35264-29-0Relevant articles and documents
Synthesis, biological evaluation and in silico studies of novel N-substituted phthalazine sulfonamide compounds as potent carbonic anhydrase and acetylcholinesterase inhibitors
Türke?, Cüneyt,Arslan, Mustafa,Demir, Yeliz,?o?aj, Liridon,Rifati Nixha, Arleta,Beydemir, ?ükrü
, (2019)
The synthesis, characterization and biological evaluation of a series of novel N-substituted phthalazine sulfonamide (5a-l) are disclosed. Phthalazines which are nitrogen-containing heterocyclic compounds are biologically preferential scaffolds, endowed with versatile pharmacological activity, such as anti-inflammatory, cardiotonic vasorelaxant, anticonvulsant, antihypertensive, antibacterial, anti-cancer action. The compounds were investigated for the inhibition against the cytosolic hCA I, II and AChE. Most screened sulfonamides showed high potency in inhibiting hCA II, widely involved in glaucoma, epilepsy, edema, and other pathologies (Kis in the ranging from 6.32 ± 0.06 to 128.93 ± 23.11 nM). hCA I was inhibited with Kis in the range of 6.80 ± 0.10–85.91 ± 7.57 nM, whereas AChE in the range of 60.79 ± 3.51–249.55 ± 7.89 nM. ADME prediction study of the designed N-substituted phthalazine sulfonamides showed that they are not only with carbonic anhydrase and acetylcholinesterase inhibitory activities but also with appropriate pharmacokinetic, physicochemical parameters and drug-likeness properties. Also, in silico docking studies were investigated the binding modes of selected compounds, to hCA I, II, and AChE.
Development of novel quinoline-based sulfonamides as selective cancer-associated carbonic anhydrase isoform ix inhibitors
Capasso, Clemente,El-Domany, Ramadan A.,Eldehna, Wagdy M.,Elsayed, Zainab M.,Ibrahim, Tamer M.,Nocentini, Alessio,Salem, Rofaida,Shaldam, Moataz,Supuran, Claudiu T.
, (2021/10/19)
A new series of quinoline-based benzenesulfonamides (QBS) were developed as potential carbonic anhydrase inhibitors (CAIs). The target QBS CAIs is based on the 4-anilinoquinoline scaffold where the primary sulphonamide functionality was grafted at C4 of t
Oxadiazole substituted benzenesulfonamide compound and preparation method thereof and application as carbonic anhydrase inhibitor
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Paragraph 0059; 0064-0066, (2020/04/02)
The invention discloses an oxadiazole substituted benzenesulfonamide compound as shown in a formula I or pharmaceutically acceptable salt thereof, a preparation method of the oxadiazole substituted benzenesulfonamide compound and an application of the oxadiazole substituted benzenesulfonamide compound as a carbonic anhydrase inhibitor. The compound is simple in preparation process, mild in reaction conditions in key steps, higher in yield, lower in energy consumption and more environment-friendly, and the compound shows a good development potential as a carbonic anhydrase inhibitor.
