50881-48-6Relevant articles and documents
"a Sweet Combination": Developing Saccharin and Acesulfame K Structures for Selectively Targeting the Tumor-Associated Carbonic Anhydrases IX and XII
Bua, Silvia,Lomelino, Carrie,Murray, Akilah B.,Osman, Sameh M.,Alothman, Zeid A.,Bozdag, Murat,Abdel-Aziz, Hatem A.,Eldehna, Wagdy M.,McKenna, Robert,Nocentini, Alessio,Supuran, Claudiu T.
, p. 321 - 333 (2020)
The sweeteners saccharin (SAC) and acesulfame K (ACE) recently entered the topic of anticancer human carbonic anhydrase (CA, EC 4.2.1.1) inhibitors, as they showed to selectively inhibit the tumor-associated CAs IX/XII over ubiquitous CAs. A drug design s
Synthesis and pharmacological activity of N-(2,2-dimethyl-3,4-dihydro-2H-1- benzopyran-4-yl)-4H-1,2,4-benzothiadiazine-3-carboxamides 1,1-dioxides on rat uterus, rat aorta and rat pancreatic β-cells
Khelili, Smail,Kihal, Nadjib,Yekhlef, Mohamed,De Tullio, Pascal,Lebrun, Philippe,Pirotte, Bernard
scheme or table, p. 873 - 878 (2012/09/10)
N-(2,2-Dimethyl-3,4-dihydro-2H-1-benzopyran-4-yl)-4H-1,2, 4-benzothiadiazine-3-carboxamides 1,1-dioxides were prepared and evaluated on rat uterus, rat aortic rings and rat pancreatic β-cells. Pharmacological studies conducted on rat uterus indicated that several of these original hybrid compounds displayed a strong myorelaxant activity. The most active compounds hold a bromine atom at the 6-position of the dihydrobenzopyran ring. Moreover, the compounds failed to display a marked inhibitory effect on insulin secretion and vascular myogenic activity. These features suggest that the 6-bromo compounds could be relatively selective towards the uterine smooth muscle.
Inhibitors of HCV NS5B polymerase: Synthesis and structure-activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring
Rockway, Todd W.,Zhang, Rong,Liu, Dachun,Betebenner, David A.,McDaniel, Keith F.,Pratt, John K.,Beno, David,Montgomery, Debra,Jiang, Wen W.,Masse, Sherie,Kati, Warren M.,Middleton, Tim,Molla, Akhteruzzaman,Maring, Clarence J.,Kempf, Dale J.
, p. 3833 - 3838 (2007/10/03)
A series of non-nucleoside HCV NS5B polymerase inhibitors based on the N-1-benzyl or N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine core substituted in the D-ring aromatic moiety have been prepared and evaluated. Aromatic substituents extending from position 7 of the D-ring exhibited excellent potency against both genotypes 1a and 1b.