149860-22-0Relevant articles and documents
Metal beta-lactamase inhibitor as well as preparation method and application thereof
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, (2020/10/14)
The invention discloses a metal beta-lactamase inhibitor as well as a preparation method and application thereof. The preparation method comprises the following steps: dissolving a pyridylamine compound in a solvent 1, adding an ester compound and carbonate, stirring at 80-100 DEG C for 11-13 hours, cooling the reaction product to room temperature, extracting, carrying out vacuum drying, and purifying to obtain a product 1; dissolving the product 1 in a solvent 2, adding ester-based hydrolysate, stirring for 1.5-2.5 hours at room temperature, and extracting, vacuum-drying and purifying a reaction product to obtain a Zn chelating agent; dissolving a beta-lactamase compound in a solvent 3, adding a Zn chelating agent and an alkali, stirring for 11-13 hours at room temperature, and extracting, vacuum-drying and purifying a reaction product to obtain the metal beta-lactamase inhibitor which can be used as a combined agent of antibiotics for inhibiting bacterial proliferation. The inhibitor is simpler to prepare and low in material cost, reduces the biotoxicity of molecules, and has higher antibacterial efficiency.
THERAPEUTIC HYDROGELS AND CONTACT LENS FOR CORNEAL MELTING
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Page/Page column 2/11, (2020/01/24)
The present invention relates to the unexpected discovery of a cross-linked polymer of 2-hydroxyethyl methacrylate and dipicolylamine-containing monomers that can be used as therapeutic lens to treat ocular diseases or disorders associated with MMP over-activity and/or over-expression, such as but not limited to corneal melting (or keratolysis).
Mitochondria-Targeting Iron(III) Catecholates for Photoactivated Anticancer Activity under Red Light
Basu, Uttara,Pant, Ila,Kondaiah, Paturu,Chakravarty, Akhil R.
, p. 1002 - 1012 (2016/03/15)
Iron(III) catecholates [Fe(R′-bpa)(R-dopa)Cl] (1, 2) with a triphenylphosphonium (TPP) moiety, where R′-bpa is 2-(TPP-N,N-bis((pyridin-2-yl)methyl)ethanamine) chloride (TPPbpa) and R-dopa is 4-{2-[(anthracen-9-yl)methylamino]ethyl}benzene-1,2-diol (andopa, 1) or 4-{2-[(pyren-1-yl)-methylamino]ethyl}benzene-1,2-diol (pydopa, 2), were synthesized and their photocytotoxicity studied. Complexes 3 and 4 with [phenyl-N,N-bis(pyridin-2-yl)methyl]methanamine (phbpa) were used as controls. The catecholate complexes showed an absorption band near 720 nm. The 5e- paramagnetic complexes showed a FeIII/FeII irreversible response near -0.45 V and a quasi-reversible catechol/semiquinone couple near 0.5 V versus saturated calomel electrode (SCE) in DMF/0.1 M tetrabutylammonium perchlorate. They showed photocytotoxicity in red/visible light in HeLa, HaCaT, MCF-7, and A549 cells. Complexes 1 and 2 displayed mitochondrial localization, reactive oxygen species (ROS) generation under red light, and apoptotic cell death. Control complexes 3 and 4 exhibited uniform distribution throughout the cell. The complexes showed DNA photocleavage under red light (785 nm), forming hydroxyl radicals as the ROS. Iron(III) catecholates bearing anthracenyl or pyrenyl groups and a dipicolylamine base with a cationic triphenylphosphonium (TPP) moiety show remarkable photocytotoxicity under red light, mitochondrial localization, reactive oxygen species (ROS) generation, and apoptotic cell death. They showed significant DNA photocleavage activity under red light (785 nm), forming hydroxyl radicals as the ROS.
Catalytic catechol oxidation by copper complexes: Development of a structure-activity relationship
Ording-Wenker, Erica C. M.,Siegler, Maxime A.,Lutz, Martin,Bouwman, Elisabeth
, p. 12196 - 12209 (2016/01/15)
A large library of CuII complexes with mononucleating and dinucleating ligands was synthesized to investigate their potential as catalysts for the catalytic oxidation of 3,5-di-tert-butylcatechol (3,5-DTBC). X-ray structure determination for a number of these complexes revealed relatively large Cu?Cu distances and the formation of polymeric species. Comparison of the 3,5-DTBC oxidation rates showed that ligands that stabilize the biomimetic dinuclear CuII μ-thiolate complex also result in copper compounds that are much more active in the oxidation of 3,5-DTBC. This oxidation activity is however inhibited by the presence of chloride ions. The highest kcat that was observed was 6900 h-1, which is one of the highest turnover frequencies reported so far for catechol oxidation in CH3CN.
Poly(ethylene carbonate) Nanoparticles as Carrier System for Chemotherapy Showing Prolonged in vivo Circulation and Anti-Tumor Efficacy
Renette, Thomas,Librizzi, Damiano,Endres, Thomas,Merkel, Olivia,Beck-Broichsitter, Moritz,Bege, Nadja,Petersen, Holger,Curdy, Catherine,Kissel, Thomas
experimental part, p. 970 - 978 (2012/09/08)
The aim of this study is to investigate the feasibility and efficacy of PEC nanoparticles as delivery system for cancer chemotherapy. Assembly of paclitaxel-loaded nanoparticles with high loading efficiency and narrow-size distribution is successful. For non-invasive in vivo tracing, nanoparticle blends of chelator bearing poly(lactide) with PEC and PLGA are successfully prepared. Pharmacokinetic studies in mice reveal a twofold higher circulation time of PEC as compared to PLGA. A tumor model shows an accumulation of PEC NPs in cancerous tissue and a higher anti-tumor efficiency compared to the standard Taxol, which is reflected in a significantly slower tumor growth compared to the NaCl control group.
Biomimetic iron(iii) complexes of N3O and N3O 2 donor ligands: Protonation of coordinated ethanolate donor enhances dioxygenase activity
Sundaravel, Karuppasamy,Sankaralingam, Muniyandi,Suresh, Eringathodi,Palaniandavar, Mallayan
experimental part, p. 8444 - 8458 (2011/10/10)
A series of iron(iii) complexes 1-4 of the tripodal tetradentate ligands N,N-bis(pyrid-2-ylmethyl)-N-(2-hydroxyethyl)amine H(L1), N,N-bis(pyrid-2- ylmethyl)-N-(2-hydroxy- propyl)amine H(L2), N,N-bis(pyrid-2-ylmethyl)-N- ethoxyethanolamine H(L3), and N-((pyrid-2-ylmethyl)(1-methylimidazol-2-ylmethyl) )-N-(2-hydroxyethyl)amine H(L4), have been isolated, characterized and studied as functional models for intradiol-cleaving catechol dioxygenases. In the X-ray crystal structure of [Fe(L1)Cl2] 1, the tertiary amine nitrogen and two pyridine nitrogen atoms of H(L1) are coordinated meridionally to iron(iii) and the deprotonated ethanolate oxygen is coordinated axially. In contrast, [Fe(HL3)Cl3] 3 contains the tertiary amine nitrogen and two pyridine nitrogen atoms coordinated facially to iron(iii) with the ligand ethoxyethanol moiety remaining uncoordinated. The X-ray structure of the bis(μ-alkoxo) dimer [{Fe(L5)Cl}2](ClO4)25, where HL is the tetradentate N3O donor ligand N,N-bis(1-methylimidazol-2-ylmethyl)-N- (2-hydroxyethyl)amine H(L5), contains the ethanolate oxygen donors coordinated to iron(iii). Interestingly, the [Fe(HL)(DBC)]+ and [Fe(HL3)(HDBC)X] adducts, generated by adding ～1 equivalent of piperidine to solutions containing equimolar quantities of iron(iii) complexes 1-5 and H2DBC (3,5-di-tert-butylcatechol), display two DBC2- → iron(iii) LMCT bands (λmax: 1, 577, 905; 2, 575,915; 3, 586, 920; 4, 563, 870; 5, 557, 856 nm; Δλmax, 299-340 nm); however, the bands are blue-shifted (λmax: 1, 443, 700; 2, 425, 702; 3, 424, 684; 4, 431, 687; 5, 434, 685 nm; Δλmax, 251-277 nm) on adding 1 more equivalent of piperidine to form the adducts [Fe(L)(DBC)] and [Fe(HL3)(HDBC)X]. Electronic spectral and pH-metric titration studies in methanol disclose that the ligand in [Fe(HL)(DBC)]+ is protonated. The [Fe(L)(DBC)] adducts of iron(iii) complexes of bis(pyridyl)-based ligands (1,2) afford higher amounts of intradiol-cleavage products, whereas those of mono/bis(imidazole)-based ligands (4,5) yield mainly the auto-oxidation product benzoquinone. It is remarkable that the adducts [Fe(HL)(DBC)] +/[Fe(HL3)(DBC)X] exhibit higher rates of oxygenation affording larger amounts of intradiol-cleavage products and lower amounts of benzoquinone. The Royal Society of Chemistry 2011.
COMPOUND HAVING ACTIVITY TO SUPPRESS DEGRANULATION AND CYTOKINE PRODUCTION AND USE THEREOF
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Page/Page column 65-66, (2009/08/14)
The present invention provides a compound represented by the formula (I): wherein L is an alkylene group;X is a bond, -O-, -S- or -CO-;Y is a bond, -NR3- or -CO-;Z is an organic group or OH;R1 and R2 are the same or different and each is an optionally substituted alkyl group, a halogen atom or a hydrogen atom; and R3 is an optionally substituted alkyl group or a hydrogen atom, or a salt thereof.
