Literature DB >> 30118983

Novel thymol bearing oxypropanolamine derivatives as potent some metabolic enzyme inhibitors - Their antidiabetic, anticholinergic and antibacterial potentials.

Mustafa Zengin1, Hayriye Genc1, Parham Taslimi2, Ali Kestane1, Ertugrul Guclu3, Aziz Ogutlu3, Oguz Karabay3, İlhami Gulçin4.   

Abstract

A series of classical and newly synthesized thymol bearing oxypropanolamine compounds were synthesized and characterized. Their in vitro antibacterial activity on A. baumannii, P. aeruginosa, E. coli and S. aureus strains were investigated with agar well diffusion method. The results were compared with commercially available drug active compounds. As well as 3a, 3b and 3c have the most significant antibacterial effect among all the tested compounds; approximately all of them have more antibacterial activity than the reference drugs. These novel thymol bearing oxypropanolamine derivatives were effective inhibitors of the α-glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and acetylcholinesterase enzymes (AChE) with Ki values in the range of 463.85-851.05 µM for α-glycosidase, 1.11-17.34 µM for hCA I, 2.97-17.83 µM for hCA II, and 13.58-31.45 µM for AChE, respectively.
Copyright © 2018 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Acetylcholinesterase; Antibacterial effects; Carbonic anhydrase; Oxypropanolamine; α-glycosidase

Mesh:

Substances:

Year:  2018        PMID: 30118983     DOI: 10.1016/j.bioorg.2018.08.003

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  8 in total

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