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The synthesis of some β-lactams and investigation of their metal-chelating activity, carbonic anhydrase and acetylcholinesterase inhibition profiles.
J Enzyme Inhib Med Chem. 2016; 31(sup1):79-88.JE

Abstract

β-Lactam antibiotics are a broad class of antibiotics, consisting of all antibiotic agents that contain a β-lactam ring in their molecular structures. Synthesis of β-lactam analogs, which are containing dichloride atoms and N-methyl, N-aromatic rings, was achieved by Schiff bases and dichloroketene compounds. All the synthesized imines and β-lactam analogs were tested against two physiologically relevant carbonic anhydrase isozymes (hCA I and II) and acetylcholinesterase (AChE). They demponstrated effective inhibitory profiles with Ki values in ranging of 3.22-11.18 nM against hCA I, 3.74-10.41 nM against hCA II, and 0.50-1.57 nM against AChE. On the other hand, acetazolamide and dorzolamide clinically used as CA inhibitors, showed Ki value of 170.34 and 129.26 nM against hCA I, and 115.43 and 135.67 nM against hCA II, respectively. Also, tacrine used as standard AChE inhibitor showed Ki value of 5.70 nM against AChE.

Authors+Show Affiliations

a Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey.a Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey. b Department of Chemistry , Faculty of Science and Arts, Kafkas University , Kars , Turkey.a Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey.a Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey.a Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey.a Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey. c Department of Zoology , College of Science, King Saud University , Riyadh , Saudi Arabia.d Dipartimento Di Chimica Ugo Schiff, Universita Degli Studi Di Firenze , Firenze , Italy , and. e Department of Neurofarba , Section of Pharmaceutical and Nutriceutical Sciences, Universita Degli Studi Di Firenze , Florence , Italy.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27075164

Citation

Turan, Burhanettin, et al. "The Synthesis of some Β-lactams and Investigation of Their Metal-chelating Activity, Carbonic Anhydrase and Acetylcholinesterase Inhibition Profiles." Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 31, no. sup1, 2016, pp. 79-88.
Turan B, Şendil K, Şengül E, et al. The synthesis of some β-lactams and investigation of their metal-chelating activity, carbonic anhydrase and acetylcholinesterase inhibition profiles. J Enzyme Inhib Med Chem. 2016;31(sup1):79-88.
Turan, B., Şendil, K., Şengül, E., Gültekin, M. S., Taslimi, P., Gulçin, İ., & Supuran, C. T. (2016). The synthesis of some β-lactams and investigation of their metal-chelating activity, carbonic anhydrase and acetylcholinesterase inhibition profiles. Journal of Enzyme Inhibition and Medicinal Chemistry, 31(sup1), 79-88.
Turan B, et al. The Synthesis of some Β-lactams and Investigation of Their Metal-chelating Activity, Carbonic Anhydrase and Acetylcholinesterase Inhibition Profiles. J Enzyme Inhib Med Chem. 2016;31(sup1):79-88. PubMed PMID: 27075164.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The synthesis of some β-lactams and investigation of their metal-chelating activity, carbonic anhydrase and acetylcholinesterase inhibition profiles. AU - Turan,Burhanettin, AU - Şendil,Kivilcim, AU - Şengül,Emin, AU - Gültekin,Mehmet Serdar, AU - Taslimi,Parham, AU - Gulçin,İlhami, AU - Supuran,Claudiu T, Y1 - 2016/04/13/ PY - 2016/4/15/pubmed PY - 2017/2/23/medline PY - 2016/4/15/entrez KW - Acetylcholinesterase KW - Schiff bases KW - carbonic anhydrase KW - enzyme inhibition KW - enzyme purification KW - β-lactams SP - 79 EP - 88 JF - Journal of enzyme inhibition and medicinal chemistry JO - J Enzyme Inhib Med Chem VL - 31 IS - sup1 N2 - β-Lactam antibiotics are a broad class of antibiotics, consisting of all antibiotic agents that contain a β-lactam ring in their molecular structures. Synthesis of β-lactam analogs, which are containing dichloride atoms and N-methyl, N-aromatic rings, was achieved by Schiff bases and dichloroketene compounds. All the synthesized imines and β-lactam analogs were tested against two physiologically relevant carbonic anhydrase isozymes (hCA I and II) and acetylcholinesterase (AChE). They demponstrated effective inhibitory profiles with Ki values in ranging of 3.22-11.18 nM against hCA I, 3.74-10.41 nM against hCA II, and 0.50-1.57 nM against AChE. On the other hand, acetazolamide and dorzolamide clinically used as CA inhibitors, showed Ki value of 170.34 and 129.26 nM against hCA I, and 115.43 and 135.67 nM against hCA II, respectively. Also, tacrine used as standard AChE inhibitor showed Ki value of 5.70 nM against AChE. SN - 1475-6374 UR - https://www.unboundmedicine.com/medline/citation/27075164/The_synthesis_of_some_β_lactams_and_investigation_of_their_metal_chelating_activity_carbonic_anhydrase_and_acetylcholinesterase_inhibition_profiles_ L2 - http://www.tandfonline.com/doi/full/10.3109/14756366.2016.1170014 DB - PRIME DP - Unbound Medicine ER -