Current Medicinal Chemistry - Volume 12, Issue 7, 2005

Scientific endeavor evolves based on developments in physics, chemistry, and biology. Progress in three critical disciplines promises new frontiers in biomedicine: 1. Fast, efficient, high resolution, high sensitivity imaging instrumentation; 2. An understanding of the genome for several species and associated genomics, proteomics, etc.; 3. Novel pharmaceuticals providing high target selectivity and specificity, including antibodies, R Read More

Magnetic resonance imaging (MRI) contrast agents are utilized adjunctively to enhance the contrast between normal and abnormal structures on MRI scans. Along with the rapid evolution of the field has come a new appreciation for the medicinal chemistry of this unique class of metallopharmaceuticals. The efficacy of MRI agents is a complex function of chemical, biophysical, and pharmacological properties, whi Read More

Assessment of gene function following the completion of human genome sequencing can be performed with nuclear medicine procedures. These techniques may be applied for the determination of gene function and regulation using established and new tracers or using in vivo reporter genes such as genes encoding enzymes, receptors, antigens, or transporters. Visualization of in vivo reporter gene expression can be done usi Read More

We review recent progress in tumor imaging in vivo using fluorescent tags, highlight the problems of fluorescence imaging in small animals, discuss recent advances in near-infrared fluorochromes and quantum dots, and point to some future possibilities. GFP-based fluorescence imaging is briefly discussed. The authors believe that improvements in near-infrared fluorochromes are required to enable practical imaging in tissues at Read More

This review will discuss the production and applications of positron-emitting radionuclides for use in Positron Emission Tomography (PET), with emphasis on radionuclides that can be produced onsite with a biomedical cyclotron. In PET the traditional radionuclides of choice are 11C, 13N, 15O and 18F and although they will be briefly discussed in this article, the emphasis of this review will be on 'non-standard' PET radionuc Read More

The fluorine atom provides an exciting tool for diverse spectroscopic and imaging applications using Magnetic Resonance. The organic chemistry of fluorine is widely established and it can provide a stable moiety for interrogating many aspects of physiology and pharmacology in vivo. Strong NMR signal, minimal background signal and exquisite sensitivity to changes in the microenvironment have been exploited to design and apply Read More

The demand for peptide drugs is increasing and in this context, “post-assembly (or posttranslational) peptide modification strategies” by chemical manipulation of intact oligo-peptides has provided several analogues. Compounds prepared by this method are useful therapeutic molecules for structure activity studies. Herein, we describe various chemical methods such as cross-coupling reactions, cycloaddition reactions, radic Read More

The 2(3H)-benzoxazolone heterocycle and its bioisosteric surrogates (such as 2(3H)-benzothiazolinone, benzoxazinone, etc.) have received considerable attention from the medicinal chemists owing to their capacity to mimic a phenol or a catechol moiety in a metabolically stable template. These heterocycles and pyrocatechol have indeed similar pKa's, electronic charge distribution, and chemical reactivity. Thera Read More