- Imidazole hydrochloride promoted synthesis of 3,5-disubstituted-1,2,4-oxadiazoles
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Imidazole hydrochloride as an additive promotes the reaction of amidoximes and DMA derivatives to generated 3,5-disubstituted-1,2,4-oxadiazoles in low to excellent yields without the use of coupling reagents, oxidants, strong acids or bases and other additives.
- Wang, Xuetong,Wang, Yin,Liu, Xiaoling,He, Tingshu,Li, Lingli,Wu, Huili,Zhou, Shangjun,Li, Dan,Liao, Siwei,Xu, Ping,Huang, Xing,Yuan, Jianyong
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supporting information
(2021/10/14)
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- Synergism of a novel 1,2,4-oxadiazole-containing derivative with oxacillin against methicillin-resistant staphylococcus aureus
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Staphylococcus aureus is an important opportunistic pathogen that causes many infections in humans and animals. The inappropriate use of antibiotics has favored the diffusion of methicillin-resistant S. aureus (MRSA), nullifying the efforts undertaken in
- Buommino, Elisabetta,D’auria, Maria Valeria,De Marino, Simona,Festa, Carmen,Piccolo, Marialuisa,Sciarretta, Martina
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- The Preparation Method of UV absorber intermediates
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The present invention relates to a method for preparing 2-hydroxybenzamidine. According to the present invention, 2-hydroxybenzonitrile is reacted with NH_2OH to prepare a 2-hydroxybenzamide oxime, and 2-hydroxybenzamide oxime is reacted with ammonium chl
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Paragraph 0028-0030
(2018/05/03)
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- Compound and application of compound in preparation of medicines
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The invention discloses a compound and its application in a medicine. the invention specifically provides a compound as shown in the formula (I) or a stereisomer, a geometrical isomer, a tautomer, a racemate, nitric oxide, hydrate, a solvate, a metabolite, pharmaceutically acceptable salts or a prodrug of the compound as shown in the formula (I). The invention also discloses an application of the compound in preparation of a medicine. The medicine is used in treating cancers.
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Paragraph 0173; 0174; 0292
(2016/10/08)
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- Practical synthesis of N -substituted cyanamides via tiemann rearrangement of amidoximes
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A facile and general synthesis of various N-substituted cyanamides was accomplished by the Tiemann rearrangement of amidoximes with benzenesulfonyl chlorides (TsCl or o-NsCl) and DIPEA.
- Lin, Chia-Chi,Hsieh, Tsung-Han,Liao, Pen-Yuan,Liao, Zhen-Yuan,Chang, Chih-Wei,Shih, Yu-Chiao,Yeh, Wen-Hsiung,Chien, Tun-Cheng
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supporting information
p. 892 - 895
(2014/03/21)
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- Benzohydroxamic acids as potent and selective anti-HCV agents
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A diverse collection of 40 derivatives of benzohydroxamic acid (BHAs) of various structural groups were synthesized and tested against hepatitis C virus (HCV) in full-genome replicon assay. Some of these compounds demonstrated an exceptional activity, suppressing viral replication at sub-micromolar concentrations. The compounds were inactive against key viral enzymes NS3, and NS5B in vitro assays, suggesting host cell inhibition target(s). The testing results were consistent with metal coordination by the BHAs hydroxamic group in complex with a target(s). Remarkably, this class of compounds did not suppress poliomyelitis virus (PV) propagation in RD cells indicating a specific antiviral activity of BHAs against HCV.
- Kozlov, Maxim V.,Kleymenova, Alla A.,Romanova, Lyudmila I.,Konduktorov, Konstantin A.,Smirnova, Olga A.,Prasolov, Vladimir S.,Kochetkov, Sergey N.
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supporting information
p. 5936 - 5940
(2013/10/22)
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- A HTS assay for the detection of organophosphorus nerve agent scavengers
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A new pro-fluorescent probe aimed at a HTS assay of scavengers is able to selectively and efficiently cleave the P-S bond of organophosphorus nerve agents and by this provides non-toxic phosphonic acid has been designed and synthesised. The previously described pro-fluorescent probes were based on a conventional activated P-Oaryl bond cleavage, whereas our approach uses a self-immolative linker strategy that allows the detection of phosphonothioase activity with respect to a non-activated P-Salkyl bond. Further, we have also developed and optimised a high-throughput screening assay for the selection of decontaminants (chemical or biochemical scavengers) that could efficiently hydrolyse highly toxic V-type nerve agents. A preliminary screening, realised on a small α-nucleophile library, allowed us to identify some preliminary "hits", among which pyridinealdoximes, α-oxo oximes, hydroxamic acids and, less active but more original, amidoximes were the most promising. Their selective phosphonothioase activity has been further confirmed by using PhX as the substrate, and thus they offer new perspectives for the synthesis of more potent V nerve agent scavengers.
- Louise-Leriche, Ludivine,Paunescu, Emilia,Saint-Andre, Geraldine,Baati, Rachid,Romieu, Anthony,Wagner, Alain,Renard, Pierre-Yves
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experimental part
p. 3510 - 3523
(2010/07/06)
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- Design and synthesis of 3-aryl-5-alicylic-[1,2,4]-oxadiazoles as novel platelet aggregation inhibitors
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A series of 4-[2-(alicyclic-[1,2,4]oxadiazol-3-yl)phenoxy]-butyric acids were synthesized from N-hydroxy-2-isopropoxy benzamidine in 4 steps with good yields. These [1,2,4]oxadiazoles are novel platelet aggregation inhibitors preventing human platelet agg
- Chern, Ching-Yuh,Chen, Shinn-Jyh,Kan, Wai-Ming
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p. 331 - 338
(2007/10/03)
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- Isoxazolylbenzamides as insecticides
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The present invention is directed to isoxazolyl and benzisoxazolyl benzamide compounds useful as insecticides.
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- 1-Benzoyl-3-(isoxazolyl or benzisoxazolyl)-ureas and insecticidal use thereof
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The present invention is directed to 1-(benzoyl)-3-(isoxazolyl or benzisoxazolyl)urea or thiourea compounds useful as insecticides.
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