116271-34-2Relevant articles and documents
Benzothiazole derivative, synthesis method thereof and application of benzothiazole derivative as antibacterial drug
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Paragraph 0012-0014, (2020/02/14)
The invention relates to a benzothiazole derivative as well as a synthesis method and application thereof as an antibacterial agent. The benzothiazole derivative has a structure shown as a formula I,wherein R is selected from H, C1-C3 alkyl, C1-C3 alkoxy
Caged mono- and divalent ligands for light-assisted disruption of PDZ domain-mediated interactions
Sainlos, Matthieu,Iskenderian-Epps, Wendy S.,Olivier, Nelson B.,Choquet, Daniel,Imperiali, Barbara
supporting information, p. 4580 - 4583 (2013/05/23)
We report a general method for light-assisted control of interactions of PDZ domain binding motifs with their cognate domains by the incorporation of a photolabile caging group onto the essential C-terminal carboxylate binding determinant of the motif. The strategy was implemented and validated for both simple monovalent and biomimetic divalent ligands, which have recently been established as powerful tools for acute perturbation of native PDZ domain-dependent interactions in live cells.
Photolabile 1-(2-Nitrophenyl)ethyl Phosphate Esters of Adenine Nucleotide Analogues. Synthesis and Mechanism of Photolysis
Walker, Jeffery W.,Reid, Gordon P.,McCray, James A.,Trentham, David R.
, p. 7170 - 7177 (2007/10/02)
A general method is described for preparing photolabile 1-(2-nitrophenyl)ethyl esters of phosphate and thiophosphate compounds.The method is based on selective alkylation of weakly ionizing phosphate groups by a new alkylating agent, 1-(2-nitrophenyl)diazoethane.ATP and the widely used structural analogues of ATP, 5'-adenylyl imidodiphosphate (ATP(β,γNH)) and adenosine 5'-(3-thiophsophate) (ATP(γS)), were alkylated on the terminal (γ) phosphate group.ATP(γS) was alkylated on oxygen or on sulfur in approximately equal amounts.Photolysis of P3-1-(2-nitrophenyl)ethyladenosine 5'-triphosphate, commonly called "caged ATP", was analyzed spectroscopically at pH values close to neutral in aqueous solvents by use of laser pulse photolysis.The kinetics of formation of the three products, ATP, 2-nitrosoacetophenone, and H+, were each monitored, as well as the kinetics of formation and decay of an intermediate presumed to be an aci-nitro compound (apparent ε406nm = 9.1 x 103 M-1 cm-1).For caged ATP in the presence of 3 mM MgCl2, and aci-nitro intermediate and H+ formed first at > 105 s-1 followed by the decay of the intermediate at 86 s-1 at pH 7.1, 21 deg C, and ionic strength 0.18 M.ATP, monitored by a biochemical assay, and 2-nitrosoacetophenone, monitored by a characteristic absorption band at 740 nm, were formed simultaneously with the decay of the intermediate under all conditions tested.The rate of decay of the aci-nitro intermediate was therefore used as a measure of the rate of release of the nucleotide analogues from their photolabile precursors.At pH 7.1, 0.18 M ionic strength, and 21 deg C the rate constants ranged from 35 to 250 s-1 and displayed a similar dependence on pH as caged ATP.The steady-state quantum yields of the 1-(2-nitrophenyl)ethyl phosphate esters were in the range 0.49 - 0.63.The deleterious effect of 2-nitrosoacetophenone on biological materials can be avoided by having thiols present.The reaction kinetics of dithiothreitol and 2-nitrosoacetophenone was described by a two-step process, the first step having a rate constant of 3.5 x 103 M-1 s-1 and the second 45 s-1 at pH 7.0, 21 deg C, and ionic strength 0.18 M.
