Patent classifications
C07C243/18
NOVEL THYROMIMETICS
Compounds are provided having the structure of Formula (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1, and Y.sup.2 are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
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NOVEL THYROMIMETICS
Compounds are provided having the structure of Formula (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1, and Y.sup.2 are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
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Electrochemical sensor for detection of heavy metal ions, and methods of preparation thereof
A surface modified electrode and a method of preparing the surface modified electrode are provided. The surface modified electrode includes a glassy carbon electrode and a coating of a compound of formula I disposed on the glassy carbon electrode. The present disclosure also relates to a method of preparing the surface modified electrode. The method includes depositing a slurry of the compound of Formula I on the glassy carbon electrode to form a film and coating a polymer matrix on the film to obtain the surface modified electrode. The present disclosure also relates to a method of preparing the compound of Formula I. The method includes condensing 4-bromobenzaldehyde (4-BBD) and 4-methyl-benzenesulphonylhydrazine (4-MBSH), to obtain a first mixture and precipitating the first mixture to obtain the compound of Formula I. The surface modified electrode is used in an electrochemical sensor for the detection of metal ions. ##STR00001##
Electrochemical sensor for detection of heavy metal ions, and methods of preparation thereof
A surface modified electrode and a method of preparing the surface modified electrode are provided. The surface modified electrode includes a glassy carbon electrode and a coating of a compound of formula I disposed on the glassy carbon electrode. The present disclosure also relates to a method of preparing the surface modified electrode. The method includes depositing a slurry of the compound of Formula I on the glassy carbon electrode to form a film and coating a polymer matrix on the film to obtain the surface modified electrode. The present disclosure also relates to a method of preparing the compound of Formula I. The method includes condensing 4-bromobenzaldehyde (4-BBD) and 4-methyl-benzenesulphonylhydrazine (4-MBSH), to obtain a first mixture and precipitating the first mixture to obtain the compound of Formula I. The surface modified electrode is used in an electrochemical sensor for the detection of metal ions. ##STR00001##
Inhibitors of histone lysine specific demethylase (LSD1) and histone deacetylases (HDACS)
A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.
Inhibitors of histone lysine specific demethylase (LSD1) and histone deacetylases (HDACS)
A series of phenelzine analogs comprising a phenelzine scaffold linked to an aromatic moiety and their use as inhibitors of lysine-specific demethylase 1 (LSD1) and/or one or more histone deacetylases (HDACs) is provided. The presently disclosed phenelzine analogs exhibit potency and selectivity for LSD1 versus MAO and LSD2 enzymes and exhibit bulk, as well as, gene specific histone methylation changes, anti-proliferative activity in several cancer cell lines, and neuroprotection in response to oxidative stress. Accordingly, the presently disclosed phenelzine analogs can be used to treat diseases, conditions, or disorders related to LSD1 and/or HDACs, including, but not limited to, cancers and neurodegenerative diseases.
COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
Photolabile linker for the solid-phase synthesis of hydrazides and pyranopyrazoles
The photolabile hydrazine linker of the present invention is based on the o-nitro-veratryl group, which is capable of releasing hydrazide derivatives upon UV irradiation. The linker allows for a new solid-phase peptide synthesis (SPPS) strategy which is fully orthogonal to the most commonly used protecting groups and chemical methods in SPPS and shows excellent compatibility with peptide composition, notably the 20 naturally occurring α-amino acid residues (even in their side-chain protected form) are accepted in the C-terminal of the peptide hydrazides. Furthermore, the linker unit can be applied to synthesize combinatorial libraries of biological interesting heterocyclic compounds, such as pyranopyrazoles.
Photolabile linker for the solid-phase synthesis of hydrazides and pyranopyrazoles
The photolabile hydrazine linker of the present invention is based on the o-nitro-veratryl group, which is capable of releasing hydrazide derivatives upon UV irradiation. The linker allows for a new solid-phase peptide synthesis (SPPS) strategy which is fully orthogonal to the most commonly used protecting groups and chemical methods in SPPS and shows excellent compatibility with peptide composition, notably the 20 naturally occurring α-amino acid residues (even in their side-chain protected form) are accepted in the C-terminal of the peptide hydrazides. Furthermore, the linker unit can be applied to synthesize combinatorial libraries of biological interesting heterocyclic compounds, such as pyranopyrazoles.