41104-56-7Relevant academic research and scientific papers
Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity
Congiu, Cenzo,Onnis, Valentina,Deplano, Alessandro,Balboni, Gianfranco,Dedeoglu, Nurcan,Supuran, Claudiu T.
, p. 3850 - 3853 (2015)
Abstract By using SLC-0111 (4-fluorophenylureido-benzenesulfonamide), a sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitor in Phase I clinical trials as an antitumor agent as lead molecule, a series of benzenesulfonamide derivatives incorporating u
Benzylaminoethyureido-tailed benzenesulfonamides: Design, synthesis, kinetic and X-ray investigations on human carbonic anhydrases
Ali, Majid,Angeli, Andrea,Berto, Paola,Bozdag, Murat,Carta, Fabrizio,Farooq, Umar,Supuran, Claudiu T.,Zanotti, Giuseppe
, (2020/04/28)
A drug design strategy of carbonic anhydrase inhibitors (CAIs) belonging to sulfonamides incorporating ureidoethylaminobenzyl tails is presented. A variety of substitution patterns on the ring and the tails, located on para- or meta- positions with respec
Benzylaminoethylureido-Tailed Benzenesulfonamides Show Potent Inhibitory Activity against Bacterial Carbonic Anhydrases
Ali, Majid,Angeli, Andrea,Bozdag, Murat,Carta, Fabrizio,Capasso, Clemente,Farooq, Umar,Supuran, Claudiu T.
, p. 2444 - 2447 (2020/10/30)
A series of benzylaminoethylureido-tailed benzenesulfonamides was analyzed for their inhibition potential against bacterial carbonic anhydrases (CAs) such as VhCA α, β, and γ from Vibrio cholerae, and BpsCA β and γ-CAs from Burkholderia pseudomallei. Grow
Preparation method of aminosulfonyl phenylurea safener
-
Paragraph 0035; 0037; 0042; 0044, (2020/07/24)
The invention discloses a preparation method of an aminosulfonyl phenylurea safener, and particularly relates to the field of aminosulfonyl phenylurea medicines, and the preparation method specifically comprises the following steps: 1, dropwise adding chl
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3
Li, Yingxiu,Ye, Tianyu,Xu, Le,Dong, Yuhong,Luo, Yong,Wang, Chu,Han, Yufei,Chen, Ke,Qin, Mingze,Liu, Yajing,Zhao, Yanfang
, (2019/08/12)
Hybridization strategy is an effective strategy to obtain multi-target inhibitors in drug design. In this study, we assembled the pharmacophores of momelotinib and tandutinib to get a series of 4-piperazinyl-2-aminopyrimidine derivatives. All compounds were tested for the inhibition of JAK2 and FLT3 enzymes, of which, compounds with potent enzyme activities were assayed for antiproliferative activities against three cancer cell lines (HEL, MV4-11, and HL60). The structure-activity relationship studies were conducted through variations in two regions, the “A” phenyl ring and “B” phenyl ring. Compound 14j showed the most balanced in vitro inhibitory activity against JAK2 and FLT3 (JAK2 IC50 = 27 nM, FLT3 IC50 = 30 nM), and it also showed potent inhibition against the above tested cell lines. In the cellular context, 14j strongly induced apoptosis by arresting cell cycle in the G1/S phase, and was selected as a promising JAK2/FLT3 dual inhibitor.
Synthesis and characterization of vanillin semicarbazones
Venkateshhan,Ravichandiran,Selvakumar,Lavakumar
experimental part, p. 4632 - 4634 (2012/02/04)
Semicarbazones have a great interest because of their chemistry and biological activities for the treatment of various human ailments. A series of seven vanillin semicarbazones (3a-g) were synthesized by reflux of aryl semicarbazides with appropriate carbonyl compound in the presence of glacial acetic acid. The aryl semicarbazides (2a-g) were synthesized from aryl carbamates by reacting with hydrazine hydrate and ethanol on hydrazinolysis. The aryl carbamates (1a-g) were obtained by the reaction between phenyl chloro formate and aniline/substituted aniline in anhydrous ether in the presence of sodium hydroxide. The structure of the newly synthesized compounds was established by various analytical techniques such as IR, 1H NMR and MASS spectral studies.
Organic Compounds
-
Page/Page column 73, (2010/12/29)
A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
Sulfamoylphenylureas
-
, (2008/06/13)
The N-acylsulfamoylphenylureas of formula I below are suitable as counter-agents (antidotes or safeners) for protecting cultivated plants from the phytotoxic action of herbicides. Suitable crops are preferably cereals, soybeans, sorghum, maize and rice, and suitable herbicides are sulfonylureas, chloroacetanilides and aryloxyphenoxypropionic acid derivatives. The N-acylsulfamoylphenylureas have the formula I STR1 wherein A is a radical selected from the group STR2 R1 is C1 -C4 -alkoxy or each of R1 and R2, independently of the other, is hydrogen, C1 -C8 alkyl, C3 -C8 cycloalkyl, C3 -C6 alkenyl, C3 -C6 alkynyl, STR3 or C1 -C4 alkyl substituted by C1 -C4 alkoxy or by STR4 or R1 and R2 together form a C4 -C6 alkylene bridge, or a C4 -C6 alkylene bridge interrupted by oxygen, sulfur, SO, SO2, NH or by --N(C1 -C4 alkyl)-, R3 is hydrogen or C1 -C4 alkyl, Ra to Rh, Rx and Ry are as defined in the disclosure.
