Abstract: There are provided alpha helix scaffolds mimicking i, i+3/i+4, i+7 or i+11 residues having the general structure oxazole-pyridazine-piperidine or oxazole-pyridazine-oxazole. The common pyridazine heterocycle originates from substituted or unsubstituted dimethyl 1,2,4,5-tetrazine-3,6-dicarboxylate. These scaffolds are synthetic counterparts of amphiphilic alpha helices having a hydrophilic face along one side and a hydrophobic face along the other side of the helix.

Abstract: The synthesis of new ?-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available dimethyl pyridazine-3,6-dicarboxylate building block. These scaffolds may be thought of as synthetic counterparts of amphiphilic ?-helices having a hydrophilic face along one side and a hydrophobic face along the other side of the helix.

Abstract: Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.

Abstract: Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.

Abstract: Amphiphilic ?-helix mimetics are provided. These compounds are constructed using an oxazole-pyrrole-piperazine (OPP) scaffold. The amphiphilic ?-helix mimetics are also employable for making libraries and for treating diseases or conditions effected by the inhibition or disruption of interactions with the alpha helix of a protein.

Abstract: The synthesis of new ?-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available building block, 6. These scaffolds may be thought of as synthetic counterparts of amphiphilic ?-helices having a “wet face” along one side and a hydrophobic face along the other side of the helix.

Abstract: The present invention provides novel glycoluril derivatives for use as core molecules in combinatorial chemistry. Core molecules of the present invention can contain from one to six building blocks. Preferred building blocks are substituted amine radicals. Combinatorial libraries containing such core molecules are also provided.

Abstract: Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.

Abstract: The present invention provides novel glycoluril derivatives for use as core molecules in combinatorial chemistry. Core molecules of the present invention can contain from one to six building blocks. Preferred building blocks are substituted amine radicals. Combinatorial libraries containing such core molecules are also provided.

Abstract: The present invention provides novel glycoluril derivatives for use as core molecules in combinatorial chemistry. Core molecules of the present invention can contain from one to six building blocks. Preferred building blocks are substituted amine radicals. Combinatorial libraries containing such core molecules are also provided.

Abstract: Methods for the generation of new compounds are disclosed. The present invention eliminates the need to know in advance the structure or chemical composition of a compound having a desired property. The disclosure of the present invention provides that diversity of unknown compounds may be produced by “random” chemistry, and such a diversity of unknown compounds may be screened for one or more desired properties to detect the presence of suitable compounds. In one aspect, a starting group of organic compounds is caused to undergo a series of chemical reactions to create a diversity of new organic compounds that are screened for the presence of organic compounds having the desired property. In another aspect of the present invention, a diversity of compounds is generated from a group of substrates which are subjected to a group of enzymes representing a diversity of catalytic activities.

Abstract: Mechanically linked energy transfer labels comprising at least one donor fluorophore, at least one acceptor fluorophore, and at least one support member, wherein steric interactions between the donor fluorophore(s), the acceptor fluorophore(s), and/or the support member(s) induce non-covalent association between the fluorophores and the support member(s), thereby forming a three-dimensional macromolecular structure which mechanically links the donor fluorophore(s) and the acceptor fluorophore(s). Fluorescence resonance energy transfer (FRET) occurs from donor fluorophore to acceptor fluorophore through space. No direct connectivity with covalent bonds exists between the fluorophores. Instead, mechanical barriers hold the donor/acceptor fluorophores in place during the FRET process.

Abstract: Methods for forming combinatorial libraries and the libraries produced thereby are provided. According to a preferred aspect of the invention, a plurality of core molecules are reacted with a plurality of different tool molecules to form a library of molecules having non-naturally occurring molecular diversity. The libraries are useful for identifying lead compounds which modulate the functional activity of a biological molecule. Protease inhibitors that have been isolated from the libraries also are disclosed.

Abstract: Certain novel aminoacyl adenylate mimics are described. An exemplary compound of this invention is ?S-(R*,R*)!-3,6-anhydro-1,2-dideoxy-1-?5-?4-?(5-nitro-2-thienyl)ethynyl!ph enyl!-2H-tetrazol-2-yl!-D-allo-heptitol 7-(2-amino-3-methyl-1-oxopentyl)sulfamate. These compounds inhibit isoleucyl-tRNA synthetases and are useful as antimicrobial and antiparasitic agents.

Abstract: The compounds of the invention comprise the condensation product, as well as derivatives thereof, of two equivalents of a trimethyl cyclohexane-anhydride acid chloride derivative with one equivalent of an aromatic diamine. The scope of the invention includes the method of using the compounds of the invention as chelating agents for metals, metal ions or ions of metal complexes. In a preferred embodiment of the invention the binding moieties of the cyclohexane derivatives are rigidly held opposite each other, by restricting their rotation about the N-C aryl bonds, in order to more effectively bind the metals or the ions.

Abstract: The compounds of the invention comprise the condensation product, as well as derivatives thereof, of two equivalents of a trimethyl cyclohexane-anhydride acid chloride derivative with one equivalent of an aromatic diamine. The scope of the invention includes the method of using the compounds of the invention as chelating agents for metals, metal ions or ions of metal complexes. In a preferred embodiment of the invention the binding moieties of the cyclohexane derivatives are rigidly held opposite each other, by restricting their rotation about the N-C aryl bonds, in order to more effectively bind the metals or the ions.