- Preparation method of benzyl aryl ether and application of benzyl aryl ether in synthesis
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and, 6-dihydrodibenzo [11 - b] oxazepine e -11 - ketone compounds are synthesized through a one-step reaction of benzaldehyde compounds and phenolic compounds through one-step reaction. The benzyl aryl ether and 6 and 11 -dihydrodibenzo [b, e] oxazepine -11 - ketone compound respectively have a chemical structure formula shown in a formula I and II. The invention discloses a synthesis method of the compound. Benzaldehyde compound After completion of the reaction, I, 6-dihydrodibenzo [11 - b] oxazepine e ketone compound -11 - can be synthesized through an oxidation or hydrolysis step and a ring closing step after the reaction is complete II.
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Paragraph 0145-0150
(2021/09/01)
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- Synthesis, characterization, and biologic activity of new acyl hydrazides and 1,3,4-oxadiazole derivatives
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Starting from isoniazid and carboxylic acids as precursors, thirteen new hydrazides and 1,3,4-oxadiazoles of 2-(4-substituted-phenoxymethyl)-benzoic acids were synthesized and characterized by appropriate means. Their biological properties were evaluated in terms of apoptosis, cell cycle blocking, and drug metabolism gene expression on HCT-8 and HT-29 cell lines. In vitro antimicrobial tests were performed by the microplate Alamar Blue assay for the anti-mycobacterial activities and an adapted agar disk diffusion technique for other non-tubercular bacterial strains. The best antibacterial activity (anti-Mycobacterium tuberculosis effects) was proved by 9. Compounds 7, 8, and 9 determined blocking of G1 phase. Compound 7 proved to be toxic, inducing apoptosis in 54percent of cells after 72 h, an effect that can be predicted by the increased expression of mRNA caspases 3 and 7 after 24 h. The influence of compounds on gene expression of enzymes implicated in drug metabolism indicates that synthesized compounds could be metabolized via other pathways than NAT2, spanning adverse effects of isoniazid. Compound 9 had the best antibacterial activity, being used as a disinfectant agent. Compounds 7, 8, and 9, seemed to have antitumor potential. Further studies on the action mechanism of these compounds on the cell cycle may bring new information regarding their biological activity.
- Bleotu, Coralia,Diaconu, Carmen Cristina,Hanganu, Anamaria,Ionita, Petre,Limban, Carmen,Matei, Lilia,Nemes, Roxana Maria,Nicolau, Ioana,Nuta, Diana Camelia,P?un, Anca,Radulescu, Cristiana,Tatibou?t, Arnaud,Zarafu, Irina
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- Iron(II) promoted direct synthesis of dibenzo[b,e]oxepin-11(6H)-one derivatives with biological activity. A short synthesis of doxepin
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A novel and efficient synthesis of dibenzo[b,e]oxepin-11(6H)-ones by direct intramolecular ortho-acylation from readily available 2-(phenoxymethyl)benzoic acids was developed. The method takes advantage of a newly developed cooperative system consisting of sustainable FeCl2 and Cl2CHOCH3 as the key components. This methodology is compatible with a wide variety of functional groups in good to excellent yields and high regioselectivity. The synthetic application of new protocol was extended to the synthesis of known tricyclic drug doxepin as well as a small library of oxepin based derivatives. For the first time, the obtained dibenzo[b,e]oxepinone derivatives were evaluated for their biological activities on the free-living nematode Caenorhabditis elegans as an effective and cost-efficient model system for anthelmintic discovery.
- Scoccia, Jimena,Castro, M. Julia,Faraoni, M. Belén,Bouzat, Cecilia,Martín, Víctor S.,Gerbino, Darío C.
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supporting information
p. 2913 - 2922
(2017/04/26)
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- Synthesis, structural characterization and microbiological assays of some new 2-methoxy-O-acyl-oximino-dibenz[b,e] oxepins
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The paper reports on the synthesis of some new 2-methoxy-O-acyl-oximino- dibenz[b,e]oxepins. The new compounds and the intermediary substances were characterized by spectroscopic data and elemental analyses. Their antibacterial activities were investigate
- Limban, Carmen,Missir, Alexandru-Vasile,Chirita, Ileana Cornelia,Guta, Rodica,Nanau-Andreescu, Doina,Nitulescu, George Mihai,Draghici, Constantin,Caproiu, Miron T.,Delcaru, Cristina,Chifiriuc, Mariana Carmen
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experimental part
p. 313 - 319
(2011/04/27)
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- New thioureides of 2-(4-methyl-phenoxymethyl)-benzoic and 2-(4-methoxy-phenoxymethyl)-benzoic acids with biological activity
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The present application is a continuation of our research concerning the synthesis and characterization of thioureides of 2-(4-methyl-phenoxymethyl)- benzoic acid and 2-(4-methoxy-phenoxymethyl)-benzoic acid with biological activities. The new compounds,
- Limban, Carmen,Missir, Alexandru-Vasile,Chirita, Ileana Cornelia,Badiceanu, Carmellina Daniela,Draghici, Constantin,Balotescu, Mariana Carmen,Stamatoiu, Oana
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experimental part
p. 595 - 602
(2010/02/16)
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- 4-Aminoquinolines: Novel nociceptin antagonists with analgesic activity
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Small-molecule nociceptin antagonists were synthesized to examine their therapeutic potential. After a 4-aminoquinoline derivative was found to bind with the human ORL1 receptor, a series of 4-aminoquinolines and related compounds were synthesized and their binding was evaluated. Elucidation of structure - Activity relationships eventually led to the optimum compounds. One of these compounds, N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide hydrochloride (11) not only antagonized nociceptin-induced allodynia in mice but also showed analgesic effect in a hot plate test using mice and in a formalin test using rats. Its analgesic effect was not antagonized by the opioid antagonist naloxone. These results indicate that this nociceptin antagonist has the potential to become a novel type of analgesic that differs from μ-opioid agonists.
- Shinkai,Ito,Iida,Kitao,Yamada,Uchida
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p. 4667 - 4677
(2007/10/03)
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- Synthesis and biological activity of 11-[4-(cinnamyl)-1-piperazinyl]-6,11-dihydrodibenz[b,e]oxepin derivatives, potential agents for the treatment of cerebrovascular disorders
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A series of 11-[4-(cinnamyl)-1-piperazinyl]-6,11-dihydrodibenz[b,e]oxepins and related compounds were synthesized and evaluated for their protective activities against complete ischemia, normobaric hypoxia, lipidperoxidation and convulsion. Structure-activity relationship studies of this series led to the finding of (E)-1-(3-fluoro-6,11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-prop enyl)piperazine dimaleate (50), AJ-3941 with the most appropriate property for combined pharmacological activities. Compound 50 also shows an inhibitory effect against cerebral edema as well when orally given to rats.
- Kurokawa,Sato,Masuda,Yoshida,Ochi,Zushi,Fujiwara,Naruto,Uno,Matsumoto
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p. 2564 - 2573
(2007/10/02)
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