosphorescent luminescent materials
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Paragraph 0048; 0050, (2017/11/16)
The invention discloses four-gear ring metal platinum (II) phosphorescent luminescent materials as shown in a formula (I) in the specification, wherein a five-membered heterocyclic aromatic group Ar is as shown in the specification; Ar is selected from one of the following: 2H-1,2,3-triazole, X1=N, X2=N, X3=CH); 1H-1,2,3-triazole, X1=CH, X2=N, X3=N; 1,3,4-oxadiazole, X1=O, X2=C, X3=N; oxazole, X1=O, X2=C, X3=CH; or thiazole, X1=S, X2=C, X3=CH. One or more of the four-gear ring metal platinum (II) phosphorescent luminescent materials disclosed by the invention are applied to a luminescent layer of an organic illuminator. The four-gear ring metal platinum (II) phosphorescent luminescent materials disclosed by the invention have strong molecular rigidity, can effectively reduce energy consumed owing to molecular vibration, and have high phosphorescent quantum efficiency, good chemical stability and good heat stability.
SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 60, (2009/12/02)
Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
Compounds enhancing antitumor activity of other cytotoxic agents
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, (2008/06/13)
This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and multidrug resistant forms of malaria, tuberculosis, leishmania and amoebic dysentery to chemotherapeutants. The compounds and their pharmaceutically acceptable salts are also inhibitors of the active drug transport capability of P-glycoprotein which is encoded by the human MDR1 gene, as well as of certain other related ATP-binding-cassette transporters from eukaryotic and prokaryotic organisms (e.g., pfmdr from Plasmodium falciprum, and murine mdr1 and mdr3 gene products).
