Selective toxicity/selectivity

Selective toxicity (selectivity) Difference in toxicity of a chemical toward different species, strains, sexes, age groups, etc. 

All of these compounds are inhibitors of dihydrofolate reductase in bacteria, plasmodia, and humans. Fortunately, they have a significantly higher affinity to bacterial and protozoal dihydrofolate reductase. Pyrimethamine, for example, inhibits dihydrofolate reductase in parasites in concentrations that are a several hundred times lower than that required to inhibit dihydrofolate reductase in humans. This is the basis of their selective toxicity. Selective toxicity can be elevated upon the host organism s production of folic acid, which parasites are not able to use. 

CgH,3BrN202. A soil-acting herbicide. White crystalline solid, m.p. 158-159" C. It is a non-selective inhibitor of photosynthesis used for weed control In citrus and cane fruit plantations. It is relatively non-toxic to animal life. 

Lead structure According to Valler and Green s definition a lead structure is a representative of a compound series with sufficient potential (as measured by potency, selectivity, pharmacokinetics, physicochemical properties, absence of toxicity and novelty) to progress to a full drug development program [12]. 

Foremost we hope - and believe - that chemoinformatics will become of increasing importance in the teaching of chemistry. The instruments and methods that are used in chemistry will continue to swamp us with data and we have to manage these data to increase our chemical knowledge. We have to understand more deeply, and exploit, the results of our experiments. Concomitantly, demands on the properties of the compounds that are produced by the chemical and pharmaceutical industries will continue to rise. We will need materials that are better we need them to be more selective, have fewer undesirable properties, able to be broken down easily in the environment without producing toxic by-products, and so on. This asks for more insight into the relationships between chemical structures and their properties. Furthermore, we have to plan and perform fewer and more efficient experiments. 

Moreover, multivariate optimization, the simultaneous optimization of several properties, will increasingly come into focus. A drug should have high selectivity in binding to different receptors and minimal toxicity, good solubility and penetration, and so on. A hair color should have a brilliant shine, be absorbed well, not be washed out, not damage the hair, not be toxic, and be stable under sunlight, etc. 

Antibiotics are toxic water-solubie compounds produced by molds or bacteria which inhibit the growth of other microorganisms. For an antibiotic to be useful in medicine it should have a high order of selective toxicity to microorganisms which are pathogenic to man. Al-... 

The term chiral recognition refers to a process m which some chiral receptor or reagent interacts selectively with one of the enantiomers of a chiral molecule Very high levels of chiral recognition are common m biological processes (—) Nicotine for exam pie IS much more toxic than (+) nicotine and (+) adrenaline is more active than (—) adrenaline m constricting blood vessels (—) Thyroxine an ammo acid of the thyroid gland that speeds up metabolism is one of the most widely used of all prescription... 

Institut Eransais du Pntrole dimethyl sulfoxide (DMSO) solvent contains up to 2% water to improve selectivity reflux con-sist of aromatics and paraffins ambient rotating-blade extractor, typically 10—12 stages low corrosion allows use of carbon steel equipment solvent has alow freezing point and is non-toxic two-stage ex-traction has dis-placement solvent in the second stage... 

Triaryl phosphates are produced from the corresponding phenols (usually mixtures) by reaction with phosphoms oxychloride, usually in the presence of a catalyst (94—96). They are subsequently distilled and usually washed with aqueous bases to the desired level of purity. Tricresyl phosphate was originally made from petroleum-derived or coal-tar-derived cresyflc acids, ie, cresols, variously admixed with phenol and xylenols. Discovery of the toxicity of the ortho-cresyl isomers led manufacturers to select cresols having very Httle ortho-isomer. 

Herbicides are also sometimes classified according to mode of action, selectivity, registered uses, and toxicity. The ever-increasing importance of herbicides and other pesticides and agrochemicals to a wide range of users, regulators, and researchers has led to the development of multiple and extensive computer databases. The primary database resources contain collected information relevant to herbicides, and numerous resource pubHcations are available to those needing information on the various aspects of herbicides (2). 

The development of malathion in 1950 was an important milestone in the emergence of selective insecticides. Malathion is from one-half to one-twentieth as toxic to insects as parathion but is only about one two-hundredths as toxic to mammals. Its worldwide usage in quantities of thousands of metric tons in the home, garden, field, orchard, woodland, on animals, and in pubHc health programs has demonstrated substantial safety coupled with pest control effectiveness. The biochemical basis for the selectivity of malathion is its rapid detoxication in the mammalian Hver, but not in the insect, through the attack of carboxyesterase enzymes on the aUphatic ester moieties of the molecule. 

Insect Growth Regulators. These compounds (40—45), unlike most conventional insecticides, interfere with biochemical processes that are unique to arthropods eg, molting, ecdysis, and formation of the chitinous exoskeleton. Therefore, they are selective insecticides with very low mammalian toxicity. 

Diketones can be prepared by oxidation of the corresponding monoketone (287) or a-hydroxyketone (288). 1,2-Diketones are used extensively as intermediates in the preparation of pharmaceuticals, flavors, and fragrances. Toxicity data for selected diketones are shown in Table 11. 

Triaryl phosphates are produced by reaction of phosphoms oxychloride with phenoHc compounds at 100—200°C with magnesium or aluminum chloride catalyst. Past use of cresols and xylenols from coal tar or petroleum is replaced for lower toxicity and cost by synthetic phenoHcs, primarily isopropyl phenol, /-butyl phenol, and phenol itself A range of viscosities is achieved by selection and proportioning of the phenols and their isomers used for the starting material. 

Table 20. Toxicity Data for Select Manganese Compounds ...

Safety. The principal concerns regarding nuclear medical imaging are those associated with the radiopharmaceuticals. Much research has gone into the selection of radiopharmaceuticals exhibiting minimal toxicities, rapid elimination from the body, and short half-life. The radioisotope must be... 

In general, the polymethacrylate esters of the lower alcohols are soluble in aromatic hydrocarbons, esters, ketones, and chlorohydrocarbons. They are insoluble, or only slightly soluble, in aUphatic hydrocarbons and alcohols. The polymethacrylate esters of the higher alcohols (>C ) are soluble in ahphatic hydrocarbons. Cost, toxicity, flammabiUty, volatihty, and chain-transfer activity are the primary considerations in the selection of a suitable solvent. 

Pigments and Extenders. Pigments are selected for use in house paints based on thek appearance and performance quaUties. Appearance includes color and opacifying abiUty. Performance quaUties include ultraviolet light resistance, fade resistance, exterior weatherabiUty, chemical resistance, as well as particle size and shape. Toxicity profiles and safety and health related properties are also important criteria in pigment selection. 

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