302912-35-2Relevant articles and documents
Discovery of lead compounds targeting the bacterial sliding clamp using a fragment-based approach
Yin, Zhou,Whittell, Louise R.,Wang, Yao,Jergic, Slobodan,Liu, Michael,Harry, Elizabeth J.,Dixon, Nicholas E.,Beck, Jennifer L.,Kelso, Michael J.,Oakley, Aaron J.
supporting information, p. 2799 - 2806 (2014/04/17)
The bacterial sliding clamp (SC), also known as the DNA polymerase III β subunit, is an emerging antibacterial target that plays a central role in DNA replication, serving as a protein-protein interaction hub with a common binding pocket to recognize linear motifs in the partner proteins. Here, fragment-based screening using X-ray crystallography produced four hits bound in the linear-motif-binding pocket of the Escherichia coli SC. Compounds structurally related to the hits were identified that inhibited the E. coli SC and SC-mediated DNA replication in vitro. A tetrahydrocarbazole derivative emerged as a promising lead whose methyl and ethyl ester prodrug forms showed minimum inhibitory concentrations in the range of 21-43 μg/mL against representative Gram-negative and Gram-positive bacteria species. The work demonstrates the utility of a fragment-based approach for identifying bacterial sliding clamp inhibitors as lead compounds with broad-spectrum antibacterial activity.
Efficient synthesis of indoles using [3,3]-sigmatropic rearrangement of N-trifluoroacetyl enehydrazines
Miyata, Okiko,Takeda, Norihiko,Kimura, Yasuo,Takemoto, Yoshiji,Tohnai, Norimitsu,Miyata, Mikiji,Naito, Takeaki
, p. 3629 - 3647 (2007/10/03)
[3,3]-Sigmatropic rearrangement of N-trifluoroacetyl enehydrazines provides a novel method for the construction of indoles. N-Trifluoroacetyl enehydrazine having a cyclopentene ring smoothly underwent [3,3]-sigmatropic rearrangement followed by cyclizatio
Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application
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Page/Page column 19, (2010/02/05)
A chemical compound of formula (I) wherein: R1and R2are independently selected from hydrogen and alkyl; R3is alkyl; R4, R6and R7are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsufoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4to R7is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2Creceptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinial disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.
Fischer indole synthesis in the absence of a solvent
Matsumoto, Kiyoshi,Tanaka, Akinori,Yukio, Ikemi,Hayashi, Naoto,Toda, Mitsuo,Bulman, Robert A.
, p. 9 - 12 (2007/10/03)
The traditional Fischer synthesis of indoles has been investigated and it has been shown that the reaction proceeds in good yield in the absence of a solvent.
