Synthesis, carbonic anhydrase inhibitory activity and antioxidant activity of some 1,3-oxazine derivatives

2018 ◽  
Vol 79 (7) ◽  
pp. 352-361 ◽  
Author(s):  
Rabia Qamar ◽  
Aamer Saeed ◽  
Maria Saeed ◽  
Zaman Ashraf ◽  
Qamar Abbas ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Oxazine Derivatives

scholarly journals In vitro activities of Acacia nilotica (L.) Delile bark fractions against Oral Bacteria, Glucosyltransferase and as antioxidant

2020 ◽  
Vol 20 (1) ◽  
Author(s):  
Ali Mahmoud Muddathir ◽  
Ebtihal Abdalla M. Mohieldin ◽  
Tohru Mitsunaga
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Gallic Acid ◽  
Crude Extract ◽  
Inhibitory Activity ◽  
Oral Bacteria ◽  
Acacia Nilotica ◽  
Assay Method ◽  
Medicinal Uses ◽  
Wide Range

Abstract Background Dental caries and periodontal disease are the most common chronic infectious oral diseases in the world. Acacia nilotica was commonly known in Sudan as Garad or Sunt has a wide range of medicinal uses. In the present study, antibacterial activity of oral bacteria (Streptococcus sobrinus and Porphyromonas gingivalis), inhibitory activity against glucosyltransferase (GTF) enzyme and antioxidant activity were assayed for methanolic crude extract of A. nilotica bark and its fractions. Methods Methanoilc crude extract of A. nilotica bark was applied to a Sephadex LH-20 column and eluted with methanol, aqueous methanol, and finally aqueous acetone to obtain four fractions (Fr1- Fr4). Furthermore, the crude extract and fractions were subjected to analytical high performance liquid chromatography (HPLC). The crude extract and its fractions were assayed for antibacterial activity against S. sobrinus and P. gingivalis using a microplate dilution assay method to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC), as well as GTF inhibition and antioxidant activity using ABTS radical scavenging method. Results Fractions (Fr1 and Fr2) exhibited MIC values of 0.3 mg/ml against the P. gingivalis. Additionally, Fr2 displayed MBC value of 1 mg/ml against two types of bacteria. Fr4 showed an especially potent GTF inhibitory activity with IC50 value of 3.9 μg/ml. Fr1 displayed the best antioxidant activity with IC50 value of 1.8 μg/ml. The main compound in Fr1 was identified as gallic acid, and Fr2 was mostly a mixture of gallic acid and methyl gallate. Conclusions The results obtained in this study provide some scientific rationale and justify the use of this plant for the treatment of dental diseases in traditional medicine. A. nilotica bark, besides their antibacterial potentiality and GTF inhibitory activity, it may be used as adjuvant antioxidants in mouthwashes. Further studies in the future are required to identify the rest of the active compounds.

scholarly journals Antioxidant activity, xanthine oxidase inhibitory activity, and compounds determination of Cipadessa baccifera leaf extract

2021 ◽  
Author(s):  
Syarifah Ramadhani Lubis ◽  
Subandi Subandi ◽  
Muntholib Muntholib ◽  
Jamilah Abbas ◽  
Tjandrawati Mozef
Keyword(s):  
Antioxidant Activity ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Leaf Extract

scholarly journals Synthesis and carbonic anhydrase I, II, IX and XII inhibitory activity of sulfamates incorporating piperazinyl-ureido moieties

2015 ◽  
Vol 23 (17) ◽  
pp. 5619-5625 ◽  
Author(s):  
Cenzo Congiu ◽  
Valentina Onnis ◽  
Alessandro Deplano ◽  
Gianfranco Balboni ◽  
Mariangela Ceruso ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Carbonic Anhydrase I

scholarly journals Again about carbonic anhydrase inhibitors: modern aspects of the use of ICA in ophthalmology

2021 ◽  
Vol 9 (2) ◽  
pp. 64-71
Author(s):  
P.A. Bezdetko
Keyword(s):  
Antioxidant Activity ◽  
Intraocular Pressure ◽  
Optic Nerve ◽  
Carbonic Anhydrase ◽  
Macular Edema ◽  
Mechanism Of Action ◽  
Corneal Endothelium ◽  
Complex Treatment ◽  
Efficacy And Safety ◽  
Carbonic Anhydrase Inhibitors

For more than 70 years, the inhibitors of carbonic anhydrase (ICA) have been used in the treatment of glaucoma. Since 1995, topical forms of ICA have appeared among antiglaucoma drugs — dorzolamide, and since 1999 — brinzolamide. The hypotensive efficacy and safety of topical ICA gave rise to the widespread use of these drugs in the treatment of various forms of glaucoma. The peculiarities of the mechanism of action made it possible to create on their basis effective fixed combinations, which allow reducing the intraocular pressure by up to 40 % in patients with glaucoma. The attractiveness of the drug has expanded due to the effect of ICA on various tissues of the organ of vision. Thus, ICAs effectively improve the hemodynamics of the eye and optic nerve. The antioxidant activity of the drug makes it possible to expand the indications for its use in patients with vascular patho-logy of the retina and optic nerve. The biomechanical characte-ristics of the drug allowed its effective and safe use in the complex treatment of macular edema of various etiologies. The adjuvant use of topical ICAs expands the possibilities of anti-VEGF therapy in the treatment of macular edema of various etiologies. Features of the action of ICA on the endothelial pump function of the cornea made it possible to formulate the rules for the use of topical ICA in patients with an insufficient function of the corneal endothelium.

scholarly journals Synthesis, Crystal Structure, Inhibitory Activity and Molecular Docking of Coumarins/Sulfonamides Containing Triazolyl Pyridine Moiety as Potent Selective Carbonic Anhydrase IX and XII Inhibitors

Crystals ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 1076
Author(s):  
Yassine Aimene ◽  
Romain Eychenne ◽  
Frédéric Rodriguez ◽  
Sonia Mallet-Ladeira ◽  
Nathalie Saffon-Merceron ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Cancer Drug ◽  
Drug Candidate ◽  
Coumarin Derivatives ◽  
X Ray Diffraction ◽  
Rhenium Complex ◽  
Pyridine Moiety ◽  
Docking Calculations

In this work, two classes of Carbonic Anhydrase (CA) inhibitors, sulfonamide and coumarin derivatives linked to pyta moiety (2a-b) and their corresponding rhenium complexes (3a-b), were designed. These compounds were synthesized and fully characterized by classical analytical methods and X-ray diffraction. All the synthesized compounds were evaluated for their inhibitory activity against the hCA isoforms I, II, IX and XII. They exhibited high inhibitory activities in the range of nanomolar for both hCA IX and hCA XII isoforms. The sulfonamide compound 2a showed the strongest inhibition against the tumour-associated hCA IX isoform with a Ki of 11.7 nM. The tumour-associated isoforms hCA IX and hCA XII were selectively inhibited by all the coumarin derivatives, with inhibition constants ranging from 12.7 nM (2b) to 44.5 nM (3b), while the hCA I and II isoforms were slightly inhibited (in the micromolar range), as expected. In terms of selectivity, compared to previously published rhenium complex-based CA inhibitors, complex 3b showed one of the highest selectivities against hCA IX and hCA XII compared to the off-target isoforms hCA I and hCA II, making it a potential anti-cancer drug candidate. Molecular docking calculations were performed to investigate the inhibition profiles of the investigated compounds at the tumour-associated hCA IX active site and to rationalize our results.

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