15062-88-1Relevant academic research and scientific papers
N1-Hetaryl substituted pyridine- and pyrazinecarboxamidrazones with antimycobacterial activity.
Ranft,Lehwark-Yvetot,Schaper,Buege
, p. 169 - 172 (1997)
A series of amidrazones was prepared and characterized by 1H NMR and mass spectroscopy. The substances were tested against M. tuberculosis, M. avium, M. intracellulare, and M. lufu. Compounds 11-13 exhibit a satisfactory inhibition of mycobacteria.
CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Paragraph 1179, (2018/04/17)
Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
Design and synthesis of prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer drugs
Nakao, Syuhei,Mabuchi, Miyuki,Shimizu, Tadashi,Itoh, Yoshihiro,Takeuchi, Yuko,Ueda, Masahiro,Mizuno, Hiroaki,Shigi, Naoko,Ohshio, Ikumi,Jinguji, Kentaro,Ueda, Yuko,Yamamoto, Masatatsu,Furukawa, Tatsuhiko,Aoki, Shunji,Tsujikawa, Kazutake,Tanaka, Akito
supporting information, p. 1071 - 1074 (2014/03/21)
A series of 1-aryl-3,4-substituted-1H-pyrazol-5-ol derivatives was synthesized and evaluated as prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors to obtain a novel anti-prostate cancer drug. After modifying 1-(1H-benzimidazol-2-yl)-3,4-dimethyl-1H-pyrazol-5-ol (1), a hit compound found during random screening using a recombinant PCA-1/ALKBH3, 1-(1H-5- methylbenzimidazol-2-yl)-4-benzyl-3-methyl-1H-pyrazol-5-ol (35, HUHS015), was obtained as a potent PCA-1/ALKBH3 inhibitor both in vitro and in vivo. The bioavailability (BA) of 35 was 7.2% in rats after oral administration. As expected, continuously administering 35 significantly suppressed the growth of DU145 cells, which are human hormone-independent prostate cancer cells, in a mouse xenograft model without untoward effects.
POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, AND OPTICALLY ANISOTROPIC MATERIAL
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Paragraph 0181, (2014/03/25)
The present invention relates to a polymerizable compound represented by a formula (I). The present invention provides a polymerizable compound, a polymerizable composition, a polymer, and an optically anisotropic article that are capable of obtaining an
INTERMEDIATE FOR MANUFACTURE OF POLYMERIZABLE COMPOUND AND PROCESS FOR MANUFACTURE THEREOF
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Paragraph 0087; 0088, (2014/08/19)
The present invention pertains to a compound represented by a formula (I) and a method for producing thereof (in the formula, Ax is an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, Ay is a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a cycloalkyl group, an alkenyl group having 2 to 18 carbon atoms, an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, or the like. Ax and Ay optionally bond to each other to form a ring, and Q is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like.). Accordinng to the invention, provided are a novel compound that makes it possible to produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band can be inexpensively produced in high yield by utilizing the compound according to one aspect of the invention as an intermediate for producing the polymerizable compound, and a method for producing thereof.
Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL
Sleebs, Brad E.,Kersten, Wilhemus J. A.,Kulasegaram, Sanji,Nikolakopoulos, George,Hatzis, Effie,Moss, Rebecca M.,Parisot, John P.,Yang, Hong,Czabotar, Peter E.,Fairlie, W. Douglas,Lee, Erinna F.,Adams, Jerry M.,Chen, Lin,Van Delft, Mark F.,Lowes, Kym N.,Wei, Andrew,Huang, David C.S.,Colman, Peter M.,Street, Ian P.,Baell, Jonathan B.,Watson, Keith,Lessene, Guillaume
, p. 5514 - 5540 (2013/07/26)
Developing potent molecules that inhibit Bcl-2 family mediated apoptosis affords opportunities to treat cancers via reactivation of the cell death machinery. We describe the hit-to-lead development of selective Bcl-X L inhibitors originating from a high-throughput screening campaign. Small structural changes to the hit compound increased binding affinity more than 300-fold (to IC50 w L. Surface plasmon resonance experiments afford strong evidence of binding affinity within the hydrophobic groove of Bcl-XL. Biological experiments using engineered Mcl-1 deficient mouse embryonic fibroblasts (MEFs, reliant only on Bcl-XL for survival) and Bax/Bak deficient MEFs (insensitive to selective activation of Bcl-2-driven apoptosis) support a mechanism-based induction of apoptosis. This manuscript describes the first series of selective small-molecule inhibitors of Bcl-XL and provides promising leads for the development of efficacious therapeutics against solid tumors and chemoresistant cancer cell lines.
Asymmetric allylation, crotylation, and cinnamylation of N-heteroaryl hydrazones
Feske, Miriam Inbar,Santanilla, Alexander Buitrago,Leighton, James L.
supporting information; experimental part, p. 688 - 691 (2010/04/02)
(Chemical Equation Presented) A new class of N-heteroaryl hydrazones has been developed as an alternative to N-acylhydrazones and 2-amlnophenol-derlved lmlnes In asymmetric allylatlon, crotylatlon, and clnnamylatlon reactions with chlral allylchlorosllanes. The hydrazones are readily and Inexpensively prepared, perform well In the allylatlon chemistry, and more Importantly, the product hydrazldes may be smoothly reduced by Pd(OH)2catalyzed hydrogenation to reveal the corresponding amine products.
Synthesis of complexes of 2-(benzooxazolyl-2-aminoimino)1,2-diphenylethanone with some bivalent transition metal ions
Dash,Mahapatra,Jena,Patjoshi
, p. 339 - 341 (2007/10/03)
A series of metal complexes having composition [M(BOAIDE)(H 2O)3]Cl and [M(BOAIDE)L3]Cl, where HBOAIDE is a Schiff base ligand, derived from 2-hydrazinobenzooxazole and benzil, M = CoII, CuII, NiII, and L = pyridine or picoline(α,β,γ) have been synthesized. The ligand acts as a monobasic tridentate donor, coordinating through azomethine nitrogen, ring oxygen atom and oxygen atom of benzil after deprotonation via tautomerization. The electronic spectra indicate the complexes to be in an approximately octahedral environment, the symmetry being Oh for the Co 11 and D4h for others. Various crystal field parameters for the Co11 and distortion parameters for the Ni11 complexes on the basis of proposed geometry have been calculated.
Synthesis of N-(thio)phosphoryl-N′-2-benzoxazolyl semicarbazides
Chen, Wen-Bin,Jin, Gui-Yu
, p. 151 - 155 (2007/10/03)
We prepared the benzoxazole derivatives bearing the (thio) phosphoryl moiety by addition reactions of 2-hydrazionbenzoxazole with isothiocyanato (thio) phosphates and characterized their structures by elementary analysis and 1H NMR and IR spectral data. From the results of biological activity screening, we found that these compounds possess some herbicidal, and plant growth regulator activities, and especially good fungicidal activity against Puccinia recondita.
Synthesis and antimicrobial activities of 2-[(α-Methylbenzylidene)hydrazino] benzoxazoles
Ersan, Seyhan,Nacak, Sultan,Berkem, Rukiye,Oezden, Tuncel
, p. 963 - 965 (2007/10/03)
New 2-[(α-methylbenzylidene)hydrazino]benzoxazole derivatives have been synthesized by reacting ortho or para substituted acetophenones with 2-hydrazinobenzoxazole in ethanol. The structures of the synthesized compounds were confirmed by microanalysis, IR
