- Synthesis of [1,4]Thiazino[4,3- a]indol-10-one Derivatives through Radical Anti Aza-Michael Addition of 2′-Aminochalcones
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An efficient method for the synthesis of [1,4]thiazino[4,3-a]indole derivatives using sodium chlorodifluoroacetate (ClCF2CO2Na) and elemental sulfur as the difluoromethylthiolating reagent system has been developed. Three-component reactions of 2′-aminochalcones, sulfur, and ClCF2CO2Na under basic conditions using TEMPO as the oxidant afforded [1,4]thiazino[4,3-a]indol-10-ones containing a difluoromethyl thioether moiety in good yields. Four bonds including one C-N, two C-S, and one C-C bonds are selectively formed in the sequential transformation process.
- Zhang, Pingshun,Yang, Linjie,Chen, Wanzhi,Liu, Miaochang,Wu, Huayue
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p. 6094 - 6098
(2021/08/01)
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- 2-aryl-2,3-dihydro-4(1H)-quinolinone semicarbazone compound and application thereof
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The invention relates to the field of medicine technology, and a series of novel 2-aryl-2,3-dihydrogen-4(1H)-quinolinone semicarbazone derivatives (I) and pharmaceutically acceptable salts, solvates,optical isomers or polymorphs are designed and synthesized. The derivative (I) and its pharmaceutically acceptable salt, solvate, optical isomer or polymorph can be mixed as an active ingredient witha pharmaceutically acceptable carrier to prepare a pharmaceutical composition. A double dilution method is used for test of the antifungal activity of the derivative (I) and its pharmaceutically acceptable salt, solvate, optical isomer or polymorph, and the results show that the derivative has stronger killing effect on clinically common pathogenic fungi, and is expected to overcome the defects oflarge toxic and side effects, easy generation of drug resistance of azole antifungal medicines which are widely used clinically. The specific formula is shown in the description.
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Paragraph 0066; 0067; 0068; 0069; 0070
(2018/10/19)
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- Aza analogs of flavones as potential antimicrobial agents
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In search for the new antimicrobial agents owing to drug resistant bacteria and fungi, a series of rationally designed aza analogs of flavones has been designed and synthesized. The design of the analogs involved incorporation of quinolone nucleus within
- Sharma, Sahil,Thakur, Vikas,Ojha, Ritu,Budhiraja, Abhishek,Nepali, Kunal,Singh Bedi, Preet Mohinder
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p. 327 - 334
(2013/07/26)
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- Synthesis of azaisoflavones and their inhibitory activities of NO production in activated microglia
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A series of azaisoflavones were synthesized and their biological activities were evaluated for nitric oxide (NO) production and inducible NO synthase (iNOS) expression in BV-2 microglia cell lines. Among these compounds, compound 8d was the most potent with IC50 7.83 μM for inhibition of NO production. Also, compound 8d inhibited expression of iNOS in LPS-induced BV2 cells. This result suggests that compound 8d inhibited the production of NO by suppressing the expression of iNOS.
- Jin, Guo Hua,Ha, Sang Keun,Park, Hye Min,Kang, Bomi,Kim, Sun Yeou,Kim, Hee-Do,Ryu, Jae-Ha,Jeon, Raok
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supporting information; experimental part
p. 4092 - 4094
(2009/04/10)
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- Chalcone derivatives as precursors of 1,2,3,4-tetrahydro-4-quinolones
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2-Aryl-1,2,3,4-tetrahydro-4-quinolones were synthesised from 2′-amino-4-methoxychalcone and its 2′-benzenesulphonamido derivative by acid and base catalysis, respectively. The α,β-dibromo and α-bromo-β-methoxy derivatives of 2′-benzenesulphonamido-4-methoxydihydrochalcone cyclised to 2-aryl-3-bromo-1,2,3,4-tefrahydro-4-quinolones as did the corresponding α-bromochalcones. 2′-Amino-4-methoxychalcone formed a stable epoxide.
- Donnelly, John A.,Farrell, David F.
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p. 885 - 894
(2007/10/02)
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