Literature DB >> 29190478

Sulfonamides containing curcumin scaffold: Synthesis, characterization, carbonic anhydrase inhibition and molecular docking studies.

Mahmood Ahmed1, Muhammad Abdul Qadir2, Abdul Hameed3, Muhammad Nadeem Arshad4, Abdullah M Asiri4, Muhammad Muddassar5.   

Abstract

Curcumin is a multi-functional pharmacologically safe natural agent with proven cytoprotective effects to healthy human cells. In this study, a new series of sulfonamides with curcumin scaffold were synthesized, characterized and investigated for their carbonic anhydrase isoenzyme I (human) and II (bovine) isoforms. The structures of newly synthesized compounds were described by IR, 1H NMR and 13C NMR spectral data. Compound 14 showed the Ki value of 0.99 µM with highest inhibitory activity among all other synthesized compounds against hCA-I enzyme. Similarly enzyme kinetic studies of compound 14, 16 and 30 against bCAII enzyme showed Ki values of 0.71, 0.67 and 0.71 µM respectively. Our biological assays results showed that most of active compounds have similar inhibitory activities compared to standard acetazolamide drug. The molecular docking predicted binding modes showed that these compounds bind with hCA-1 enzyme in similar fashion.
Copyright © 2017 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Carbonic anhydrase; Curcumin; Molecular docking; Sulfonamides

Mesh:

Substances:

Year:  2017        PMID: 29190478     DOI: 10.1016/j.bioorg.2017.11.015

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


  3 in total

1.  Folic acid-sulfonamide conjugates as antibacterial agents: design, synthesis and molecular docking studies.

Authors:  Shabnam Shahzad; Muhammad Abdul Qadir; Mahmood Ahmed; Saghir Ahmad; Muhammad Jadoon Khan; Asad Gulzar; Muhammad Muddassar
Journal:  RSC Adv       Date:  2020-11-25       Impact factor: 4.036

2.  Molecular modeling piloted analysis for semicarbazone derivative of curcumin as a potent Abl-kinase inhibitor targeting colon cancer.

Authors:  Fiona C Rodrigues; Gangadhar Hari; K S R Pai; Akhil Suresh; Usha Y Nayak; N V Anilkumar; Goutam Thakur
Journal:  3 Biotech       Date:  2021-11-22       Impact factor: 2.406

3.  Microwave (MW), Ultrasound (US) and Combined Synergic MW-US Strategies for Rapid Functionalization of Pharmaceutical Use Phenols.

Authors:  Anna Pawełczyk; Katarzyna Sowa-Kasprzak; Dorota Olender; Lucjusz Zaprutko
Journal:  Molecules       Date:  2018-09-15       Impact factor: 4.411

  3 in total

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