Synthesis and characterization of novel dioxoacridine sulfonamide derivatives as new carbonic anhydrase inhibitors

Rapid synthesis of novel 1,8-dioxoacridine carboxylic acid derivatives by microwave irradiation and their free radical scavenging activity

“…Acridine derivatives have similar structures to NADH (nicotinamide adenine dinucleotide) (Hempel et al, 1979); thus, this molecule group has important biological actives as antimalarial (Thull and Testa, 1994), anticancer (Grove et al, 1982), antiglaucoma (Kaya et al, 2012;Ulus et al, 2013;Yeşildag et al, 2014), antimicrobial (Kaya et al, 2015), calcium channel blocking (Di Stilo et al, 1998), and potassium cannel opening (Li et al, 1996). In addition to the properties of this molecule group, they are also known as laser dyes and intercalated agent (Lerman, 1963).…”

A simple one-pot synthesis of new 9-aroyl-3,4,6,7,9,10-hexahydro-1,8(2H,5H)-acridinediones

“…13 There are many reports on the synthesis of acridinedione derivatives including multi-component reactions (MCRs) of aromatic aldehydes, 1,3-diketones and various aromatic amines or ammonium acetate in the presence of different catalysts. [14][15][16][17][18][19][20] Alginic acid is a naturally occurring polysaccharide that can also be produced by a microbial fermentation. It has many carboxylic acid and hydroxyl groups in its backbone.…”

Synthesis of novel acridine bis-sulfonamides with effective inhibitory activity against the carbonic anhydrase isoforms I, II, IX and XII

“…11 By catalyzing this simple reaction CAs participate in many physiological processes such as regulation of respiration and gas exchange, bone resorption, calcification, pH and CO 2 homeostasis, electrolyte secretion in a variety of tissues/ organs, biosynthetic reactions. [11][12][13] This diversity of roles makes different isoforms interesting drug targets for a variety of conditions.…”

“…11 By catalyzing this simple reaction CAs participate in many physiological processes such as regulation of respiration and gas exchange, bone resorption, calcification, pH and CO 2 homeostasis, electrolyte secretion in a variety of tissues/ organs, biosynthetic reactions. [11][12][13] This diversity of roles makes different isoforms interesting drug targets for a variety of conditions. [1,10]phenanthrolin-9-one; CAIs, carbonic anhydrase inhibitors; IR, infrared; NMR, nuclear magnetic resonance; HRMS, high resolution mass spectroscopy; SAR, structure-activity relationship; DMSO, dimethyl sulfoxide; LC, liquid chromatography; DBSA, p-dodecylbenzenesulfonic acid; TLC, tine layer chromatography; mp, melting point; Lit, literature; ESI, electron spray ionization; TEA, trimethylamine; lM, micromolar; nM, nanomolar; K I , inhibition constant.…”

“…Antiglaucoma CAI-drugs mainly target CA II, IV and XII; the diuretics CA II, IV, XII and XIV; the antiepileptic CA VII and XIV. 11,14,16,17 The selective inhibition of the CA IX and XII isoforms results in antitumor and antimetastatic effects. 13,14 In vivo experiments showed that silencing of hCA IX reduces xenograft tumors to 40% of the volume along with up-regulation response of the gene encoding for hCA XII.…”