- List fluoro Radicamine compounds and their use and preparation method
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The invention discloses a mono-fluorinated Radicamine compound which has a structure as shown in a formula (1), and further provides a preparation method for the mono-fluorinated Radicamine compound with the structure as shown in the formula (1) and an application of the mono-fluorinated Radicamine compound or the mono-fluorinated Radicamine compound prepared with the method to preparation of drugs for preventing and/or treating diabetes, drugs for preventing and/or treating Gaucher's diseases, drugs for preventing and/or treating tumors or antiviral drugs. The mono-fluorinated Radicamine compound provided by the invention is good in glycosidase inhibition activity.
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Paragraph 0086-0088
(2017/12/02)
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- Discovery of New 2-[(4,6-Dimethoxy-1,3,5-triazin-2-yl)oxy]-6-(substituted phenoxy)benzoic Acids as Flexible Inhibitors of Arabidopsis thaliana Acetohydroxyacid Synthase and Its P197L Mutant
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In the search for new antiresistance acetohydroxyacid synthase (AHAS, EC 2.2.1.6) inhibitors to combat weed resistance associated with AHAS mutations, a series of 2-[(4,6-dimethoxy-1,3,5-triazin-2-yl)oxy]-6-(substituted phenoxy)benzoic acids 11-38 were de
- Qu, Ren-Yu,Yang, Jing-Fang,Devendar, Ponnam,Kang, Wei-Ming,Liu, Yu-Chao,Chen, Qiong,Niu, Cong-Wei,Xi, Zhen,Yang, Guang-Fu
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p. 11170 - 11178
(2018/01/10)
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- Fluorinated Radicamine A and B: Synthesis and Glycosidase Inhibition
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Fluorinated derivatives of radicamine A and radicamine B have been synthesized from D-arabinose-derived cyclic nitrone. Structure-activity relationship studies showed that glycosidase inhibition of these fluorinated derivatives was significantly influenced by the position of the fluorine atom. C-7 or C-11 fluorination of the aromatic ring decreased α-glucosidase inhibition of the derivatives, whereas C-8 or C-10 fluorination preserved glycosidase inhibitory activities. Fluorinated derivatives of radicamine A and B have been synthesized from D-arabinose-derived cyclic nitrone. Structure-activity relationship studies revealed that glycosidase inhibition of these fluorinated derivatives was significantly influenced by the position of the fluorine atom.
- Li, Yi-Xian,Iwaki, Ren,Kato, Atsushi,Jia, Yue-Mei,Fleet, George W. J.,Zhao, Xuan,Xiao, Min,Yu, Chu-Yi
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p. 1429 - 1438
(2016/03/16)
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- The Key Role of the Nonchelating Conformation of the Benzylidene Ligand on the Formation and Initiation of Hoveyda-Grubbs Metathesis Catalysts
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Experimental studies of Hoveyda-Grubbs metathesis catalysts reveal important consequences of substitution at the 6-position of the chelating benzylidene ligand. The structural modification varies conformational preferences of the ligand that affects its exchange due to the interaction of the coordinating site with the ruthenium center. As a consequence, when typical S-chelated systems are formed as kinetic trans-Cl2 products, for 6-substituted benzylidenes the preference is altered toward direct formation of thermodynamic cis-Cl2 isomers. Activity data and reactions with tricyclohexylphosphine (PCy3) support also a similar scenario for O-chelated complexes, which display fast trans-Cl2?cis-Cl2 equilibrium observed by NMR EXSY studies. The presented conformational model reveals that catalysts, which cannot adopt the optimal nonchelating conformation of benzylidene ligand, initiate through a high-energy associative mechanism.
- Bieszczad, Bartosz,Barbasiewicz, Micha?
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supporting information
p. 10322 - 10325
(2015/07/07)
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- MULTIPLE KINASE PATHWAY INHIBITORS
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Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.
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- Regioselective formylation of 1,3-disubstituted benzenes through in situ lithiation
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A facile method of regioselective formylation of disubstituted benzene via in situ deprotonation/metalation using n-BuLi/TMEDA/DIPA has been developed. Effect of different electron withdrawing and electron donating substituents in 1,3-interrelated aromatic system was studied; the metalation mostly occurred at the 2-position to afford the desired products in high yields.
- Wang, Le,Wang, Yan,Guo, Fangxu,Zheng, Yue,Bhadury, Pinaki S.,Sun, Zhihua
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supporting information
p. 6053 - 6056
(2013/10/22)
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- NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
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The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
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Page/Page column 100
(2012/12/13)
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- NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
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The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
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Page/Page column 100; 101
(2012/11/14)
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- 4-Substituted (benzo[b]thiophene-2-carbonyl)guanidines as novel Na +/H+ exchanger isoform-1 (NHE-1) inhibitors
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A series of 4-substituted (benzo[b]thiophene-2-carbonyl)guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardioprotective efficacy both in vitro and in vivo. Several analogs exhibited a strong inhibition on NHE-1, and which was generally well correlated with their cardioprotective efficacy. Especially the 4-nitro 20 and cyano 50 compounds excellently improved the cardiac function and reduced infarct size against ischemia/reperfusion injury.
- Lee, Sunkyung,Lee, Hyunsuk,Kyu, Yang Yi,Byung, Ho Lee,Yoo, Sung-Eun,Lee, Kyunghee,Nam, Sook Cho
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p. 2998 - 3001
(2007/10/03)
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- Pyrazolopyrimidines as therapeutic agents
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The present invention is directed to pyrazolopyrimidine derivatives of formula (I) wherein the substituents are defined herein, which are useful as kinase inhibitors and as such are useful for affecting angiogenesis and diseases and conditions associated with angiogenesis.
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- Pyrazolopyrimidines as therapeutic agents
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The present invention provides compounds of Formula I, including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R2, and R3 are defined as described herein.
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- Total synthesis of the ansamycin antibiotic (+)-thiazinotrienomycin E
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The first total synthesis of (+)-thiazinotrienomycin E (1), member of a novel class of cytotoxic ansamycin antibiotics, has been achieved. Key features of the synthetic strategy include (a) the efficient construction of sulfone 7 incorporating TBS protection of the aniline, (b) an improved synthesis of allyl chloride (-)-6, the advanced intermediate employed in our trienomycins A and F total syntheses, (c) application of the Kocienski modified Julia protocol to elaborate the E,E,E-triene subunit in a stereo- controlled fashion, (d) an efficient union of sulfone 7 with advanced iodide 62, and (e) Mukaiyama macrolactamization to access the thiazinotrienomycin macrocyclic ring.
- Smith III, Amos B.,Wan, Zehong
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p. 3738 - 3753
(2007/10/03)
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- Total synthesis of (+)-thiazinotrienomycin E
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(equation presented) The first total synthesis of (+)-thiazinotrienomycin E (1), member of a novel class of cytotoxic ansamycin antibiotics, has been achieved. The synthesis features a highly efficient construction of the aromatic fragment 3 incorporating
- Smith III, Amos B.,Wan, Zehong
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p. 1491 - 1494
(2008/02/09)
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- Heterocyclcarboxamide derivatives and their use as therapeutic agents
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Compounds of formula I STR1 and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q
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- Fluorine as an ortho-directing group in aromatic metalation: A two step preparation of substituted benzo[b] thiophene-2-carboxylates
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A simple 2-step synthesis of B-ring substituted benzo[b]thiophene-2-carboxylates from aryl fluorides has been developed. The route involves a selective lithiation ortho to fluorine, followed by formylation, and subsequently, displacement of fluorine with
- Bridges, Alexander J.,Lee, Arthur,Maduakor, Emmanuel C.,Eric Schwartz
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p. 7499 - 7502
(2007/10/02)
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- Ring-Substituted y1,2-Bis(4-hydroxyphenyl)ethylenediamine>dichloroplatinum(II) Complexes: Compounds with a Selective Effect on the Hormone-Dependent Mammary Carcinoma
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dichloroplatinum(II) complexes with one substituent in the 2-position (CH3, CF3, F, Br, I: meso- and dl-1-PtCl2, meso-(3-5)-PtCl2, meso-(7 and 8)-PtCl2) or two substituents in the 2,6-position (CH3, Cl: meso-2-PtCl2, meso- and dl-6-PtCl2) in both benzene rings were synthesized and tested for estrogenic and toxic activities.Two complexes (meso-6-PtCl2 and meso-7-PtCl2) possess both effects.In comparative tests on estrogen receptor positive and negative mammary tumors in cell culture (MCF 7, ER+ and MDA-MB 231, ER-) and in animals (MXT, ER+ and MXT, ER-, mouse), meso-6-PtCl2 shows a selective effect on the estrogen receptor positive mammary carcinoma.A further increase of efficacy was achieved with the water-soluble (sulfato)platinum(II) derivative (meso-6-PtSO4).On the DMBA-induced hormone dependent mammary carcinoma of the SD rat, meso-6-PtSO4 is significantly more active than its ligand (meso-6) and cisplatin.
- Karl, Johann,Gust, Ronald,Spruss, Thilo,Schneider, Martin R.,Schoenenberg, Helmut,et al.
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