Synthesis of Novel Hydrazide-Hydrazone Compounds and In Vitro and In Silico Investigation of Their Biological Activities against AChE, BChE, and hCA I and II.

ABSTRACT: The abnormal levels of the human carbonic anhydrase isoenzymes I and II (hCA I and II) and cholinesterase enzymes, namely, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), are linked with various disorders including Alzheimer's disease. In this study, six new nicotinic hydrazide derivatives (7-12) were designed and synthesized for the first time, and their inhibitory profiles against hCA I, hCA II, AChE, and BChE were investigated by in vitro assays and in silico studies. The structures of novel molecules were elucidated by using spectroscopic techniques and elemental analysis. These molecules showed inhibitory activities against hCA I and II with IC₅₀ values ranging from 7.12 to 45.12 nM. Compared to reference drug acetazolamide (AZA), c

SUBMITTER: Cakmak R 

PROVIDER: S-EPMC11079868 | biostudies-literature | 2024 May

REPOSITORIES: biostudies-literature