Therapeutic utility

These studies trace the evolution of penicillin investigations from microbiological curiosity through the development of increasing therapeutic utility to increasingly sophisticated chemical manipulations. This chapter will focus primarily on the chemical aspects of this area. Because of the vast amount of relevant literature, it has been possible to discuss only selected studies which hopefully are representative of the different investigative directions. The reader is urged to consult the cited references for more detailed discussion and for references to related studies. 

Forskolin is an activator of the enzyme adenylate cyclase which has therapeutic utility. Outlined below are stereocontrolled routes to racemic and natural chiral forms of forskolin derived by multistrategic retrosynthedc analysis. 

Though the therapeutic utility of aspiri n has been recognized for well over a century, this venerable drug was not classified as a nonsteroid antiinflammatory until recently. The first drug to be so classified was in fact, indomethacin (1), a very useful agent introduced... 

Figure 8.4b). Some of the early antihistamines were found to exert antidepressant and antipsychotic properties. These led to modem psychopharmaceuticals. The immunosuppressant activity of the fungal agent cyclosporine also was exploited for therapeutic utility. 

The therapeutic utility of systemically administered ASON had been limited by their short plasma half life (sometimes even less than 3 min). This is due to their sensitivity to nuclease digestion. When the first-generation ASON were chemically modified, e.g., by replacing the oxygen in the phosphodiester bond with sulfur (phosphorothiorate) they obtained an increased stability in biological fluids while their antisense effect has been maintained. First-generation agents can be delivered via intravitreal injection, parenterally, by topical cream, enema, and inhaled aerosol. These antisense... 

In conclusion, H3 ligands offer the attractive vista of multiple applications in various disorders, but the ultimate definition of their therapeutic utility will have to await clinical trial results. Future work will determine whether inverse agonists, neutral antagonists, or protean agonists will constitute the more useful pharmacological intervention. 

Pharmacists should also take a dim view of changes in the particle size, size distribution, or particulate nature of semisolid suspensions. They are the consequence of crystal growth, changes in crystalline habit, or the reversion of the crystalline materials to a more stable polymorphic form. Any crystalline alteration can lead to a pronounced reduction in the drug-delivery capabilities and therapeutic utility of a formulation. Thus, products exhibiting such changes are seriously physically unstable and unusable. 

Cannabis sativa, one of the oldest plants farmed by man, has been known for its medicinal properties for at least four millennia (Peters, 1999). The psychoactive-euphoric effects of this plant, as well as its facile and wide climatic range of cultivation, have rendered it a very popular recreational drug. Today, cannabis, or marijuana, is still the focus of strong social, legal, and medical controversy over its therapeutic utility. 

Diaminopyrimidines antibacterials, 3 9 preparation and manufacture, 3 16 therapeutic utility, 3 20... 

See also Antibacterial oxazolidinones antibacterials, 3 8 binding sites in, 77 736 optically pure, 77 740 preparation and manufacture, 3 13-14 therapeutic utility, 3 18 world market for, 3 16t Oxazolidone products, 70 410 Oxichromic developers, dye images from, 79 287-288... 

Pharmacotherapies contribute greatly to human health and longevity. As such, researchers in the public and private sectors make an enormous investment in drug design and refinement and preclinical and clinical testing. Such efforts often result in a marketed compound that expands the options for the treatment and prevention of human diseases. However, on rare occasions, medications associated with adverse effects - ranging from undesirable to potentially fatal - that greatly reduce or even eliminate their therapeutic utility reach the marketplace. 

Retinoic acid works through a family of retinoic acid receptors. Activated retinoic acid receptors act as transcription factors, just as activated steroid receptors do (chapter 20), and alter the transcription of genes affecting cell division and survival. This underlies both the teratogenic potential and the therapeutic utilities of these potent molecules. 

This relatively small DCL yielded the first peptidic ligand for G-quadruplex DNA, providing a lead compound for the further development of novel G-quadruplex ligands with possible therapeutic utility. 

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