Pharmaceutical Potential

Synthetic Derivatives of Indoles as Pharmaceuticals. Thousands of indole derivatives have been prepared and evaluated as potential pharmaceuticals (32). Of those which have been put into use perhaps the most important are the nonsteroidal antiinflammatory agent indomethacin [53-86-1] (10) (33) and the p-adrenergic blocker pindolol [13823-86-9] (11) (34). 

Organ oselenium compounds, such as phosphine selenides, are being evaluated in solvent extraction systems for silver and gold (63). Also, potential pharmaceuticals containing selenium have been prepared (64). 

Formate-FDFI system was also applied in the reduction of 6-bromotetralone to (S)-6-bromotetralol, a potential pharmaceutical precursor, with the NADFI-depen-dent ketone reductase from Trichosporon capitatum [4b]. A resin (XAD L-323) was used to bind the product (Figure 8.4). 

At the point a compound is recognized and then considered for potential pharmaceutic or therapeutic usefulness, researchers will be both consumers of and contributors to the data-information-knowledge cycle that characterizes science. Initially, in the synthesis and purification phase of drug development, information about the compound s chemistry and physical properties may be both sought and created. Whether or not the compound has been of interest to other researchers may be determined by searching public records of grant and contract awards and also by searching resources that cover preliminary and early research results. The patent status of the compound may need to be established. 

A number of radiometals have nuclear properties suitable for diagnostic and/or therapeutic applications. The radiometals that form the basis of current radiopharmaceuticals, and those with nuclear properties most suitable for diagnostic or therapeutic applications, are discussed in terms of their chemistry, nuclear properties, and potential pharmaceutical applications. Two clearly... 

Many volumes have been written on the natural toxins of plants. While the negative elfects of plant toxins on people and the impact of plant toxins on livestock producers have been the most publicized, the diversity of these toxins and their potential as new pharmaceutical agents for the treatment of diseases in people and animals has received widespread interest in modern society. Scientists are actively screening plants from all regions of the world for bioactivity and potential pharmaceuticals for the treatment or prevention of many diseases. 

An pFl-dependent coordination isomerism has been observed for the tumor targeting rhenium(V) 0x0 complex [ReO(DMSA)2] (DMSA = 2,3-mercaptosuccinate). In solution the crystallo-graphically characterized syn,endo-isomQx (87a) slowly isomerizes into the anti- (87b) and the iyn,exo-isomers (87c) which has consequences for the biodistribution of the potential pharmaceutical (Scheme 10). The conversion rate decreases with increasing pH suggesting an acid catalyzed reaction. The syn,exo-comy> ex is favored in alkaline solutions (pH > 8.4) which can be understood in terms of the repulsions between the deprotonated carboxylic groups and the 0x0 ligand. 

The synthesis of amines from oximes is exemplified by the reduction of oxime 332 to 333 (99W032453) and of bicyclic oximes (derived from ketones 3 and 23a), for instance, of oxime 387 (Scheme 87) to amine 388 that is acylated to yield potential pharmaceutical agent 390 (92BML1147). Nucleophilic substitution of chloropyridine 384 generates morpholino derivative 385 (76IJB400). 

Clinical trials have been carried out on sydnofen (451) and sydnocarb (452) as psychostimulants or antidepressants. These two potential pharmaceuticals are of Russian origin. 

Microorganisms, particularly bacteria and fungi, have also proved to be a rich source of bioactive molecules such as antibiotics and anticancer agents (Chapter 1). Again, as in the case of plants, an incredibly rich array of microbial species inhabit the earth and their characteristic metabolic flexibility generates an enormous bank of potential pharmaceutical products. Most... 

The possibility of bench testing for screening potential pharmaceutical active substances for confirmation of the outcomes of silicon tests. This may shorten the time frame to reach clinical trials for potential drug candidates and allow a more systematic drug development process... 

Recent Trends in the Use of Natural Products and Their Derivatives as Potential Pharmaceutical Agents... 

In any case, the goal of the effort is to obtain a prototype lead compound, which, when appropriately modified, will yield a drug candidate for further development. Historically, most prototype bioactive substances have been natural products, and evidence that natural products continue to offer a virtually unlimited supply of potential pharmaceuticals and agrochemicals abounds in the literature. It has been estimated that there are more than 250,000 species of higher plants on our planet, yet only a fraction of these have been investigated to characterize their chemical constituents, and an even smaller number have been... 

Several complexes have been tested for potential pharmaceutical applications and some of them have been introduced into practice.84,126 Isolation of antibiotics of boron complex type (Section 24.3.3.2) and results obtained with carboxyborane complexes that are analogues of amino acids (Section 24.2.2) are likely to stimulate further studies. Quite a few boron complexes have found application in 10B neutron capture therapy based on the 10B(n, a)7Li nuclear reaction.84,126,172... 

The Ugi four-component condensation (U-4CC) between an aldehyde, an amine, a carboxylic acid and an isocyanide allows the rapid preparation of a-aminoacyl amide derivatives. The Ugi Reaction products can exemplify a wide variety of substitution patterns, and constitute peptidomimetics that have potential pharmaceutical applications. This reaction is thus very important for generating compound libraries for screening purposes. 

---