• Bulletin of the Korean Chemical Society
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• v.25 no.6
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• pp.869-872
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• 2004

Newly synthesized 8-hydroxyquinoline based benzothiazole derivative 2 showed a distinctive $Hg^{2+}$-selectivity over other transition metal ions in aqueous solution. The fluorescence emission at 455 nm of 2 was completely quenched upon interaction with $Hg^{2+}$ ions in dioxane-$H_2O$ system (9 : 1, v/v). The selectivity was decreased in the order of $Hg^{2+}\;>>\;Cu^{2+}\;>\;Cd^{2+}\;>\;Pb^{2+}\;{\thickapprox}\;Zn^{2+}\;{\thickapprox}\;Ni^{2+},\;and\;Hg^{2+}$ concentration dependent fluorescence quenching profile was observed in the presence of common interfering metal ions as background. The fluorescence behavior of 2 suggests that the prepared compound could be used as a fluorescent signaling subunit for the construction of new $Hg^{2+}$-sensitive ON-OFF type supramolecular switching systems.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.8 no.1
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• pp.17-23
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• 2022

Boron neutron capture therapy is a precision treatment technology that selectively destroys only tumor cells by irradiating thermal neutrons after accumulating boron drugs in tumor cells. Brain tumor is difficult to diagnose and treat due to the low permeability and targeting of drugs caused by the blood-brain-barrier. Crossing the BBB is essential for drug delivery to the brain. In this study, we designed and synthesized a novel compound incorporating benzothiazole to develop a boron drug with high BBB permeability and selectivity for brain tumor cells. In addition, their potential as a BNCT drugs was evaluated.

• Bulletin of the Korean Chemical Society
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• v.34 no.12
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• pp.3654-3658
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• 2013

The synthesis of a DO3A conjugate of [(p-aniline benzothiazole)methyl]pyridine ($L^2H_3$) and its gadolinium complex of the type [$Gd(L^2)(H_2O)$] ($GdL^2$) is described. The $R_1$ relaxivity ($=4.50mM^{-1}sec^{-1}$) and kinetic inertness of $GdL^2$ compares well with those of structurally analogous Dotarem$^{(R)}$ ($R_1=3.70mM^{-1}sec^{-1}$), a typical extracellular (ECF) MRI contrast agent (CA). Yet, by comparison with Dotarem$^{(R)}$, $GdL^2$ exhibits non-covalent interactions with human serum albumin (HSA) as evidenced by the ${\varepsilon}^*$ titration curve along with in vivo MR signal enhancement in both aorta and heart. Liver-specific nature of $GdL^2$ is also observed as excretion is made through gallbladder. Most notably, $GdL^2$ further demonstrates specificity toward the MDA-MB-231 breast cancer.

• Bulletin of the Korean Chemical Society
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• v.18 no.4
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• pp.442-444
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• 1997

• Proceedings of the Korean Society of Dyers and Finishers Conference
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• 2008.10a
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• pp.83-84
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• 2008

A highly selective colorimetric chemosensor for $Hg^{2+}$ based on the semisquaraine(BSQ) containing benzothiazole moiety was investigated. BSQ showed color change only with $Hg^{2+}$ but it showed no significant changes upon addition of other metal ions such as $Ca^{2+},\;Pb^{2+},\;Al^{3+},\;Ce^{2+},\;Ba^{2+},\;Ni^{2+},\;Cd^{2+},\;Zn^{2+},\;and\;Mg^{2+}$. $Hg^{2+}$ ions coordinated to the BSQ forming 1:1 complex. The experimental data and conclusions are rationalized by $DMol^3$ calculation results.

• Bulletin of the Korean Chemical Society
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• v.27 no.2
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• pp.266-272
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• 2006

Three-dimensional quantitative structure-activity relationship (3D-QSAR) models were developed for 67 molecules of 2-amino-benzothiazole-6-anilide derivatives against lymphocyte-specific protein tyrosine kinase (P56 LCK). The molecular field analysis (MFA) and receptor surface analysis (RSA) were employed for QSAR studies and the predictive ability of the model was validated by 15 test set molecules. Structure-based investigations using molecular docking simulation were performed with the crystal structure of P56 LCK. Good correlation between predicted fitness scores versus observed activities was demonstrated. The results suggested that the nature of substitutions at the 2-amino and 6-anilide positions were crucial in enhancing the activity, thereby providing new guidelines for the design of novel P56 LCK inhibitors.

• Bulletin of the Korean Chemical Society
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• v.32 no.1
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• pp.131-136
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• 2011

Synthesis of N-(1H-benzimidazol-2-yl)-6-substituted-1,3-benzothiazol-2-amines and 6-substituted-N-(4,5-dihydro-1H-imidazol-2-yl)-1,3-benzothiazol-2-amines by the reaction of substituted 2-aminobenzothiazoles with carbon disulphide and methyl iodide followed by the reaction with o-phenylene diamine/ethylene diamine are reported. All the synthesized compounds were characterized by elemental analysis, IR spectra and $^1H$ NMR spectral studies. The potent antibacterial and entomological (antifeedant, acaricidal, contact toxicity and stomach toxicity) activities of the synthesized compounds were investigated.

• Archives of Pharmacal Research
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• v.29 no.5
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• pp.394-399
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• 2006

Benzothiazole derivatives of thiazolidinediones (TZD) were synthesized using a modified Mitsunobu reaction of 2-(benzothiazol-2-ylmethylamino)ethanol (2) with 5-(4-hydroxybenzyl)-3-triphenylmethylthiazolidine-2,4-dione and assayed for activity on peroxisome proliferator-activated receptor (PPAR) subtypes and inhibitory activity of NO production in lipopolysaccharide-activated macrophages. Most of the tested compounds were identified as potent $PPAR_\gamma$ agonists, indicating their potential as drug candidates for diabetes.

• Nuclear Medicine and Molecular Imaging
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• v.41 no.2
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• pp.112-117
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• 2007

Imaging distribution of ${\beta}-amyloid$ plaques in Alzheimer's disease is very important for early and accurate diagnosis. Early trial of the ${\beta}-amyloid$ plaques includes using radiolabeled peptides which can be only applied for peripheral ${\beta}-amyloid$ plaques due to limited penetration through the blood brain barrier (BBB). Congo red or Chrysamine G derivatives were labeled with Tc-99m for imaging ${\beta}-amyloid$ plaques of Alzheimer patient's brain without success due to problem with BBB penetration. Thioflavin T derivatives gave breakthrough for ${\beta}-amyloid$ imaging in vivo, and a benzothiazole derivative [C-11]6-OH-BTA-1 brought a great success. Many other benzothiazole, benzoxazole, benzofuran, imidazopyridine, and styrylbenzene derivatives have been labeled with F-18 and I-123 to improve the imaging quality. However, [C-11]6-OH-BTA-1 still remains as the best. However, short half-life of C-11 is a limitation of wide distribution of this agent. So, it is still required to develop an Tc-99m, F-18 or I-123 labeled agent for ${\beta}-amyloid$ imaging agent.

• Bulletin of the Korean Chemical Society
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• v.30 no.12
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• pp.2865-2866
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• 2009