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  • 1
    Electronic Resource
    Electronic Resource
    Design, synthesis and use of binary encoded synthetic chemical libraries (1996)
    Springer
    Molecular diversity 2 (1996), S. 81-88 
    Details
    ISSN: 1573-501X
    Keywords: Library construction ; Split synthesis ; Split-and-pool ; Dihydrobenzopyran library
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary With the advent of combinatorial chemistry a new paradigm is evolving in the field of drug discovery. The approach is based on an integration of chemistry, high-throughput screening and automation engineering. The chemistry arm is usually based on solid-phase synthesis technology as the preferred approach to library construction. One of the most powerful of the solid-phase methods is encoded split synthesis, in which the reaction history experience by each polymeric bead is unambiguously recorded. This split-and-pool approach, employing chemically robust tags, was used to construct a 85 000-membered dihydrobenzopyran library.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01718704
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Interaction of the component enantiomers of the putative dopamine autoreceptor agonist, TL-99 (6,7-dihydroxy-2-dimethylamino tetralin) with dopaminergic systems in mammalian brain and teleost retina (1983)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 324 (1983), S. 275-280 
    Details
    ISSN: 1432-1912
    Keywords: Dopamine autoreceptor ; Dopamine receptors ; TL-99
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The enantiomers of the putative dopamine auto-receptor agonist, TL-99 (6,7-dihydroxy-2-dimethylaminotetralin) were examined in a number of in vivo and in vitro test paradigms to further examine the reported autoreceptor selectivity of this compound. The (+)-isomer of the aminotetralin was more active as a dopamine agonist than either the racemate or the (−)-enantiomer. In addition to this dopaminergic activity, TL-99 was found to be a potent α2-adrenoceptor agonist, this activity being more prominent in the (+)-isomer. The (−)-isomer, however, was a weak α2/DA receptor agonist and unlike the (+)-enantiomer was devoid of activity in the D-1-selective carp retina adenylate cyclase assay. Pharmacological examination of the effects of TL-99 on mouse locomotor activity showed that the effects of the aminotetralin in this dopamine autoreceptor test system were antagonized by either the α2-antagonist, yohimbine or by the dopamine antagonist, sulpiride. TL-99 also produced contralateral turning in 6-OHDA lesioned rats. It is concluded that the apparent dopamine autoreceptor selectivity of TL-99 as assessed by in vivo animal test systems may be due partially to its α2-agonist activity. The sedation and consequent reduction in mouse locomotor activity and in turning in the rat as the dose level is increased undoubtedly occurs via α2-agonist and dopamine autoreceptor acitivity and cannot be interpreted as selectivity for the dopamine autoreceptor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00502623
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Binary encoded small-molecule libraries in drug discovery and optimization (1995)
    Springer
    Perspectives in drug discovery and design 2 (1995), S. 305-318 
    Details
    ISSN: 1573-9023
    Keywords: Combinatorial library ; Encoded ; Binary ; Tag ; Structure-function ; Solid support
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary A variety of small-molecule combinatorial libraries have been prepared on solid support using a binary encoding strategy employing non-sequenceable encoding molecules. Library members are attached to the support using photolabile linkers which permit their release for assay free in solution. The encoding molecules are attached using a carbene insertion reaction and are released via oxidation. A wide variety of synthetic reactions have been utilized for library synthesis including, for example, cyclocondensations, reductive aminations, and heteroaromatic halide displacements, as well as acylations and sulfonylations. Initial screening of two such libraries identified lead structures for the inhibition of carbonic anhydrase. Subsequently, based upon these leads a smaller focused combinatorial library was constructed and used to analyze the structure-activity relationships (SARs) governing enzyme inhibition and isozyme selectivity. The combination of random screening with a broad diversity of compounds, followed by focused libraries for detailed SARs and selectivity, demonstrates the power of binary encoded small-molecule combinatorial libraries for drug discovery.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02172069
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    Paper (German National Licenses)
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