Library of 1,4-Disubstituted 1,2,3-Triazole Analogs of Oxazolidinone RNA-Binding Agents
摘要:
The design and synthesis of small molecules that target RNA is immensely important in antibacterial therapy. We had previously reported on the RNA binding of a series of 4,5-disubstituted 2-oxazolidinones that bind to a highly conserved bulge region of bacterial RNA. This biological target T box antitermination system, which is found mainly in Gram-positive bacteria, regulates the expression of several amino acid related genes. In an effort to amplify our library, we have prepared a library of I,4-disubstituted 1,2,3-triazole analogs that entails an isosteric replacement of the oxazolidinone nucleus. The synthesis of the new analogs was enhanced via copper(I) catalysis of an azide and alkyne cycloaddition reaction. A total of 108 1,4-disubstituted 1,2,3-triazole compounds have been prepared. All compounds were evaluated as RNA binding agents.
COMPOSITIONS AND METHODS FOR TREATMENT OF RENAL FAILURE
申请人:Technion Research and Development of Foundation,
Ltd.
公开号:EP1942881A2
公开(公告)日:2008-07-16
TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES
申请人:Oryzon Genomics SA
公开号:EP2195029A2
公开(公告)日:2010-06-16
METHODS AND REAGENTS FOR RADIOLABELING
申请人:Memorial Sloan-Kettering Cancer Center
公开号:US20170029426A1
公开(公告)日:2017-02-02
The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things, novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I.
[EN] COMPOSITIONS AND METHODS FOR TREATMENT OF RENAL FAILURE<br/>[FR] COMPOSITIONS ET METHODES DE TRAITEMENT DE L'INSUFFISANCE RENALE
申请人:TECHNION RES & DEV FOUNDATION
公开号:WO2007039909A2
公开(公告)日:2007-04-12
[EN] Propargylamine, propargylamine derivatives including N-propargyl-1-aminoindan and analogs thereof, and pharmaceutically acceptable salts thereof, are useful for prevention or treatment of renal failure. [FR] L'invention concerne la propargylamine, des dérivés de la propargylamine comprenant N-propargyl-1-aminoindan et des analogues de celui-ci et des sels acceptables sur le plan pharmaceutique de ceux-ci, utiles dans la prévention ou le traitement de l'insuffisance rénale.
[EN] TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES<br/>[FR] TRAITEMENT ET PRÉVENTION DE MALADIES NEURODÉGÉNÉRATIVES
申请人:ORYZON GENOMICS SA
公开号:WO2009027349A2
公开(公告)日:2009-03-05
The treatment and prevention of neurodegenerative diseases by repression of the transcriptional complex that silences the promoter of the UCHL1 gene.