Abstract: A combinatorial method for discovering or optimizing materials is disclosed. The method uses solution-based components that are mixed and dispensed into regions on a substrate for drying and/or heat-treating. The drying and/or heat-treating produces materials that can be tested for a desired property.

Abstract: Disclosed are cyclic imino oligomers and polymers comprised of subunits of the formula: Also disclosed are combinatorial libraries and arrays of the cyclic imino compounds.

Abstract: Agonist analogues of amylin and related pharmaceutical compositions, and methods of treatment of diabetes and other insulin-requiring states, as well as methods of treatment of hypoglycemia, are provided.

Abstract: The present invention relates to methods for identifying compounds that modulate enzymatic activity by contacting covalently bonded PTP-extender complexes or modified covalently bonded PTP-extender complexes with ligand candidates.

Abstract: This invention relates to the enzymatic synthesis of oligophenols on solid support by sequential enzymatic addition of reaction solutions containing phenols. The oligomers are then selectively built up on the solid surface. When used in a specific format, the oligomers can be generated in a spatially addressable array, which can then be screened for some type of biological interaction. The synthetic compounds of the present invention are synthesized in a combinatorial manner on solid support using peroxidase or other related enzymatic catalysis, and the products are generated in spatially addressable microarrays. Oligophenols of the present invention have shown significance as potential inhibitors of NADPH oxidase assembly, an enzyme that has been implicated in a wide range of diseases stemming from vascular hyperpermeability.

Abstract: The invention encompasses an improved, rapid, size-exclusive method for screening for small molecular weight ligands that bind specifically to a protein target, using size-exclusion separation, ultrafiltration, and mass spectrometry.

Abstract: A process is disclosed for modifying a parent ligand by attaching to the parent ligand a conjugation agent that is reactive with a moiety of a target receptor to which the parent ligand binds such that a covalent bond is formable between the conjugation agent and the receptor moiety. Also disclosed are compositions, probes and methods of detecting and/or quantifying receptors using the modified ligands of the invention.

Abstract: One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.

Abstract: A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide.

Abstract: A combinatorial library includes a gelcast substrate defining a plurality of cavities in at least one surface thereof; and a plurality of gelcast test materials in the cavities, at least two of the test materials differing from the substrate in at least one compositional characteristic, the two test materials differing from each other in at least one compositional characteristic.

Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.

Abstract: This invention provides methods for treating a mycobacterial infection by administering to an animal a pharmaceutical composition containing a compound having the formula R—SOn—Z—CO—Y, where R is an alkyl group having 6-20 carbons; Z is a radical selected from —CH2—, —O—, and —NH—, two of these radicals coupled together, or —CH2═CH2—; Y is —NH2, O—CH2—C6H5, —CO—CO—O—CH3, or O—CH3; and n is 1 or 2. It has been discovered that these compounds inhibit growth of microbial cells which synthesize &agr;-substitued, &bgr;-hydroxy fatty acids, particularly corynemycolic acid, nocardic acid, and mycolic acid. These compounds may be used to inhibit growth of mycobacterial cells, such as Mycobacterium tuberculosis, drug-resistant M. tuberculosis, M. avium intracellulare, and M. leprae.

Abstract: The use of hydroxyphenylvinylthiazoles of formula wherein R1, R2, R3 and R4 are each independently of the others hydrogen; halogen; hydroxy, C1-C16-alkyl, C1-C16alkoxy, phenyl; phenyl-C1-C3alkyl; C6-C10aryloxy, amino, mono-C1-C5alkyl-amino, di-C1-C5alkylamino or -NO2; wherein at least one of the radicals R1, R2, R3 and R4 is hydroxy; R5 is C1-C5alkyl; C1-C5alkoxy; or unsubstituted or halo-, C1-C5alkyl-, C1-C5alkoxy-, hydroxy- or pyrrolidinyl-substituted phenyl; as microbicidal active ingredients is described. The compounds exhibit a pronounced action against pathogenic gram-positive and gram-negative bacteria, and also against yeasts and moulds. Accordingly, they are suitable for the antimicrobial treatment, especially the preservation and disinfection, of surfaces.