• Nuclear Medicine and Molecular Imaging
• /
• 제41권2호
• /
• pp.91-96
• /
• 2007

The measurement of pathologically low levels of tissue $pO_2$ is an important diagnostic goal for determining the prognosis of many clinically important diseases including cardiovascular insufficiency, stroke and cancer. The target tissues nowaday have mostly been tumors or the myocardium, with less attention centered on the brain. Radiolabelled nitroimidazole or derivatives may be useful in identifying the hypoxic cells in cerebrovascular disease or traumatic brain injury, and hypoxic-ischemic encephalopathy. In acute stroke, the target of therapy is the severely hypoxic but salvageable tissue. $^{18}F-MISO$ PET and $^{99}mTc-EC-metronidazole$ SPECT in patients with acute ischemic stroke identified hypoxic tissues and ischemic penumbra, and predicted its outcome. A study using $^{123}I-IAZA$ in patient with closed head injury detected the hypoxic tissues after head injury. Up till now these radiopharmaceuticals have drawbacks due to its relatively low concentration with hypoxic tissues associated with/without low blood-brain barrier permeability and the necessity to wait a long time to achieve acceptable target to background ratios for imaging in acute ischemic stroke. It is needed to develop new hypoxic marker exhibiting more rapid localization in the hypoxic region in the brain. And then, the hypoxic brain imaging with imidazoles or non-imidazoles may be very useful in detecting the hypoxic tissues, determining therapeutic strategies and developing therapeutic drugs in several neurological disease, especially, in acute ischemic stroke.

• Bulletin of the Korean Chemical Society
• /
• 제25권3호
• /
• pp.392-394
• /
• 2004

• 대한약학회:학술대회논문집
• /
• 대한약학회 2004년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.151-151
• /
• 2004

• Bulletin of the Korean Chemical Society
• /
• 제35권10호
• /
• pp.3009-3014
• /
• 2014

A palladium-catalyzed C-H arylation reaction of nitroimidazoles and nitropyrazoles was developed using aryl bromides as arene donors. The electron-withdrawing effect of the nitro group allows for direct C-H arylation reactions of the nitro diazoles with high regioselectivity under mild conditions. The new C-H arylation approach is thus complementary to nucleophilic substitution reactions, enabling the preparation of complex nitroazole compounds.

• 대한방사성의약품학회지
• /
• 제2권1호
• /
• pp.22-36
• /
• 2016

$^{68}Ga$ is a promising radionuclide for positron emission tomography (PET). It is a generator-produced ($^{68}Ge/^{68}Ga$-generator) radionuclide with a half-life of 68 min. The employment of $^{68}Ga$ for basic research and clinical applications is growing exponentially. Bifunctional chelators (BFCs) that can be efficiently radiolabeled with $^{68}Ga$ to yield complexes with good in vivo stability are needed. Given the practical advantages of $^{68}Ga$ in PET applications, gallium complexes are gaining increasing attention in biomedical imaging. However, new $^{68}Ga$-labeled radiopharmaceuticals that can replace $^{18}F$-labeled agents like [$^{18}F$]fluorodeoxyglucose (FDG) are needed. The majority of $^{68}Ga$-labeled derivatives currently in use consist of peptide agents, but the development of other agents, such as amino acid or nitroimidazole derivatives and glycosylated human serum albumin, is being actively pursued in many laboratories. Thus, the availability of new $^{68}Ga$-labeled radiopharmaceuticals with high impact is expected in the near future. Here, we present an overview of the different new classes of chelators for application in molecular imaging using $^{68}Ga$ PET.

• Bulletin of the Korean Chemical Society
• /
• 제16권10호
• /
• pp.912-915
• /
• 1995

Ornidazole, C7H10ClN3O3, crystallizes in the triclinic, space group P1^, with a=13.605(2), b=14.054(1), c=8.913(5) Å, α=71.59(2), β=78.73(2), γ=64.86(1)°, μ=3.26 cm-1, Dc=1.499 g/cm3, Dm=1.497g/cm3, F(000)=684, and z=6. Intensities for 2693 unique reflections were measured on a CAD4 diffractometer with graphite-monochromated Mo-Kα radiation. The structure was solved by direct method and refined by block-diagonal least squares to a final R of 0.081 (Rw=0.047) for 1952 reflections with Fo>3σ (Fo). The asymmetric unit contains three independent molecules of the title compound. The bond lengths and bond angles are comparable with the values found in the other nitro-substituted compounds. The nitro groups are rotated (6.9°, 6.6°, 2.6° for the three independent molecule, respectively) about the C-N axes from the imidazole planes. The crystal structures are linked by two intermolecular hydrogen bonds of O-H---N type and one intermolecular hydrogen bond of O-H---O type.