Literature DB >> 30769267

Synthesis, biological evaluation and molecular docking of novel pyrazole derivatives as potent carbonic anhydrase and acetylcholinesterase inhibitors.

Fikret Turkan1, Adnan Cetin2, Parham Taslimi3, Muhammet Karaman4, İlhami Gulçin5.   

Abstract

A series of substituted pyrazole compounds (1-8 and 9a, b) were synthesized and their structure was characterized by IR, NMR, and Mass analysis. These obtained novel pyrazole derivatives (1-8 and 9a, b) were emerged as effective inhibitors of the cytosolic carbonic anhydrase I and II isoforms (hCA I and II) and acetylcholinesterase (AChE) enzymes with Ki values in the range of 1.03 ± 0.23-22.65 ± 5.36 µM for hCA I, 1.82 ± 0.30-27.94 ± 4.74 µM for hCA II, and 48.94 ± 9.63-116.05 ± 14.95 µM for AChE, respectively. Docking studies were performed for the most active compounds, 2 and 5, and binding mode between the compounds and the receptors were determined.
Copyright © 2019. Published by Elsevier Inc.

Entities:  

Keywords:  Acetylcholinesterase; Carbonic anhydrase; Enzyme inhibition; Substituted pyrazole

Year:  2019        PMID: 30769267     DOI: 10.1016/j.bioorg.2019.02.013

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  10 in total

1.  Design, synthesis, in vivo and in vitro studies of 1,2,3,4-tetrahydro-9H-carbazole derivatives, highly selective and potent butyrylcholinesterase inhibitors.

Authors:  Roshanak Ghobadian; Roghaieh Esfandyari; Hamid Nadri; Alireza Moradi; Mohammad Mahdavi; Tahmineh Akbarzadeh; Hossein Khaleghzadeh-Ahangar; Najmeh Edraki; Mohammad Sharifzadeh; Mohsen Amini
Journal:  Mol Divers       Date:  2019-03-29       Impact factor: 2.943

2.  Inhibition effects of some pesticides and heavy metals on carbonic anhydrase enzyme activity purified from horse mackerel (Trachurus trachurus) gill tissues.

Authors:  Cuneyt Caglayan; Parham Taslimi; Cebrahil Türk; İlhami Gulcin; Fatih Mehmet Kandemir; Yeliz Demir; Şükrü Beydemir
Journal:  Environ Sci Pollut Res Int       Date:  2020-01-15       Impact factor: 4.223

3.  Co(II), Ni(II), and Zn(II) complexes based on new hybrid imine-pyrazole ligands: structural, spectroscopic, and electronic properties.

Authors:  Gabriel Rodrigues Martins; Cristiane Storck Schwalm; Cláudio Teodoro de Carvalho; Leandro Moreira de Campos Pinto
Journal:  J Mol Model       Date:  2022-05-21       Impact factor: 1.810

Review 4.  Emerging trends in environmental and industrial applications of marine carbonic anhydrase: a review.

Authors:  Sudabeh Iraninasab; Sana Sharifian; Ahmad Homaei; Mozafar Bagherzadeh Homaee; Tanvi Sharma; Ashok Kumar Nadda; John F Kennedy; Muhammad Bilal; Hafiz M N Iqbal
Journal:  Bioprocess Biosyst Eng       Date:  2021-11-25       Impact factor: 3.210

5.  Resveratrol Inhibits Pseudorabies Virus Replication by Targeting IE180 Protein.

Authors:  Xiangxiu Chen; Xu Song; Lixia Li; Yaqin Chen; Renyong Jia; Yuanfeng Zou; Hongping Wan; Ling Zhao; Huaqiao Tang; Cheng Lv; Xinghong Zhao; Zhongqiong Yin
Journal:  Front Microbiol       Date:  2022-06-02       Impact factor: 6.064

6.  Screening of Carbonic Anhydrase, Acetylcholinesterase, Butyrylcholinesterase, and α-Glycosidase Enzyme Inhibition Effects and Antioxidant Activity of Coumestrol.

Authors:  Lokman Durmaz; Adem Erturk; Mehmet Akyüz; Leyla Polat Kose; Eda Mehtap Uc; Zeynebe Bingol; Ruya Saglamtas; Saleh Alwasel; İlhami Gulcin
Journal:  Molecules       Date:  2022-05-11       Impact factor: 4.927

7.  Biochemical characterization of a novel azo reductase named BVU5 from the bacterial flora DDMZ1: application for decolorization of azo dyes.

Authors:  Junhao Cong; Xuehui Xie; Yanbiao Liu; Yan Qin; Jiao Fan; Yingrong Fang; Na Liu; Qingyun Zhang; Xinshan Song; Wolfgang Sand
Journal:  RSC Adv       Date:  2022-01-12       Impact factor: 3.361

8.  Identifying Possible AChE Inhibitors from Drug-like Molecules via Machine Learning and Experimental Studies.

Authors:  Trung Hai Nguyen; Phuong-Thao Tran; Ngoc Quynh Anh Pham; Van-Hai Hoang; Dinh Minh Hiep; Son Tung Ngo
Journal:  ACS Omega       Date:  2022-06-08

9.  Antioxidant, Antidiabetic, Anticholinergic, and Antiglaucoma Effects of Magnofluorine.

Authors:  Lokman Durmaz; Hatice Kiziltas; Leyla Guven; Hasan Karagecili; Saleh Alwasel; İlhami Gulcin
Journal:  Molecules       Date:  2022-09-11       Impact factor: 4.927

10.  The palladium-based complexes bearing 1,3-dibenzylbenzimidazolium with morpholine, triphenylphosphine, and pyridine derivate ligands: synthesis, characterization, structure and enzyme inhibitions.

Authors:  Aydın Aktaş; Gül Yakalı; Yeliz Demir; İlhami Gülçin; Muhittin Aygün; Yetkin Gök
Journal:  Heliyon       Date:  2022-09-16
  10 in total

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