Korkmaz_2022_Biotechnol.Appl.Biochem__

Reference

Title : 2-Amino thiazole derivatives as inhibitors of some metabolic enzymes: An in vitro and in silico study - Korkmaz_2022_Biotechnol.Appl.Biochem__
Author(s) : Korkmaz IN
Ref : Biotechnol Appl Biochem , : , 2022
Abstract :

The thiazole derivatives are desirable compounds in the evaluation of their biological activities such as antiprotozoal antibacterial, antifungal, antituberculosis. Considering the medical application potential of 2-amino thiazole compounds, we aimed to determine the effects of 2-amino thiazole derivatives on the activities of carbonic anhydrase I-II isoenzymes, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Among the chemicals we used in our study, 2-amino-4-(4-chlorophenyl)thiazole compound exhibited the best inhibition against hCA I with K(i) of 0.008 +/- 0.001 microM. The 2-amino-4-(4-bromophenyl)thiazole compound exhibited the best inhibition against hCA II, AChE, and BChE with K(i) of 0.124 +/- 0.017, 0.129 +/- 0.030, and 0.083 +/- 0.041 microM, respectively. Molecular docking analysis showed that compound 2-amino-4-(5,6,7,8-tetrahydro-2-naphthyl)thiazole had the highest inhibitory potency against hCA I, hCA II, AChE, BChE with the estimated binding energy of -6.75, -7.61, -7.86, -7.96 kcal/mol, respectively.

PubMedSearch : Korkmaz_2022_Biotechnol.Appl.Biochem__
PubMedID: 35857901

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Citations formats

Korkmaz IN (2022)
2-Amino thiazole derivatives as inhibitors of some metabolic enzymes: An in vitro and in silico study
Biotechnol Appl Biochem :

Korkmaz IN (2022)
Biotechnol Appl Biochem :