51757-37-0Relevant articles and documents
Synthesis, characterization, inhibition effects, and molecular docking studies as acetylcholinesterase, α-glycosidase, and carbonic anhydrase inhibitors of novel benzenesulfonamides incorporating 1,3,5-triazine structural motifs
Durgun, Mustafa,Lolak, Nebih,Taslimi, Parham,Akocak, Süleyman,Beydemir, ?ükrü,Gül?in, ?lhami,I??k, Mesut,Türke?, Cüneyt
, (2020)
Some metabolic enzyme inhibitors can be used in the treatment of many diseases. Therefore, synthesis and determination of alternative inhibitors are essential. In this study, the inhibition effect of newly synthesized compounds on carbonic anhydrase (cytosolic isoforms, hCA I and hCA II), α-glycosidase (α-GLY), and acetylcholinesterase (AChE) were investigated. The possible binding mechanism of the compounds with a high inhibitory effect on the active site of the enzyme was demonstrated by molecular docking method. We investigated the inhibition effects of novel synthesized compounds (MZ1-MZ11) on metabolic enzymes such as α-GLY, AChE, and hCA I and II. The compound MZ6 for AChE, MZ8 for CA I and CA II and MZ7 for α-GLY showed a very active inhibition profile (KIs 51.67 ± 4.76 for hCA I, 40.35 ± 5.74 nM for hCA II, 41.74 ± 8.08 nM for α-GLY and 335.76 ± 46.91 nM for AChE). The novel synthesized compounds (MZ1-MZ11) have a higher enzyme (α-GLY, AChE, hCA I, and II) inhibitory potential than ACR, TAC, and AZA, respectively. The compounds may have the potential to be used as alternative medicines after further research in the treatment of many diseases such as diabetes, Alzheimer's disease, heart failure, ulcer, and epilepsy.
Indoloxytriazines as binding molecules for the JAK2 JH2 pseudokinase domain and its V617F variant
Newton, Ana S.,Liosi, Maria-Elena,Henry, Sean P.,Deiana, Luca,Faver, John C.,Krimmer, Stefan G.,Puleo, David E.,Schlessinger, Joseph,Jorgensen, William L.
supporting information, (2021/07/20)
Small molecules that selectively bind to the pseudokinase JH2 domain over the JH1 kinase domain of JAK2 kinase are sought. Virtual screening led to the purchase of 17 compounds among which 9 were found to bind to V617F JAK2 JH2 with affinities of 40 – 300
Optimization and comparison of synthetic procedures for a group of triazinyl-substituted benzene-sulfonamide conjugates with amino acids
Kraj?iová, Dominika,Pecher, Daniel,Garaj, Vladimír,Miku, Peter
, (2017/09/25)
Sulfonamides incorporating 1,3,5-triazine moieties can selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII, and XIV over cytosolic isoforms I and II. In the present work, a highly effective synthetic procedure was proposed f
