- Perovskite as Recyclable Photocatalyst for Annulation Reaction of N-Sulfonyl Ketimines
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A sustainable and cost-effective manner for the photocatalytic annulation reaction of N-sulfonyl ketimines with N-arylglycines to synthesize imidazolidine-fused sulfamidates (31 examples) by employing CsPbBr3 as a heterogeneous photocatalyst has been developed. The catalyst CsPbBr3 can be simply recovered from the reaction mixture and reused at least five times without an obvious reduction in its photocatalytic reactivity, exhibiting a high catalyst economic feature.
- Shi, Anzai,Sun, Kai,Chen, Xiaolan,Qu, Lingbo,Zhao, Yufen,Yu, Bing
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supporting information
p. 299 - 303
(2022/01/04)
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- Ethyl cellulose derived porous iron@N-doped carbon material for N–H carbene insertion reaction
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A newly developed, facile and sustainable strategy, in which zinc salt, melamine and ethyl cellulose are applied as pore-forming agent, nitrogen and carbon source respectively, has been disclosed for the synthesis of Fe/N-codoped carbon materials. This material exhibits excellent catalytic efficiency towards N–H carbene insertion reaction for the synthesis of unnatural amino acid derivatives. Fe/FeOx nanoparticles tranfer electrons to N-doped carbon owing to the Mott-Schottky Effect, which is beneficial to the formation of iron carbene intermediate. N-doping can offer more Lewis base sites, which promotes the proton transfer process. Fe/FeOx nanoparticles are coated with graphitic carbon, thereby avoiding the loss and deactivation of iron sites in this material. Therefore, this material can be reused at least four times without significant loss in activity.
- Lin, Yamei,Wang, Fei,Lu, Guo-Ping,Zhang, Xing
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- Visible-Light-Induced Oxidative α-Alkylation of Glycine Derivatives with Ethers under Metal-Free Conditions
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In this work, a visible-light-induced oxidative α-alkylation of glycine derivatives with ethers has been developed in the presence of catalytic Eosin Y. Under the blue light of a 3 W LED, a range of α-etherized glycine derivatives, including α-amino esters, α-amino ketones and α-amino amides, were achieved with good to excellent yields and functional group tolerance with tert-butyl hydroperoxide (TBHP) as oxidant at ambient temperature. The operationally easy procedure provides an economical, metal-free, and mild alternative for the synthesis of the α-etherized glycine derivatives.
- Song, Yang,Zhang, Hao,Guo, Jiabao,Shao, Yifei,Ding, Yuzhou,Zhu, Li,Yao, Xiaoquan
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p. 5914 - 5921
(2021/11/22)
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- Unnatural α-Amino Acid Synthesized through α-Alkylation of Glycine Derivatives by Diacyl Peroxides
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We have developed a protocol for catalyst- and additive-free α-alkylation reactions of glycine derivatives with diacyl peroxides, which proceed by a pathway involving addition of alkyl radicals to imine intermediates. The diacyl peroxide substrate acts as both alkylation agent and oxidizing agent, which means it is atom-economical. It was applied to various glycine derivatives, dipeptides, and a 3,4-dihydroquinoxalin-2(1H)-one derivative and could be carried out on a gram scale, indicating its utility for late-stage functionalization.
- Tian, Hao,Xu, Wentao,Liu, Yuxiu,Wang, Qingmin
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supporting information
p. 5005 - 5008
(2020/07/04)
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- 1,3,4-oxadiazole derivative, and preparation method and application thereof
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The invention provides a 1,3,4-oxadiazole derivative, and a preparation method and application thereof, and belongs to the field of tumor related pharmacology. According to the 1,3,4-oxadiazole derivative, the structure of the 1,3,4-oxadiazole derivative
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Paragraph 0026-0028
(2019/11/12)
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- FERROCHELATASE INHIBITORS AND METHODS OF USE
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The invention relates to a method of treatment of a patient with a ferrochelatase inhibitor, or a pharmaceutically acceptable salt thereof, or a derivative thereof. Also, the invention relates to a method of treatment of a patient with a ferrochelatase in
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Page/Page column 59
(2019/11/19)
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- Arylamino containing hydroxamic acids as potent urease inhibitors for the treatment of Helicobacter pylori infection
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A novel series of aniline-containing hydroxamic acids were designed, synthesized and evaluated as anti-virulence agents for the treatment of gastritis and gastric ulcer caused by Helicobacter pylori. In vitro enzyme-based screen together with in vivo assays and structure?activity relationship (SAR) studies led to the discovery of three potent urease inhibitors 3-(3,5-dichlorophenylamino)–N-hydroxypropanamide (3a), 3-(2-chlorophenylamino)–N-hydroxypropanamide (3d) and 3-(2,4-dichlorophenylamino)–N-hydroxypropanamide (3n). Compounds 3a, 3d and 3n showed excellent urease inhibition with IC50 values 0.043 ± 0.005, 0.055 ± 0.008 and 0.018 ± 0.002 μM, and significantly depressed gastritis developing at the dose of 32 mg/kg b. i.d with eradication rates of H. pylori reaching 92.3, 84.6 and 100%, respectively. Preliminary safety studies (acute toxicity in mice) disclosed that 3a, 3d and 3n was well-tolerated in KM mice with LD50s of 2982.8, 3349.4 and 3126.9 mg/kg, respectively. Collectively, the data obtained in this study indicate that 3a, 3d and 3n, in particular 3n, could considered as promising candidates for the potential treatment of H. pylori caused gastritis and gastric ulcer, and hence merit further studies.
- Liu, Qi,Shi, Wei-Kang,Ren, Shen-Zhen,Ni, Wei-Wei,Li, Wei-Yi,Chen, Hui-Min,Liu, Pei,Yuan, Jing,He, Xiao-Su,Liu, Jia-Jia,Cao, Peng,Yang, Pu-Zhen,Xiao, Zhu-Ping,Zhu, Hai-Liang
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p. 126 - 136
(2018/07/13)
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- Compound with kinase inhibition activity and its preparation method and use
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The invention discloses a compound shown in the general formula I or its pharmaceutically acceptable salt, enantiomer, diastereomer or raceme, and a preparation method and pharmacal use thereof. All groups are defined in the patent specification. The comp
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Paragraph 0250; 0251; 0252; 0253
(2017/08/02)
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- Stable radical cation salt initiated N-H insertion and related proton-transfer-delay three-component reaction
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The N-H insertion reaction forms the single addition product exclusively, and does not require slow addition of the diazo component. More importantly, we present the reaction of anilines with both diazoacetates and azodicarboxylates in the presence of catalytic amounts of triarylaminium salt giving the corresponding complex unsymmetrical aminals in high yields. This is the first example of stable radical cation salt promoted proton-transfer-delay three-component reaction.
- Huo, Congde,Xie, Haisheng,Yang, Caixia,Dong, Jie,Wang, Yajun
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p. 2179 - 2182
(2016/05/02)
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- Direct amide formation from N-arylglycine ethyl esters and carboxylic acids catalysed by phenylboronic acid
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The phenylboronic acid-catalysed reaction of an N-arylglycine ethyl ester with various carboxylic acids, including N-acyl-N-phenylglycines, directly affords an amide or a dipeptide in 13-73% yields.
- Huang, Wenhua,Sha, Wen-Bin
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p. 460 - 463
(2013/09/12)
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- Design, synthesis, structural characterization by IR, 1H, 13C, 15N, 2D-NMR, X-ray diffraction and evaluation of a new class of phenylaminoacetic acid benzylidene hydrazines as pfenr Inhibitors
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Recent studies have revealed that plasmodial enoyl-ACP reductase (pfENR, FabI), one of the crucial enzymes in the plasmodial type II fatty acid synthesis II (FAS II) pathway, is a promising target for liver stage malaria infections. Hence, pfENR inhibitors have the potential to be used as causal malarial prophylactic agents. In this study, we report the design, synthesis, structural characterization and evaluation of a new class of pfENR inhibitors. The search for inhibitors began with a virtual screen of the iResearch database by molecular docking. Hits obtained from the virtual screen were ranked according to their Glide score. One hit was selected as a lead and modified to improve its binding to pfENR; from this, a series of phenylamino acetic acid benzylidene hydrazides were designed and synthesized. These molecules were thoroughly characterized by IR, 1H, 13C, 15N, 2D-NMR (COSY, NOESY, 1H-13C, 1H-15N HSQC and HMBC), and X-ray diffraction. NMR studies revealed the existence of conformational/configurational isomers around the amide and imine functionalities. The major species in DMSO solution is the E, E form, which is in dynamic equilibrium with the Z, E isomer. In the solid state, the molecule has a completely extended conformation and forms helical structures that are stabilized by strong hydrogen bond interactions, forming a helical structure stabilized by N-H...O interactions, a feature unique to this class of compounds. Furthermore, detailed investigation of the NMR spectra indicated the presence of a minor impurity in most compounds. The structure of this impurity was deduced as an imidazoline-4-one derivative based on 1H-13C and 1H-15H HMBC spectra and was confirmed from the NOESY spectra. The molecules were screened for in vitro activity against recombinant pfENR enzyme by a spectrophotometric assay. Four molecules, viz. 17, 7, 10, and 12 were found to be active at 7, 8, 10, and 12?μm concentration, respectively, showing promising pfENR inhibitory potential. A classification model was derived based on a binary QSAR approach termed recursive partitioning (RP) to highlight structural characteristics that could be tuned to improve activity.
- Samal, Ramanuj P.,Khedkar, Vijay M.,Pissurlenkar, Raghuvir R. S.,Bwalya, Angela Gono,Tasdemir, Deniz,Joshi, Ramesh A.,Rajamohanan,Puranik, Vedavati G.,Coutinho, Evans C.
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p. 715 - 729
(2013/07/05)
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- Hydrazide compounds
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Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydra
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Page/Page column 11
(2010/11/27)
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- Angiotensin converting enzyme inhibitors: N-substituted monocyclic and bicyclic amino acid derivatives
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The synthesis of N-(3-mercaptopropionyl)-N-arylglycines (14a-x), -N-arylalanines (15a,b), -N-cycloalkylglycines (16a-k), and -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids (17a-d), -1,2,3,4-tetrahydroquinoline-2-carboxylic acids (18a-f), and -indoline-2-carboxylic acids (19a-k) is described. In vitro inhibition of angiotensin converting enzyme (ACE) is reported for each compound, and the structure-activity relationship for each series is discussed. The in vivo inhibition of ACE and antihypertensive effects of representative compounds from each series are discussed. The most potent compound, 19d, had an in vitro ACE IC50 of 2.6 x 10-9 M and lowered blood pressure in spontaneous hypertensive rats 85 mm at a dose of 10 mg/kg po.
- Stanton,Gruenfeld,Babiarz,Ackerman,Friedmann,Yuan,Macchia
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p. 1267 - 1277
(2007/10/02)
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