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Synthesis of novel 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/-nonsubstituted benzal)hydrazone derivatives and acetylcholinesterase and butyrylcholinesterase inhibitory activities in vitro.
Arzneimittelforschung. 2011; 61(1):1-7.A

Abstract

In this study thirteen 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/nonsubstituted benzal)hydrazone V derivatives were synthesized as acetylcholinesterase and butyrylcholinesterase inhibitors. Ten of the synthesized compounds were synthesized for the first time in this study and the rest of them had been synthesized in a previous study. The structures of compounds V were elucidated by IR, 1H-NMR and MASS spectra. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChe) inhibitory activities of V derivatives were measured using Ellman's method. While some of the 6-substituted-3(2H)-pyridazinone-2-propyl-3-(substituted/-nonsubstituted benzal)hydrazone V derivatives exhibited significant AChE inhibitory activity, none of the compoundsshowed BChE inhibitory activity. Theseresults indicate that V derivatives were AChE inhibitors with AChE/ BChE selectivity.

Authors+Show Affiliations

Mersin University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Mersin, Turkey.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21355440

Citation

Utku, Semra, et al. "Synthesis of Novel 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/-nonsubstituted Benzal)hydrazone Derivatives and Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities in Vitro." Arzneimittel-Forschung, vol. 61, no. 1, 2011, pp. 1-7.
Utku S, Gökçe M, Orhan I, et al. Synthesis of novel 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/-nonsubstituted benzal)hydrazone derivatives and acetylcholinesterase and butyrylcholinesterase inhibitory activities in vitro. Arzneimittelforschung. 2011;61(1):1-7.
Utku, S., Gökçe, M., Orhan, I., & Sahin, M. F. (2011). Synthesis of novel 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/-nonsubstituted benzal)hydrazone derivatives and acetylcholinesterase and butyrylcholinesterase inhibitory activities in vitro. Arzneimittel-Forschung, 61(1), 1-7. https://doi.org/10.1055/s-0031-1296161
Utku S, et al. Synthesis of Novel 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/-nonsubstituted Benzal)hydrazone Derivatives and Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities in Vitro. Arzneimittelforschung. 2011;61(1):1-7. PubMed PMID: 21355440.
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TY - JOUR T1 - Synthesis of novel 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/-nonsubstituted benzal)hydrazone derivatives and acetylcholinesterase and butyrylcholinesterase inhibitory activities in vitro. AU - Utku,Semra, AU - Gökçe,Mehtap, AU - Orhan,Ilkay, AU - Sahin,M Fethi, PY - 2011/3/2/entrez PY - 2011/3/2/pubmed PY - 2011/3/23/medline SP - 1 EP - 7 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 61 IS - 1 N2 - In this study thirteen 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/nonsubstituted benzal)hydrazone V derivatives were synthesized as acetylcholinesterase and butyrylcholinesterase inhibitors. Ten of the synthesized compounds were synthesized for the first time in this study and the rest of them had been synthesized in a previous study. The structures of compounds V were elucidated by IR, 1H-NMR and MASS spectra. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChe) inhibitory activities of V derivatives were measured using Ellman's method. While some of the 6-substituted-3(2H)-pyridazinone-2-propyl-3-(substituted/-nonsubstituted benzal)hydrazone V derivatives exhibited significant AChE inhibitory activity, none of the compoundsshowed BChE inhibitory activity. Theseresults indicate that V derivatives were AChE inhibitors with AChE/ BChE selectivity. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/21355440/Synthesis_of_novel_6_substituted_3_2H__pyridazinone_2_acetyl_2__substituted/_nonsubstituted_benzal_hydrazone_derivatives_and_acetylcholinesterase_and_butyrylcholinesterase_inhibitory_activities_in_vitro_ L2 - http://www.thieme-connect.com/DOI/DOI?10.1055/s-0031-1296161 DB - PRIME DP - Unbound Medicine ER -