129053-83-4Relevant articles and documents
Synthesis and antibacterial evaluation of (E)-1-(1H-indol-3-yl) ethanone O-benzyl oxime derivatives against MRSA and VRSA strains
Akunuri, Ravikumar,Veerareddy, Vaishnavi,Kaul, Grace,Akhir, Abdul,Unnissa, Tanveer,Parupalli, Ramulu,Madhavi,Chopra, Sidharth,Nanduri, Srinivas
supporting information, (2021/08/27)
Infections caused due to multidrug resistant organisms have emerged as a constant menace to human health. Even though numerous antibiotics are currently available for treating infectious diseases, a great number of bacterial strains have acquired resistance to many of them. Among these, infections caused due to Staphylococcus aureus are predominant in adult and paediatric population. Indole is a prominent chemical scaffold found in many pharmacologically active natural products and synthetic drugs. A number of oxime ether containing compounds have attracted attention of researchers owing to their interesting biological properties. Current work details the synthesis of indole containing oxime ether derivatives and their evaluation for antimicrobial activity against a panel of bacterial and mycobacterial strains. Synthesized compounds demonstrated good to moderate activity against drug-resistant S. aureus including resistant to vancomycin. Among all, compound 5h was found to possess potent activity against susceptible as well as MRSA and VRSA strains of S. aureus with MIC of 1 μg/mL and 2–4 μg/mL respectively. In addition, compound 5h was found to be non-toxic to Vero cells and exhibited good selectivity index of >40. Further, 5h, E-9a and E-9b possessed good biofilm inhibition against S. aureus. With these assuring biological properties, synthesized compounds could be potential prospective antimicrobial agents.
Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine
White, Alex W.,Carpenter, Nicholas,Lottin, Jerome R. P.,McClelland, Richard A.,Nicholson, Robert I.
, p. 246 - 253,8 (2012/12/11)
The tetrahydroazepinone pharmacophore is a component of many interesting compounds, including several marine natural products, with anti-cancer properties. The synthesis and biological evaluation of a novel series of pyrroloazepinone and indoloazepinone oximes is reported. These compounds showed promising growth inhibition activity against four human cancer cell lines but did not significantly inhibit the cell cycle regulator cyclin dependent kinase 2. The most active compounds in this series displayed improved anti-proliferative activity over the related synthetic indoloazepine kenpaullone. The structure activity relationships exhibited by the azepinone pharmacophore suggests several novel lead compounds for anti-cancer drug discovery.
Pyrrolo[2,3-c]azepine derivatives: A new class of potent protein tyrosine phosphatase 1B inhibitors
Xie, Jianwei,Tian, Jinying,Su, Li,Huang, Manna,Zhu, Xinhai,Ye, Fei,Wan, Yiqian
supporting information; scheme or table, p. 4306 - 4309 (2011/08/10)
A series of pyrrolo[2,3-c]azepine derivatives was designed, synthesized, and evaluated as a new class of inhibitors against protein tyrosine phosphatase 1B (PTP1B) in vitro. The results demonstrated that compounds bearing a biphenyl moiety were proved to
Stereoselective synthesis of (Z)-axino- and (Z)-debromoaxinohydantoin
Tutino, Federico,Posteri, Helena,Borghi, Daniela,Quartieri, Francesca,Mongelli, Nicola,Papeo, Gianluca
experimental part, p. 2372 - 2376 (2009/07/18)
(Z)-Axinohydantoin and (Z)-debromoaxinohydantoin, two pyrrole-imidazole alkaloids isolated from different marine sponges, possess moderate activities in inhibiting the progress of the cell cycle at different phases. A stereoselective synthesis of both nat
WNT SIGNALING INHIBITORS, AND METHODS FOR MAKING AND USING THEM
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Page/Page column 34-35, (2009/01/20)
The invention provides dBHD-based compositions and dBHD analog compositions, and pharmaceutical compositions comprising them, e.g., in the form of liposomes and nanoparticles comprising them, and methods of making and using them. In one embodiment, these dBHD analogs are used to inhibit a dysfunctional stem cell and/or a cancer (tumor) stem cell.
A new glycociamidine ring precursor: Syntheses of (Z)-hymenialdisine, (Z)-2-debromohymenialdisine, and (±)-endo-2-debromohymenialdisine
Papeo, Gianluca,Posteri, Helena,Borghi, Daniela,Varasi, Mario
, p. 5641 - 5644 (2007/10/03)
(Chemical Equation Presented) The synthesis of the C11H 5 marine sponge alkaloids, (Z)-hymenialdisine and (Z)-2-debromohymenialdisine, is described. A key step was the condensation between aldisine or its monobromo derivative and a n
An expeditious multigram preparation of the marine protein kinase inhibitor debromohymenialdisine
Portevin, Bernard,Golsteyn, Roy M.,Pierré, Alain,De Nanteuil, Guillaume
, p. 9263 - 9265 (2007/10/03)
A short synthesis of the protein kinase inhibitor debromohymenialdisine is described, which allowed the preparation of several grams of the desired compound.
Dihydroindol-7(6H)-ones and 6,7-Dihydropyrroloazepine-4,8(1H,5H)-dione
Kasum, Bruno,Prager, Rolf H.,Tsopelas, Chris
, p. 355 - 365 (2007/10/02)
3-Methylcyclohexenones may be converted into dihydroindol-7(6H)-ones by conversion of the epoxide into the 2-benzylamino-3-methylcyclohexenone, which reacts with dimethylformamide dimethyl acetal to give N-benzyldihydroindol-7(6H)-ones.The limitations of the process are discussed, as is the failure to convert the dihydroindol-7(6H)-ones into dihydropyrroloazepinediones by Beckmann or Schmidt rearrangements.An example of the latter compounds was made by a simple procedure from pyrrolecarboxylic acid.
