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Synthesis and AChE Inhibitory Activity of Novel Thiazolylhydrazone Derivatives.
Molecules. 2019 Jun 28; 24(13)M

Abstract

Alzheimer's disease (AD) is the most common of the degenerative brain diseases and is described together with the impairment of cognitive function. Patients with AD lose the capability to code new memories, and life conditions are extremely difficult. The development of new drugs in this area continues at a great pace. A novel series of thiazole-piperazine hybrids, aimed against Alzheimer's disease (AD), have been synthesized. The structure identification of synthesized compounds was elucidated by 1HNMR, 13C-NMR, and LCMSMS spectroscopic methods. The inhibitory potential of the synthesized compounds on cholinesterase enzymes was investigated. The compounds 3a, 3c and 3i showed significant inhibitory activity on the acetylcholinesterase (AChE) enzyme. On the other hand, none of the compounds showed significant inhibitory activity on the butyrylcholinesterase (BChE) enzyme. In addition to enzyme inhibition studies, enzyme kinetic studies were performed to observe the effects of the most active inhibitor compounds on the substrate-enzyme relationship. In addition to in vitro tests, docking studies also indicated that compound 3c potentially acts as a dual binding site AChE inhibitor.

Authors+Show Affiliations

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey. Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey.Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey. Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey.Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey. Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey.Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey. Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey.Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey.Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey. yozkay@anadolu.edu.tr. Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey. yozkay@anadolu.edu.tr.Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey.Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu Universty, 26470 Eskişehir, Turkey.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31261693

Citation

Osmaniye, Derya, et al. "Synthesis and AChE Inhibitory Activity of Novel Thiazolylhydrazone Derivatives." Molecules (Basel, Switzerland), vol. 24, no. 13, 2019.
Osmaniye D, Sağlık BN, Acar Çevik U, et al. Synthesis and AChE Inhibitory Activity of Novel Thiazolylhydrazone Derivatives. Molecules. 2019;24(13).
Osmaniye, D., Sağlık, B. N., Acar Çevik, U., Levent, S., Kaya Çavuşoğlu, B., Özkay, Y., Kaplancıklı, Z. A., & Turan, G. (2019). Synthesis and AChE Inhibitory Activity of Novel Thiazolylhydrazone Derivatives. Molecules (Basel, Switzerland), 24(13). https://doi.org/10.3390/molecules24132392
Osmaniye D, et al. Synthesis and AChE Inhibitory Activity of Novel Thiazolylhydrazone Derivatives. Molecules. 2019 Jun 28;24(13) PubMed PMID: 31261693.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and AChE Inhibitory Activity of Novel Thiazolylhydrazone Derivatives. AU - Osmaniye,Derya, AU - Sağlık,Begüm Nurpelin, AU - Acar Çevik,Ulviye, AU - Levent,Serkan, AU - Kaya Çavuşoğlu,Betül, AU - Özkay,Yusuf, AU - Kaplancıklı,Zafer Asım, AU - Turan,Gülhan, Y1 - 2019/06/28/ PY - 2019/05/30/received PY - 2019/06/24/revised PY - 2019/06/25/accepted PY - 2019/7/3/entrez PY - 2019/7/3/pubmed PY - 2019/12/19/medline KW - acetylcholinesterase KW - butyrylcholinesterase KW - docking KW - enzyme inhibition KW - thiazolylhydrazone JF - Molecules (Basel, Switzerland) JO - Molecules VL - 24 IS - 13 N2 - Alzheimer's disease (AD) is the most common of the degenerative brain diseases and is described together with the impairment of cognitive function. Patients with AD lose the capability to code new memories, and life conditions are extremely difficult. The development of new drugs in this area continues at a great pace. A novel series of thiazole-piperazine hybrids, aimed against Alzheimer's disease (AD), have been synthesized. The structure identification of synthesized compounds was elucidated by 1HNMR, 13C-NMR, and LCMSMS spectroscopic methods. The inhibitory potential of the synthesized compounds on cholinesterase enzymes was investigated. The compounds 3a, 3c and 3i showed significant inhibitory activity on the acetylcholinesterase (AChE) enzyme. On the other hand, none of the compounds showed significant inhibitory activity on the butyrylcholinesterase (BChE) enzyme. In addition to enzyme inhibition studies, enzyme kinetic studies were performed to observe the effects of the most active inhibitor compounds on the substrate-enzyme relationship. In addition to in vitro tests, docking studies also indicated that compound 3c potentially acts as a dual binding site AChE inhibitor. SN - 1420-3049 UR - https://www.unboundmedicine.com/medline/citation/31261693/Synthesis_and_AChE_Inhibitory_Activity_of_Novel_Thiazolylhydrazone_Derivatives_ L2 - https://www.mdpi.com/resolver?pii=molecules24132392 DB - PRIME DP - Unbound Medicine ER -