22952-24-5Relevant articles and documents
Synthesis method of foramsulfuron intermediate
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Paragraph 0045-0048, (2021/01/04)
The invention discloses a synthesis method of a foramsulfuron intermediate, which comprises the following steps of: carrying out one-pot chlorination, alcoholysis and ammonolysis cyclization on 2-sulfo-4-nitrobenzoic acid used as a starting raw material t
Research on Controllable Degradation of Novel Sulfonylurea Herbicides in Acidic and Alkaline Soils
Zhou, Shaa,Hua, Xue-Wen,Wei, Wei,Gu, Yu-Cheng,Liu, Xiao-Qing,Chen, Jing-Huo,Chen, Ming-Gui,Xie, Yong-Tao,Zhou, Sha,Meng, Xiang-De,Zhang, Yan,Li, Yong-Hong,Wang, Bao-Lei,Song, Hai-Bin,Li, Zheng-Ming
, p. 7661 - 7668 (2017/09/15)
The degradation issue of sulfonylurea (SU) has become one of the biggest challenges that hamper the development and application of this class of herbicides, especially in the alkaline soils of northern China. On the basis of the previous discovery that some substituents on the fifth position of the benzene ring in Chlorsulfuron could hasten its degradation rate, apparently in acidic soil, this work on Metsulfuron-methyl showed more convincing results. Two novel compounds (I-1 and I-2) were designed and synthesized, and they still retained potent herbicidal activity in tests against both dicotyledons and monocotyledons. The half-lives of degradation (DT50) assay revealed that I-1 showed an accelerated degradation rate in acidic soil (pH 5.59). Moreover, we delighted to find that the degradation rate of I-1 was 9-10-fold faster than that of Metsulfuron-methyl and Chlorsulfuron when in alkaline soil (pH 8.46), which has more practical value. This research suggests that a modified structure that has potent herbicidal activity as well as accelerated degradation rate could be realized and this approach may provide a way to improve the residue problem of SUs in farmlands with alkaline soil.
A convenient synthesis of 2-methoxycarbonyl-5-iodobenzene sulfonamide
Cai, Xinhong,Chen, Qiulu,Guan, Jing,Gong, Shunze,Fu, Hao,Xu, Defeng
, p. 1622 - 1624 (2017/05/29)
A convenient and concise synthesis of 2-methyl-5-nitrobenzene sulfonamide can be achieved by sulfochlorination and ammoniation with p-nitrotoluene as raw materials for an 81.2 % yield. 6-Aminosaccharin can be produced via oxidation and reduction in a 64.3
In vitro inhibition effect and structure-activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase i and II
Sonmez, Fatih,Bilen, Cigdem,Sumersan, Sinem,Gencer, Nahit,Isik, Semra,Arslan, Oktay,Kucukislamoglu, Mustafa
, p. 118 - 123 (2014/03/21)
In this study, in vitro inhibitory effects of some saccharin derivatives on purified carbonic anhydrase I and II were investigated using CO2 as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among the compounds, 6-(p-tolylthiourenyl) saccharin (6m) was found to be the most active one for hCA I activity (IC50 = 13.67 μM) and 6-(m-methoxyphenylurenyl) saccharin (6b) was found to be the most active one for hCA II activity (IC50 = 6.54 μM). Structure-activity relationships (SARs) study showed that, generally, thiourea derivatives (6l - v) inhibited more hCA I and hCA II than urea derivatives (6a-k). All compounds (excluding 6c and 6r) have higher inhibitory activity on hCA II than on hCA I.
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors
Han, Leiqiang,Wang, Lei,Hou, Xuben,Fu, Huansheng,Song, Weiguo,Tang, Weiping,Fang, Hao
, p. 1529 - 1538 (2014/03/21)
Histone deacetylase (HDAC) is a clinically validated target for antitumor therapy. In order to increase HDAC inhibition and efficiency, we developed a novel series of saccharin hydroxamic acids as potent HDAC inhibitors. Among them, compounds 11e, 11m, 11
Cyclic secondary sulfonamides: Unusually good inhibitors of cancer-related carbonic anhydrase enzymes
Moeker, Janina,Peat, Thomas S.,Bornaghi, Laurent F.,Vullo, Daniela,Supuran, Claudiu T.,Poulsen, Sally-Ann
, p. 3522 - 3531 (2014/05/20)
Carbonic anhydrase IX (CA IX) is a target for hypoxic cancer therapies, and the discovery of CA IX selective ligands is imperative for the development of these agents. Primary sulfonamides are broad specificity inhibitors of CA enzymes, while secondary su
FURO[3,2-d]PYRIMIDINE COMPOUNDS
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, (2012/04/23)
The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
New saccharin derivatives as tyrosinase inhibitors
Gener, Nahit,Demir, Dudu,Sonmez, Fatih,Kucukislamoglu, Mustafa
experimental part, p. 2811 - 2821 (2012/06/29)
A newly series of 6-(phenylurenyl/thiourenyl) saccharin (6a-y) derivatives were synthesized and their inhibitory effects on the diphenolase activity of banana tyrosinase were evaluated. A 70-fold purification of the enzyme with 6.85% yield was achieved by using a Sepharose 4B-l-tyrosine-p-amino benzoic acid affinity column. The result showed that all the synthesized compounds inhibited the tyrosinase enzyme activity. Among the compounds synthesized, 6-(3-iodophenylthiourenyl) saccharin (6s) was found to be most active one (Ki = 3.95 μM) and the inhibition kinetics analyzed by Lineweaver-Burk double reciprocal plots revealed that compound 6s was a competitive inhibitor. Structure-activity relationships study showed that generally, most of the 6-(phenylthiourenyl) saccharin derivatives (6m-y) exhibited higher inhibitory activity than 6-(phenylurenyl) saccharin derivatives (6a-l). An electron-withdrawing group at 3-position of phenylurenyl-ring increased in activity and the halogen series at 3-position of phenylthiourenyl-ring showed a qualitative relationship for higher inhibitory activity with increasing size and polarizability. We also calculated HOMO-LUMO energy levels and dipole moments of some selected the synthesized compounds (6a, 6h, 6m and 6s) using Gaussian software.
A highly selective space-folded photo-induced electron transfer fluorescent probe for carbonic anhydrase isozymes IX and its applications for biological imaging
Zhang, Shenyi,Yang, Chunmei,Lu, Weiqiang,Huang, Jin,Zhu, Weiping,Li, Honglin,Xu, Yufang,Qian, Xuhong
supporting information; experimental part, p. 8301 - 8303 (2011/09/14)
The first highly selective and sensitive fluorescent probe Z1 for detection of carbonic anhydrase IX (CA IX) over isoforms CA I and CA II was developed. As demonstrated, Z1 worked effectively in both enzymatic systems and living hypoxia cells.
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase
Kim, Sun Hee,Tran, Martin T.,Ruebsam, Frank,Xiang, Alan X.,Ayida, Benjamin,McGuire, Helen,Ellis, David,Blazel, Julie,Tran, Chinh V.,Murphy, Douglas E.,Webber, Stephen E.,Zhou, Yuefen,Shah, Amit M.,Tsan, Mei,Showalter, Richard E.,Patel, Rupal,Gobbi, Alberto,LeBrun, Laurie A.,Bartkowski, Darian M.,Nolan, Thomas G.,Norris, Daniel A.,Sergeeva, Maria V.,Kirkovsky, Leo,Zhao, Qiang,Han, Qing,Kissinger, Charles R.
supporting information; scheme or table, p. 4181 - 4185 (2009/04/16)
A novel series of HCV NS5B polymerase inhibitors comprising 1,1-dioxoisothiazoles and benzo[b]thiophene-1,1-dioxides were designed, synthesized, and evaluated. SAR studies guided by structure-based design led to the identification of a number of potent NS
