26518-71-8Relevant academic research and scientific papers
Synthesis of 6-cinnamoyl-2H-benzo[b][1,4]oxazin-3(4H)-ones and their effects on A549 lung cancer cell growth
Zhou, Xue-Wen,Ma, Han-Lin,Zhang, Xuan,Jing, Shi-Yao,Miao, Jun-Ying,Zhao, Bao-Xiang
, p. 95 - 101 (2014/05/06)
A series of novel 6-cinnamoyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives was synthesized. The structures of compounds were characterized by 1H NMR, IR, and MS. Moreover, representative crystal structure was determined by X-ray diffraction ana
Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose) polymerase inhibitors
Gangloff, Anthony R.,Brown, Jason,De Jong, Ron,Dougan, Douglas R.,Grimshaw, Charles E.,Hixon, Mark,Jennings, Andy,Kamran, Ruhi,Kiryanov, Andre,O'Connell, Shawn,Taylor, Ewan,Vu, Phong
supporting information, p. 4501 - 4505 (2013/08/15)
Structure based drug design of a series of novel 1,4-benzoxazin-3-one derived PARP-1 inhibitors are described. The synthesis, enzymatic & cellular activities and pharmacodynamic effects are described. Optimized analogs demonstrated inhibition of poly-ADP-ribosylation in SW620 tumor bearing nude mice through 24 h following a single dose.
Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists
Hasui, Tomoaki,Ohra, Taiichi,Ohyabu, Norio,Asano, Kouhei,Matsui, Hideki,Mizukami, Atsushi,Habuka, Noriyuki,Sogabe, Satoshi,Endo, Satoshi,Siedem, Christopher S.,Tang, Tony P.,Gauthier, Cassandra,De Meese, Lisa A.,Boyd, Steven A.,Fukumoto, Shoji
, p. 5983 - 5994 (2013/09/23)
Dihydrofuran-2-one and dihydropyrrol-2-one derivatives were identified as novel, potent and selective mineralocorticoid receptor (MR) antagonists by the structure-based drug design approach utilizing the crystal structure of MR/compound complex. Introduct
Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors
Geng, Bolin,Comita-Prevoir, Janelle,Eyermann, Charles J.,Reck, Folkert,Fisher, Stewart
scheme or table, p. 5432 - 5435 (2011/10/12)
An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron donating groups (EDG) and electron withdrawing groups (EWG) are tolerated for antibacterial activity. Cyano was identified as a preferred substituent that affords good antibacterial potency while minimizing hERG cardiac channel activity.
POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS
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Page/Page column 80, (2010/11/04)
Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds,
COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS
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Page/Page column 101, (2010/11/25)
The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
