Abstract: The present invention provides methods for high-throughput screening for bioactive compounds, in particular those that bind to RNA sequences involved in the pathogenesis of disease or in regulation of a physiological function. The methods involve measuring the conformation of an RNA target in the presence and absence of test ligands, and identifying as a ligand any test ligand that causes a measurable change in target RNA conformation.

Abstract: The present invention provides pharmaceutical formulations comprising 1,3,5-triazine derivatives. The compounds and formulations of the present invention exhibit a range of activities, including antiviral and antibiotic activities, and the formulations may be used, alone or in combination, as a method of treating a patient in need of antiviral and/or antibiotic therapy. The triazine derivatives of the present invention bind to and inhibit functional nucleic acids, and hence, have broad applicability in the treatment of conditions associated with DNA and RNA viruses.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: Disclosed are pharmaceutical compositions and formulations comprising the compound: wherein: (a) R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, or optionally substituted alkyl, aryl, vinyl, alkyl(aryl), vinyl(aryl), amine, amide; or at least one of R1 and R2, together, and R3 and R4, together, form an optionally substituted ring system, wherein the ring system is optionally interrupted by at least one heteroatom; (b) X is hydrogen, NO2, CN, halogen, OH, SO2, alkyl, alkoxy, or vinyl; and (c) wherein when R1, R2, R3, and R4 are alkyl, aryl, vinyl, alkyl(aryl), vinyl(aryl), amine or amide, R1, R2, R3, and R4 are optionally interrupted with at least one heteroatom, or a salt thereof; and a pharmaceutically acceptable carrier or diluent. Also disclosed are methods of inhibiting microbial replication and treating microbial infections, comprising administration of a pharmaceutical composition or formulation of the invention.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: The present invention provides azo and stilbene compounds having the structure: wherein XY is N.dbd.N, CH.dbd.CH, (C.dbd.O)--NH or NH--(C.dbd.O); wherein Z is CR.sub.6 or N; wherein R.sub.1, R.sub.2 and R.sub.5 are independently hydrogen, halogen, NO.sub.2 or CF.sub.3 ; wherein R.sub.3 is hydrogen, halogen, CF.sub.3, aryl or heteroaryl, NO.sub.2 or OCF.sub.3 ; wherein R.sub.4 is hydrogen, halogen, CF.sub.3, aryl or heteroaryl, NO.sub.2 or linear or branched chain alkoxy; wherein R.sub.6 is hydrogen or linear or branched alkyl; wherein R.sub.7 is hydrogen, cyano, hydroxyalkyl, carboxyl, halogen, hydroxyl, formyl, NO.sub.2 or halogen; and wherein R.sub.8 is hydroxyl or substituted or unsubstituted amino; and wherein R.sub.9 and R.sub.10 are independently hydrogen, CN or hydroxyalkyl. Said compounds are useful as antifungal therapeutics, fungicides and fungistats.

Abstract: 2-Deoxystreptamine is an aminocyclitol whose structural stability and abundant functionality make it an attractive scaffold for the combinatorial generation of small molecules. The ability to selectively functionalize the various positions of 2-deoxystreptamine with an almost infinite number of different groups ensures that the libraries so generated will be both spatially and functionally diverse. These compounds can then be screened for biological activity to afford lead compounds for pharmaceutical programs. Additionally, biological ligand mimics based on 2-deoxystreptamine can be readily appended, either directly or through a tether, to solid surfaces or incorporated covalently into gels to afford novel materials useful in separation science.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: Disclosed is a method for screening for inhibitors of Hepatitis B Virus pX activity. The method involves contacting a test compound with (I) the pX protein of HBV, (ii) a transcription factor comprising the bZIP domain, or fragments that comprise a minimal a bZIP domain, and (iii) an oligoduplex comprising a target DNA sequence of the transcription factor to form a test mixture. After incubating the test mixture under appropriate conditions and for a sufficient time to allow pX-mediated dimerization and DNA binding of the transcription factor to occur, the level of DNA binding of the transcription factor in each test mixture is determined. A test compound is considered to be any compound that causes a decrease in the level of DNA binding in the test mixture relative to the level of DNA binding in control mixtures.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: Disclosed is a method for the inhibition of binding of a ligand to an RNA, the inhibition being mediated by a small organic molecule that binds to the RNA, thereby inhibiting ligand binding. A preferred class of small organic molecules are compounds exemplified by 2,5-Bis[3-(2-N,N-dimethylaminopropylamidino)phenyl]furan.

Abstract: The invention provides novel yeast cells comprising genes whose expression can be modulated by growth in the presence or absence of metal ions, methods for making such yeast cells, and methods of using such yeast cells for determining the requirement for expression of particular genes for the growth or viability of the yeast cells.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: This invention provides a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.3 independently are hydrogen, --CHO, --COCH.sub.3, --COR.sup.7, --A--Ar--(Q).sub.z, etc.; wherein D is a C.sub.1-6 linear, C.sub.3-8 branched or cyclic group having from 4 to about 15 atoms, consisting of C, etc.; wherein D is unsubstituted or substituted with one or more groups independently selected from the group consisting of --OH, NH.sub.2, --NHR.sub.7, etc.; wherein each Q is independently --CNH(NHY), --NHCNH(NHY), --SO.sub.2 W, --SOW, etc.; wherein Y is hydrogen, alkyl, alkenyl, --B--NH.sub.2, --B--NHR.sup.8, etc.; wherein W is alkyl, alkenyl, --B--NH.sub.2, etc.; wherein A nd B independently are a bond, or a C.sub.1-6 linear, C.sub.3-8 branched or cyclic linking group having from 1 to about 15 atoms, consisting of C, optionally interrupted by N, S, P and O; wherein A and B independently are unsubstituted or substituted with --OH, NH.sub.2, etc.; wherein R.sup.7 is an alkyl, a branched alkyl, etc.; wherein R.sup.

Abstract: The subject invention, provides arylhydrazone compounds having the Formula 1: ##STR1## wherein A and B are independently aryl or heteroaryl and A and B independently are substituted with at least one group selected from alkyl, halogen, CN, COOR.sup.7, NR.sup.7 R.sup.8, CONR.sup.7 R.sup.8, NO.sub.2, SR.sup.7, SOR.sup.7, SO.sub.2 R.sup.7, NHCOR.sup.7, NHSO.sub.2 R.sup.7, OR.sup.7, hydroxyalkyl, and aminoalkyl. The compounds of this invention are useful for treating a wide variety of bacterial infections, including diseases of the skin, e.g., acne and skin ulcers, gastroenteritis, colitis, meningitis, keratinitis, conjunctivitis, diseases of the urinary and genital tracts, etc.

Abstract: A novel method for screening chemical compounds, test ligands, for potential pharmaceutical effectiveness. The disclosed method identifies possible therapeutic test ligands by placing them in the presence of target proteins and determining the ability of test ligands to increase the ratio of folded target protein to unfolded target protein. This differs significantly from known methods of novel pharmaceutical testing in that the biochemical function of the target protein need not be known and, except for one of the five embodiments of the method, the existence of any known ligands of the target protein is unnecessary.

Abstract: Disclosed is a method for the inhibition of binding of a ligand to an RNA, the inhibition being mediated by a small organic molecule that binds to the RNA, thereby inhibiting ligand binding. A preferred class of small organic molecules are compounds exemplified by 2,5-Bis[3-(2-N,N-dimethylaminopropylamidino)phenyl]furan.

Abstract: A novel method for screening chemical compounds, test ligands, for potential pharmaceutical effectiveness. The disclosed method identifies possible therapeutic test ligands by placing them in the presence of target proteins and determining the ability of test ligands to increase the ratio of folded target protein to unfolded target protein. This differs significantly from known methods of novel pharmaceutical testing in that the biochemical function of the target protein need not be known and, except for one of the five embodiments of the method, the existence of any known ligands of the target protein is unnecessary.