71254-67-6Relevant academic research and scientific papers
"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 (2020/01/02)
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
Radiosynthesis of a carbon-11-labeled AMPAR allosteric modulator as a new PET radioligand candidate for imaging of Alzheimer's disease
Miao, Caihong,Dong, Fugui,Jia, Limeng,Li, Wei,Wang, Min,Zheng, Qi-Huang,Xu, Zhidong
, p. 1177 - 1181 (2019/03/27)
To develop PET tracers for imaging of Alzheimer's disease, a new carbon-11-labeled AMPAR allosteric modulator 4-cyclopropyl-7-(3-[11C]methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide ([11C]8) has been synthesized
FUSED [1,2,4]THIADIAZINE DERIVATIVES WHICH ACT AS KAT INHIBITORS OF THE MYST FAMILY
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Page/Page column 224, (2019/03/17)
A compound of formula (I): which inhibits the activity of one or more KATs of the MYST family, i.e., TIP60, KAT6B, MOZ, HBO1 and MOF.
Design of Benzoxathiazin-3-one 1,1-Dioxides as a New Class of Irreversible Serine Hydrolase Inhibitors: Discovery of a Uniquely Selective PNPLA4 Inhibitor
Kornahrens, Anne F.,Cognetta, Armand B.,Brody, Daniel M.,Matthews, Megan L.,Cravatt, Benjamin F.,Boger, Dale L.
supporting information, p. 7052 - 7061 (2017/05/31)
The design and examination of 4,1,2-benzoxathiazin-3-one 1,1-dioxides as candidate serine hydrolase inhibitors are disclosed, and represent the synthesis and study of a previously unexplored heterocycle. This new class of activated cyclic carbamates provi
BENZOTHIADIAZINE COMPOUNDS
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Page/Page column 147-148, (2017/07/23)
The invention is directed to substituted benzothiadiazine derivatives. Specifically, the invention is directed to compounds according to Formula (I):wherein R, R1, R2, R3, R4 and R5 are as defined herein. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, autoimmune diseases, infections, atherosclerosis, and ischemia-reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Effect of C7 Modifications on Benzothiadiazine-1,1-dioxide Derivatives on Their Inhibitory Activity and Selectivity toward Aldose Reductase
Zhang, Shuzhen,Chen, Xin,Parveen, Shagufta,Hussain, Saghir,Yang, Yanchun,Jing, Chaojun,Zhu, Changjin
, p. 603 - 613 (2013/08/22)
The development and progression of chronic complications in diabetic patients, such as retinopathy, nephropathy, neuropathy, cataracts, and stroke, are related to the activation and/or overexpression of aldose reductase (ALR2), which is a member of the al
Hydroxylated analogues of ATP-sensitive potassium channel openers belonging to the group of 6- and/or 7-substituted 3-Isopropylamino-4H-1,2,4- benzothiadiazine 1,1-dioxides: Toward an improvement in sulfonylurea receptor 1 selectivity and metabolism stabi
De Tullio, Pascal,Servais, Anne-Catherine,Fillet, Marianne,Gillotin, Florian,Somers, Fabian,Chiap, Patrice,Lebrun, Philippe,Pirotte, Bernard
scheme or table, p. 8353 - 8361 (2012/02/04)
Diversely substituted 3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides are known to be potent KATP channel openers, with several drugs being selective for the SUR1/Kir6.2 channel subtype. This work examined the biological activity, tissu
PYRRO[1,2-B]PYRIDAZINONE COMPOUNDS
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Page/Page column 49; 65-66, (2008/06/13)
The invention is directed to pyrro[l,2-b]pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
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.
PYRIDAZINONE COMPOUNDS
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Page/Page column 76-77, (2010/11/08)
The invention is directed to pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
