Lolak_2020_Bioorg.Chem_100_103897

Reference

Title : Synthesis, characterization, inhibition effects, and molecular docking studies as acetylcholinesterase, alpha-glycosidase, and carbonic anhydrase inhibitors of novel benzenesulfonamides incorporating 1,3,5-triazine structural motifs - Lolak_2020_Bioorg.Chem_100_103897
Author(s) : Lolak N , Akocak S , Turkes C , Taslimi P , Isik M , Beydemir S , Gulcin I , Durgun M
Ref : Bioorg Chem , 100 :103897 , 2020
Abstract :

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), alpha-glycosidase (alpha-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 alpha-GLY, AChE, and hCA I and II. The compound MZ6 for AChE, MZ8 for CA I and CA II and MZ7 for alpha-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 alpha-GLY and 335.76 +/- 46.91 nM for AChE). The novel synthesized compounds (MZ1-MZ11) have a higher enzyme (alpha-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.

PubMedSearch : Lolak_2020_Bioorg.Chem_100_103897
PubMedID: 32413628

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Citations formats

Lolak N, Akocak S, Turkes C, Taslimi P, Isik M, Beydemir S, Gulcin I, Durgun M (2020)
Synthesis, characterization, inhibition effects, and molecular docking studies as acetylcholinesterase, alpha-glycosidase, and carbonic anhydrase inhibitors of novel benzenesulfonamides incorporating 1,3,5-triazine structural motifs
Bioorg Chem 100 :103897

Lolak N, Akocak S, Turkes C, Taslimi P, Isik M, Beydemir S, Gulcin I, Durgun M (2020)
Bioorg Chem 100 :103897