- Synthesis, antitumor activity, enzyme assay, DNA binding and molecular docking of Bis-Schiff bases of pyrazoles
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A novel series of Bis-Schiff bases of pyrazoles 9–24 were synthesized by the direct condensation of 5-aminopyrazoles 4a–d with dialdehydes 8a–d in ethanol. The newly synthesized Bis-Schiff bases of pyrazoles 9–24 were characterized and confirmed by analyt
- Morsy, Nesrin M.,Hassan, Ashraf S.,Hafez, Taghrid S.,Mahran, Mohamed R. H.,Sadawe, Inass A.,Gbaj, Abdul M.
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- BIVALENT LECA INHIBITORS TARGETING BIOFILM FORMATION OF PSEUDOMONAS AERUGINOSA
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The present invention relates to divalent compounds binding to LecA. The compounds are useful to block biofilm formation of Pseudomonas aeruginosa. The invention further relates to pharmaceutical compositions comprising these compounds and to therapeutic methods and uses of these compounds, in particular to therapeutic methods and uses for the treatment of Pseudomonas aeruginosa infections in a subject. The invention also relates to imaging of infections, such as biofilms produced by Pseudomonas aeruginosa, by using these divalent compounds.
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Page/Page column 31-32; 42
(2021/05/15)
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- A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d-galactose pentaacetate
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Chronic infections with Pseudomonas aeruginosa are associated with the formation of bacterial biofilms. The tetrameric P. aeruginosa lectin LecA is a virulence factor and an anti-biofilm drug target. Increasing the overall binding affinity by multivalent
- Hirsch, Anna K. H.,Imberty, Anne,Kinsinger, Thorsten,Kuhaudomlarp, Sakonwan,Lepsik, Martin,Minervini, Saverio,Titz, Alexander,Yousaf, Sultaan,Zahorska, Eva
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p. 8822 - 8825
(2020/08/17)
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- Experimental and theoretical insights into the corrosion inhibition activity of novel Schiff bases for aluminum alloy in acidic medium
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Three novel Schiff bases, namely N-(4-((4-((phenylimino)methyl)phenoxy)methoxy)benzylidene)benzenamine (UA), N-(3-methoxy-4-((2-methoxy-4-((phenylimino)methyl)phenoxy)methoxy)benzylidene)benzenamine (UB), and N-(3-ethyl-4-((2-ethyl-4-((phenylimino)methyl)
- Nazir, Uzma,Akhter, Zareen,Ali, Naveed Zafar,Shah, Faiz Ullah
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p. 36455 - 36470
(2019/11/20)
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- Y-shaped bis-arylethenesulfonic acid esters: Potential potent and membrane permeable protein tyrosine phosphatase 1B inhibitors
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Known PTP1B inhibitors with bis-anionic moieties exhibit potent inhibitory activity, good selectivity, however, they are incapable of penetrating cellular membranes. Based upon our finding of a new pharmacophoric group in inhibition of PTP1B and the struc
- Yang, Fengzhi,Xie, Fangzhou,Zhang, Ying,Xia, Yu,Liu, Wenlu,Jiang, Faqin,Lam, Celine,Qiao, Yixue,Xie, Dongsheng,Li, Jianqi,Fu, Lei
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supporting information
p. 2166 - 2170
(2017/04/27)
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- Novel PTP1B enzyme inhibitor, preparation method and applications thereof
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The present invention provides a novel PTP1B enzyme inhibitor, a preparation method and applications thereof, and particularly discloses a class of bis 2-substituted ethylene sulfonate compounds and a preparation method thereof, and uses of the bis 2-substituted ethylene sulfonate compounds as the PTP1B enzyme activity inhibitor. According to the present invention, the prepared novel compound has good PTP1B enzyme activity inhibition effect, and has the application value in preparation of drugs for treatment and prevention of diabetes and obesity.
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Paragraph 0108-0109
(2017/08/31)
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- Synthesis and mesomorphic properties of new methylene-linked linear symmetrical liquid crystal dimers
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A series of methylene-linked symmetrical liquid crystal dimers were synthesized. Their structures were confirmed by physicochemical techniques. Differential scanning calorimetry and polarizing optical microscopy verified the liquid crystal behaviors and t
- Al-Hamdani, Uhood J.,Al-Ibrahim, Aiman G.,Abbo, Hanna S.,Titinchi, Salam J.J.
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- Biological evaluation of bisbenzaldehydes against four Mycobacterium species
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A series of bisbenzaldehydes and structurally related analogs, conveniently synthesized via microwave-assisted reactions, were evaluated in vitro against drug susceptible and multi-drug resistant Mycobacterium tuberculosis, against virulent Mycobacterium bovis, against Mycobacterium ulcerans and against two Mycobacterium avium subspecies. Among the 33 substances that were tested, compound 12, i.e. 4,4′-[1,12-dodecanediyl(oxy)]bisbenzaldehyde, emerged as the most promising hit. Its activity was further confirmed in an intracellular growth inhibition assay of M. tb in murine J774 A.1 macrophages. None of the compounds showed significant cytotoxicity on human C3A hepatocytes in a neutral red dye uptake assay and no genotoxicity or mutagenicity was observed as demonstrated by a VITOTOX test and confirmed with a comet assay.
- Cappoen, Davie,Forge, Delphine,Vercammen, Frank,Mathys, Vanessa,Kiass, Mehdi,Roupie, Virginie,Anthonissen, Roel,Verschaeve, Luc,Vanden Eynde, Jean Jacques,Huygen, Kris
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p. 731 - 738
(2013/07/25)
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- Bis(oxyphenylene)benzimidazoles: A novel class of anti-Plasmodium falciparum agents
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A small library of 26 2,2′-[alkane-α,ω- diylbis(oxyphenylene)]bis-1H-benzimidazoles has been prepared and evaluated against Giardia intestinalis, Entamoeba histolytica, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium
- Mayence, Annie,Vanden Eynde, Jean Jacques,Kaiser, Marcel,Brun, Reto,Yarlett, Nigel,Huang, Tien L.
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experimental part
p. 7493 - 7500
(2012/01/03)
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- Synthesis of Diaryloxymethanes using Poly(ethylene glycol) as a Phase-transfer Catalyst
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Diaryloxymethanes have been synthesized in high yields under conditions of solid-liquid phase-transfer catalysis using poly(ethylene glycol)-600 (PEG-600) as the catalyst.
- Salunkhe, Manikrao M.,Kavitake, Bhanudas P.,Patil, Sucheta V.,Wadgaonkar, Prakash P.
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- A New Synthesis of 1,4-Diaryl-1,3-butadienes Utilizing the Anil Synthesis
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The anil synthesis was employed in the preparation of 1,4-diarylsubstituted 1,3-butadienes 7 from 1-arylpropenes 5 and N-arylideneanilines (aromatic Schiff bases) 6 in dimethylformamide solution and a strong base as catalyst obtained in situ by reacting metallic sodium with this solvent.
- Paventi, M.,Hay, A. S.
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p. 878 - 881
(2007/10/02)
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- POLYMER SUPPORTED REAGENTS: AN EFFICIENT METHOD FOR THE SYNTHESIS OF DIARYLOXYMETHANES
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Diaryloxymethanes were synthesized in high yield and in high purity by the treatment of polymer supported phenoxide ions with dichloromethane.
- Salunkhe, M. M.,Salunkhe, D. G.,Kanade, A. S.,Mane, R. B.,Wadgaonkar, P. P.
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p. 1143 - 1147
(2007/10/02)
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