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Cholinesterase Inhibitory Activities of N-Phenylthiazol-2-Amine Derivatives and their Molecular Docking Studies.
Med Chem. 2015; 11(5):489-96.MC

Abstract

Alzheimer's disease (AD) is a type of neurodegenerative disorder which is responsible for many cognitive dysfunctions. According to the most accepted cholinergic hypothesis, cholinesterases have a major role in AD symptoms. The use of small molecules as inhibitors is one of the most useful strategies to control AD. In the present work, a series of N-phenylthiazol-2-amine derivatives was screened against acetylcholinesterase (AChE) from Electrophorus electricus and butyrylcholinesterase (BChE) from horse serum by using Ellman's method, using neostigmine and donepezil as reference drugs. Some of the assayed compounds proved to be potent inhibitors for AChE and BChE activity. N-(2,3-dimethylphenyl)thiazol-2-amine, 3j was found to be the most active inhibitor among the series with IC50 value of 0.009 ± 0.002 µM and 0.646 ± 0.012 µM against AChE and BChE, respectively. Molecular docking studies were carried out in order to better understand the ligand binding site interactions.

Authors+Show Affiliations

Centre for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan. jamshediqb@googlemail.com.No affiliation info availableNo affiliation info availableNo affiliation info availableNo 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

25537128

Citation

Iqbal, Jamshed, et al. "Cholinesterase Inhibitory Activities of N-Phenylthiazol-2-Amine Derivatives and Their Molecular Docking Studies." Medicinal Chemistry (Shariqah (United Arab Emirates)), vol. 11, no. 5, 2015, pp. 489-96.
Iqbal J, al-Rashida M, Babar A, et al. Cholinesterase Inhibitory Activities of N-Phenylthiazol-2-Amine Derivatives and their Molecular Docking Studies. Med Chem. 2015;11(5):489-96.
Iqbal, J., al-Rashida, M., Babar, A., Hameed, A., Khan, M. S., Munawar, M. A., & Khan, A. F. (2015). Cholinesterase Inhibitory Activities of N-Phenylthiazol-2-Amine Derivatives and their Molecular Docking Studies. Medicinal Chemistry (Shariqah (United Arab Emirates)), 11(5), 489-96.
Iqbal J, et al. Cholinesterase Inhibitory Activities of N-Phenylthiazol-2-Amine Derivatives and Their Molecular Docking Studies. Med Chem. 2015;11(5):489-96. PubMed PMID: 25537128.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Cholinesterase Inhibitory Activities of N-Phenylthiazol-2-Amine Derivatives and their Molecular Docking Studies. AU - Iqbal,Jamshed, AU - al-Rashida,Mariya, AU - Babar,Ayesha, AU - Hameed,Abdul, AU - Khan,Muhammad Siraj, AU - Munawar,Munawar Ali, AU - Khan,Ather Farooq, PY - 2014/08/06/received PY - 2014/12/15/accepted PY - 2014/12/25/entrez PY - 2014/12/30/pubmed PY - 2016/4/20/medline SP - 489 EP - 96 JF - Medicinal chemistry (Shariqah (United Arab Emirates)) JO - Med Chem VL - 11 IS - 5 N2 - Alzheimer's disease (AD) is a type of neurodegenerative disorder which is responsible for many cognitive dysfunctions. According to the most accepted cholinergic hypothesis, cholinesterases have a major role in AD symptoms. The use of small molecules as inhibitors is one of the most useful strategies to control AD. In the present work, a series of N-phenylthiazol-2-amine derivatives was screened against acetylcholinesterase (AChE) from Electrophorus electricus and butyrylcholinesterase (BChE) from horse serum by using Ellman's method, using neostigmine and donepezil as reference drugs. Some of the assayed compounds proved to be potent inhibitors for AChE and BChE activity. N-(2,3-dimethylphenyl)thiazol-2-amine, 3j was found to be the most active inhibitor among the series with IC50 value of 0.009 ± 0.002 µM and 0.646 ± 0.012 µM against AChE and BChE, respectively. Molecular docking studies were carried out in order to better understand the ligand binding site interactions. SN - 1875-6638 UR - https://www.unboundmedicine.com/medline/citation/25537128/Cholinesterase_Inhibitory_Activities_of_N_Phenylthiazol_2_Amine_Derivatives_and_their_Molecular_Docking_Studies_ L2 - http://www.eurekaselect.com/127235/article DB - PRIME DP - Unbound Medicine ER -