- "a Sweet Combination": Developing Saccharin and Acesulfame K Structures for Selectively Targeting the Tumor-Associated Carbonic Anhydrases IX and XII
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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
- 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.
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Read Online
- Substituted pyrazolyl pyrazole sulfonamide compound or pesticide acceptable salt and composition, and application thereof
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The invention belongs to the field of pesticides, and particularly relates to a substituted pyrazolyl pyrazole sulfonamide compound or a pesticide acceptable salt and a composition, and an applicationthereof. The compound has the structure represented by
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Paragraph 0118-0121
(2019/12/25)
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- 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
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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.
- Khelili, Smail,Kihal, Nadjib,Yekhlef, Mohamed,De Tullio, Pascal,Lebrun, Philippe,Pirotte, Bernard
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scheme or table
p. 873 - 878
(2012/09/10)
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- Acetic acid derivatives of 3,4-dihydro-2 H-1,2,4-benzothiadiazine 1,1-dioxide as a novel class of potent aldose reductase inhibitors
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A series of novel benzothiadiazine 1,1-dioxide derivatives were synthesized and tested for their inhibitory activity against aldose reductase. Of these derivatives, 17 compounds, having a substituted N2-benzyl group and a N4-acetic acid group on the benzothiadiazine, were found to be potent and selective aldose reductase inhibitors in vitro with IC50 values ranging from 0.032 to 0.975 μM. 9m proved to be the most active in vitro. The eight top-scoring compounds coming from the in vitro test for ALR2 inhibition activity were then tested in vivo, whereby three derivatives, 9i, 9j, and 9m, demonstrated a significantly preventive effect on sorbitol accumulation in the sciatic nerve in the 5-day streptozotocin-induced diabetic rats in vivo. Structure-activity relationship and molecular docking studies highlighted the importance of substitution features of N4-acetic acid group and halogen-substituted N2-benzyl group in the benzothiadiazine scaffold and indicated that substitution with hallogen at C-7 had a remarkably strong effect on ALR2 inhibition potency.
- Chen, Xin,Zhu, Changjin,Guo, Fan,Qiu, Xiaowei,Yang, Yanchun,Zhang, Shuzhen,He, Minlan,Parveen, Shagufta,Jing, Chaojun,Li, Yan,Ma, Bing
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experimental part
p. 8330 - 8344
(2011/02/23)
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- 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
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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.
- 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.
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p. 3833 - 3838
(2007/10/03)
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