92126-32-4Relevant academic research and scientific papers
HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
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Paragraph 00314, (2015/12/30)
Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, or pharmaceutically acceptable salts thereof, compositions thereof, and methods of their use. The condition or disorder mediated by HDAC comprises a neurodegenerative pathology. Accordingly, also provided is a method of treating a neurodegenerative pathology mediated by HDAC in a subject in need of such a treatment, comprising administering to the subject a therapeutically effective amount of at least one compound, or pharmaceutically acceptable salt thereof, described herein.
Nitrile Sulfides Part 16.1,2Synthesis of 1,2-benzisothiazolesvia nitrile sulfide cycloaddition reactions
Ross, John F.,Delipala, Christina,Watson, Matthew C.,Crosby, John,Paton, R. Michael
, p. 1 - 18 (2013/07/25)
The cycloaddition reactions of nitrile sulfides have been used to prepare benzisothiazole quinones and 1,2-benzisothiazole-5,6-dicarboxylates. The nitrile sulfides, generated by thermal decarboxylation of 1,3,4-oxathiazol-2-ones, reacted with 1,4-naphthoquinone to afford 3-substituted naphtho[2,3-d] isothiazole-4,9-diones (17), together with nitriles as by-products. The corresponding reactions with 1,4-benzoquinone yielded regioisomeric mixtures of 2:1 adducts. The 1,2-benzisothiazole-5,6-dicarboxylates were synthesised by a sequence involving both nitrile sulfide and Diels-Alder cycloaddition reactions. Dimethyl 3-phenylisothiazole-4,5-dicarboxylate (34), prepared from benzonitrile sulfide and dimethyl acetylenedicarboxylate (DMAD), was converted into the 4,5-bis(dibromomethyl) analogue 37 via the bis(dihydroxymethyl) compound 35. Treatment of 37 with sodium iodide in the presence of DMAD afforded dimethyl 3-phenyl-1,2-benzisothiazole-5,6-dicarboxylate (30) via the isothiazole o-quinodimethane 32. ARKAT-USA, Inc.
Synthesis and evaluation of furan, thiophene, and azole bis[(carbamoyloxy)methyl] derivatives as potential antineoplastic agents
Anderson,Jones
, p. 1559 - 1565 (2007/10/02)
A series of bis(hydroxymethyl)-substituted heterocycles were synthesized and converted to the corresponding bis(methylcarbamate) derivatives. The heterocyclic systems studied were based on 2-phenyl-3-methylfuran, 1-phenylpyrazole, 1-phenyl-5-methylpyrazole, 1-phenyl-5-methylthiopene, 1-phenyl-1,2,3-triazole, 3-phenylisoxazole, 3-phenylisothiazole, 2-phenylthiazole, and 2-phenyloxazole. None of the bis(carbamates) prepared was active against murine P388 lymphocytic leukemia. Pyrrole bis(carbamate), which exhibited antileukemic activity, also showed reactivity toward 4-(p-nitrobenzyl)pyridine while the inactive bis(carbamates) were unreactive in the 4-(p-nitrobenzyl)pyridine assay.
