5-Chloro-1-methyl-4-nitroimidazole ..

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291. Hoigebazar L, Jeong JM, Choi SY, Choi JY, Shetty D, Lee YS. . Synthesis and characterization of nitroimidazole derivatives for 68Ga-labeling and testing in tumor xenografted mice. 2010;53:6378-85

5-Nitroimidazole derivatives: A scope of Modification for Medicinal chemists

of 2‐methyl‐5‐nitroimidazole ..

The spatial and temporal resolution of instrumentation, radionuclide decay mode and energy as well as organ movement and size influence the accuracy of PET quantitation which is especially crucial when monitoring the treatment response with marginal changes. Scanning technology and data reconstruction technique have been improved during last 10-15 years in order to meet the requirements. These advances will definitely stimulate development of 68Ga-based imaging agents, empowered by the relation to the therapy selection and planning. It should be stressed that the full potential of the imaging technology can only be realized if new imaging agents for specific indications emerge. Improved clinical outcomes of molecular imaging-guided radiation therapy have already been demonstrated []. PET radiopharmaceuticals induce adverse reactions extremely seldom with no serious or life-threatening events []. While hybrid imaging, PET-CT and PET-MRI, may require high dose of CT and MRI contrast agents thus enhancing the probability of adverse events.

One of the most rapidly expanding areas is the development of peptide-based agents for targeted imaging. Metal and halogen radionuclides such as 64Cu, 89Zr, 99mTc, 111In, 18F, and 124I are most commonly used for the design of the agents. Typically, the metal ion coordination chemistry is straightforward and mild. However, it requires attachment of a rather bulky chelator to the vector molecule what may deteriorate the biological activity. Simple direct iodination has been used for decades introducing minor modification at tyrosine amino acid residue though demonstrating poor residualizing of the radioactive iodine catabolites in the cell. On the contrary hydrophilic complexes of radiometals stay trapped in the cell after the degradation of the internalized imaging agent. The incorporation of 18F can be accomplished by the conventional nucleophilic or electrophilic addition, or via prosthetic groups []. However, the synthesis might be rather complex with harsh conditions and high macromolecule concentration. A novel method utilizing similarity of Al18F2+ with metal cations and thus possibility of coordination labelling chemistry has potential for kit type production like radiometals []. The relatively long half-life (110 min) of 18F enables centralized production and distribution of either the radionuclide or prepared imaging agents to the satellite clinical centres. Most of the PET agents used in clinical studies are 18F-based. Nevertheless, the simpler labelling chemistry of 68Ga and its availability from the generator system which can be used even at distant and isolated medical centres make 68Ga more preferable.

Synthesis of Metal-Organic Frameworks (MOFs): Routes …

129. Azad BB, Cho CF, Lewis JD, Luyt LG. Synthesis, radiometal labeling and in vitro evaluation of a targeted PPIX derivative. 2012;70:505-11

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Norbert Stock has received his Ph.D. degree in chemistry with Prof. Schnick in 1998 at the University of Bayreuth and has spent the next 15 months as a postdoc in the groups of Prof. Ferey, Prof. Cheetham, and Prof. Stucky at the University of Versailles and University of California at Santa Barbara. In 2000, he joined the group of Prof. Bein at the Ludwig-Maximilians University of Munich, where he finished his habilitation in 2004. In the same year, he became Professor at the Institute of Inorganic Chemistry at the Christian-Albrechts-University in Kiel. His research interests are within the field of inorganic–organic hybrid compounds. He has been involved in the development and application of high-throughput methods for reactions under solvothermal conditions. Thus, he is interested in the discovery of new hybrid compounds, in understanding their formation, as well as in setting up synthesis–structure relationships.

August « 2017 « New Drug Approvals

134. Knor S, Modlinger A, Poethko T, Schottelius M, Wester HJ, Kessler H. Synthesis of novel 1,4,7,10-tetraazacyclodecane-1,4,7,10-tetraacetic acid (DOTA) derivatives for chemoselective attachment to unprotected polyfunctionalized compounds. 2007;13:6082-90

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138. Yim CB, van der Wildt B, Dijkgraaf I, Joosten L, Eek A, Versluis C. . Spacer effects on in vivo properties of DOTA-conjugated dimeric [Tyr3]octreotate peptides synthesized by a "Cu(I)-click" and "sulfo-click" ligation method. 2011;12:750-60