63189-98-0Relevant academic research and scientific papers
Synthesis and Characterization of an Epidermal Growth Factor Receptor-Selective RuII Polypyridyl–Nanobody Conjugate as a Photosensitizer for Photodynamic Therapy
Karges, Johannes,Jakubaszek, Marta,Mari, Cristina,Zarschler, Kristof,Goud, Bruno,Stephan, Holger,Gasser, Gilles
, p. 531 - 542 (2019/11/13)
There is a current surge of interest in the development of novel photosensitizers (PSs) for photodynamic therapy (PDT), as those currently approved are not completely ideal. Among the tested compounds, we have previously investigated the use of RuII
DNA intercalating RuII polypyridyl complexes as effective photosensitizers in photodynamic therapy
Mari, Cristina,Pierroz, Vanessa,Rubbiani, Riccardo,Patra, Malay,Hess, Jeannine,Spingler, Bernhard,Oehninger, Luciano,Schur, Julia,Ott, Ingo,Salassa, Luca,Ferrari, Stefano,Gasser, Gilles
, p. 14421 - 14436 (2015/03/30)
Six substitutionally inert [RuII(bipy)2dppz]2+ derivatives (bipy=2,2′-bipyridine, dppz = dipyrido[3,2-a:2′,3′-c]phenazine) bearing different functional groups on the dppz ligand [NH2 (1),OMe (2),OAc (3),OH (4),C
A highly selective ratiometric fluorescent probe for 1,4-dithiothreitol (DTT) detection
Zhu, Baocun,Zhang, Xiaoling,Jia, Hongying,Li, Yamin,Liu, Haipeng,Tan, Weihong
scheme or table, p. 1650 - 1654 (2010/07/04)
A highly selective ratiometric fluorescent probe, which contains an aminonaphthalimide fluorophore and a self-immolative spacer for 1,4-dithiothreitol (DTT) detection was designed and synthesized. The probe displays a 66 nm red-shift of fluorescence emiss
The First Synthesis of Protected 5-Hydroxymethyl-2-cyanomethylbenzimidazole
Katsuyama, Isamu,Kubo, Masanori
, p. 2491 - 2497 (2008/09/18)
Protected 5-hydroxymethyl-2-cyanomethylbenzimidazole 4 has successfully been synthesized starting from 3,4-diaminobenzoic acid 1. The benzimidazole 4 is expected to be a useful intermediate for the synthesis of new functional molecules such as drugs, agro
Structure-activity relationship of omeprazole and analogues as Helicobacter pylori urease inhibitors
Kuhler,Fryklund,Bergman,Weilitz,Lee,Larsson
, p. 4906 - 4916 (2007/10/03)
Helicobacter pylori urease belongs to a family of highly conserved urea- hydrolyzing enzymes. A common feature of these enzymes is the presence of two Lewis acid nickel ions and a reactive cysteine residue in the active site. The H+/K+-ATPase inhibitor omeprazole is a prodrug of a sulfenamide which covalently modifies cysteine residues on the luminal side of the H+/K+- ATPase of gastric parietal cells. Omeprazole and eight analogues were selected based on their chemical, electronic, and kinetic properties, and each was incubated with viable H. pylori in phosphate-buffered saline at pH 7.4 for 30 min, after which 100 mM urea was added and the amount of ammonia formed analyzed after a further 10 min. Inhibition between 0% and 100% at a 0.1 mM concentration was observed for the different analogues and could be expressed as a function of the pK(a)-value of the pyridine, the pK(a)-value of the benzimidazole, the overall lipophilicity, and, most importantly, the rate of sulfenamide formation, in a quantitative structure-activity relationship. The inhibition was potentiated by a lower pH (favoring the formation of the sulfenamide) but abolished in the presence of β- mercaptoethanol (a scavenger of the sulfenamide). Structural analogues incapable of yielding the sulfenamide did not inhibit ammonia production. Treatment of Helicobacter felis-infected mice with 230 μmol/kg flurofamide b.i.d. for 4 weeks, known to potently inhibit urease activity in vivo, as a means of eradicating the infection, was tested and compared with the effect of 125 μmol/kg omeprazole b.i.d. for 4 weeks. Neither treatment proved efficacious.
Synthesis and structure-activity relationship of new cephalosporins with amino heterocycles at C-7. Dependence of the antibacterial spectrum and β-lactamase stability on the pK(a) of the C-7 heterocycle
Jung,Delvare,Boucherot,Hamon,Ackerley,Betts
, p. 1110 - 1116 (2007/10/02)
Cephalosporins with new aminobenzimidazole and aminoimidazoline heterocycles at C-7 have been synthesized starting with versatile C-7 isocyanide dihalide synthons. The aminobenzimidazoles have a broad spectrum of antibacterial activity, including Gram-positive and Gram-negative organisms, but possess limited β-lactamase stability. In contrast, the aminoimidazolines have a narrow spectrum of antibacterial activity, limited to Gram-negative strains only, but possess outstanding β-lactamase stability. Structure-activity relationships are discussed in terms of their dependence on the pK(a) of the C-7 amino heterocycle, basic C-7 residues giving cephalosporins with exceptional β-lactamase stability.
Possible Anthelmintic Agents: Syntheses of Methyl 5(6)-Substituted-benzimidazole-2-carbamates
Akhtar, M. Shamim,Seth, M.,Bhaduri, A. P.
, p. 395 - 399 (2007/10/02)
Syntheses of α-phenyl-propionitrile (2), α-phenyl-acrylonitrile (3), methyl 5(6)-hydroxymethylbenzimidazole-2-carbamate (6), β-(2-methoxycarbonylamino)-5(6)-benzi
5-[4-(Diarylmethyl)-1-piperazinylalkyl]benzimidazole derivatives
-
, (2008/06/13)
Novel 5-[4-(diarylmethyl)-1-piperazinylalkyl]benzimidazole derivatives having antiallergic and antihistaminic properties.
