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Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase.
J Enzyme Inhib Med Chem. 2016 Dec; 31(6):1498-501.JE

Abstract

The effects of isatin Mannich bases incorporating (1-[piperidin-1-yl (P1)/morpholin-4-yl (P2)/N-methylpiperazin-1-yl (P3)]methyl)-1H-indole-2,3-dione) moieties against human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoenzymes hCA I and hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes were evaluated. P1-P3 demonstrated impressive inhibition profiles against AChE and BChE and also inhibited both CAs at nanomolar level. These inhibitory effects were more powerful in all cases than the reference compounds used for all these enzymes. This study suggests that isatin Mannich bases P1-P3 are good candidate compounds especially for the development of new cholinesterase inhibitors since they were 2.2-5.9 times better inhibitors than clinically used drug Tacrine.

Authors+Show Affiliations

a Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Agri Ibrahim Cecen University , Agri , Turkey .b Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Ataturk University , Erzurum , Turkey .b Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Ataturk University , Erzurum , Turkey .c Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey .c Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey . d Department of Zoology, College of Science , King Saud University , Riyadh , Saudi Arabia .e Department of Biology, Faculty of Science , Agri Ibrahim Cecen University , Agri , Turkey , and.f Neurofarba Department e Laboratorio di Chimica Bioinorganica, Universita Degli Studi di Firenze , Sesto Fiorentino (Florence) , Italy.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

26928426

Citation

Ozgun, Dilan Ozmen, et al. "Inhibitory Effects of Isatin Mannich Bases On Carbonic Anhydrases, Acetylcholinesterase, and Butyrylcholinesterase." Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 31, no. 6, 2016, pp. 1498-501.
Ozgun DO, Yamali C, Gul HI, et al. Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase. J Enzyme Inhib Med Chem. 2016;31(6):1498-501.
Ozgun, D. O., Yamali, C., Gul, H. I., Taslimi, P., Gulcin, I., Yanik, T., & Supuran, C. T. (2016). Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase. Journal of Enzyme Inhibition and Medicinal Chemistry, 31(6), 1498-501. https://doi.org/10.3109/14756366.2016.1149479
Ozgun DO, et al. Inhibitory Effects of Isatin Mannich Bases On Carbonic Anhydrases, Acetylcholinesterase, and Butyrylcholinesterase. J Enzyme Inhib Med Chem. 2016;31(6):1498-501. PubMed PMID: 26928426.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase. AU - Ozgun,Dilan Ozmen, AU - Yamali,Cem, AU - Gul,Halise Inci, AU - Taslimi,Parham, AU - Gulcin,Ilhami, AU - Yanik,Telat, AU - Supuran,Claudiu T, Y1 - 2016/03/01/ PY - 2016/3/2/entrez PY - 2016/3/2/pubmed PY - 2017/3/7/medline KW - Acetylcholinesterase KW - Mannich bases KW - butyrylcholinesterase KW - carbonic anhydrase KW - isatin SP - 1498 EP - 501 JF - Journal of enzyme inhibition and medicinal chemistry JO - J Enzyme Inhib Med Chem VL - 31 IS - 6 N2 - The effects of isatin Mannich bases incorporating (1-[piperidin-1-yl (P1)/morpholin-4-yl (P2)/N-methylpiperazin-1-yl (P3)]methyl)-1H-indole-2,3-dione) moieties against human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoenzymes hCA I and hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes were evaluated. P1-P3 demonstrated impressive inhibition profiles against AChE and BChE and also inhibited both CAs at nanomolar level. These inhibitory effects were more powerful in all cases than the reference compounds used for all these enzymes. This study suggests that isatin Mannich bases P1-P3 are good candidate compounds especially for the development of new cholinesterase inhibitors since they were 2.2-5.9 times better inhibitors than clinically used drug Tacrine. SN - 1475-6374 UR - https://www.unboundmedicine.com/medline/citation/26928426/Inhibitory_effects_of_isatin_Mannich_bases_on_carbonic_anhydrases_acetylcholinesterase_and_butyrylcholinesterase_ L2 - http://www.tandfonline.com/doi/full/10.3109/14756366.2016.1149479 DB - PRIME DP - Unbound Medicine ER -