Target Oriented Selective Synthesis of Antibacterial Active Tyrosinase Enzyme Inhibitor Coumarin Core Derivatives

Kumbhar, Digambar R.; Patil, Reshma; Patil, Dayanand; Patravale, Ajinkya A.; Chandam, Dattatray; Jadhav, S. D.; Chavan, Dattatray; Choudhari, Prafulla; Bhatia, Manish S.; Deshmukh, M. B.

doi:10.5958/0974-4150.2015.00081.4

Cited by 4 publications

(3 citation statements)

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“…All the compounds were screened for their in vitro antibacterial activity and the results revealed that the compound 20 exhibited remarkable activity against S. aureus. Furthermore, it was established from docking studies that interactions with Arg 138 (or) Lys 36 in coumarin based thiazoles might play a pivotal role in binding of inhibitors to topoisomerase [67][68][69].…”

Section: Antibacterial Activitymentioning

confidence: 99%

Coumarin: A Valid Scaffold in Medicinal Chemistry

Surana¹,

Mahajan²,

Patil³

2021

JASR

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The coumarin scaffold is an important structure in medicinal chemistry because it is found in several naturally occurring molecules which exhibit a variety of biological activities, such as anti-cancer, anti-inflammatory, anti-diabetic, antimicrobial, and antiviral, antifungal. In addition, various synthetic coumarins motifs are present in marketed drugs. They are also involved in the actions of the photosynthesis, control of respiration, plant growth hormones and growth regulators, and also defense against infection. This review will provide an overview of coumarin moieties with medicinal aspects synthesized in the last 15 years and will cover the most potent molecule in each report. In this review, different synthesis methods of coumarin and their derivatives have been covered.

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Section: Antibacterial Activitymentioning

confidence: 99%

Coumarin: A Valid Scaffold in Medicinal Chemistry

Surana¹,

Mahajan²,

Patil³

2021

JASR

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“…Carbonic anhydrase (EC 4.2.1.1) is a metalloenzyme that occurs in many tissues of living organisms and has Zn +2 ion in its active site 17,18 . The most important task of this enzyme is to ensure that CO 2 formed in the cell is transported to other cells or excreted so that living cells can survive 19–21 .…”

Section: Introductionmentioning

confidence: 99%

“…Carbonic anhydrase (EC 4.2.1.1) is a metalloenzyme that occurs in many tissues of living organisms and has Zn +2 ion in its active site. 17,18 The most important task of this enzyme is to ensure that CO 2 formed in the cell is transported to other cells or excreted so that living cells can survive. [19][20][21] Since its other task is the transport of CO 2 , it provides the accumulation of H + and HCO 3 À in tissues (kidney, eye lens, erythrocytes, brain).…”

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confidence: 99%

Investigation of the effects of some pesticides on carbonic anhydrase isoenzymes

Baltacı

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Gençer

2023

J of Molecular Recognition

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The aim of this study was to investigate the inhibitory effects of some pesticides known to have harmful effects on human health on carbonic anhydrase isoenzymes. Therefore, carbonic anhydrase isoenzymes (hCA I and II) were purified from human erythrocytes. The isoenzymes were purified from human erythrocytes by using an affinity column that has the chemical structure of Sepharose‐4B‐4‐(6‐amino‐hexyloxy)‐benzenesulfonamide. The purity of the isoenzymes was checked by sodium dodecyl sulphate polyacrylamide gel electrophoresis (SDSPAGE). It was determined that the pesticides used in this study inhibit hCA I and hCA II isoenzymes at different levels in vitro. It was determined that the strongest inhibitor for the hCA I enzyme was Carbofuran (IC50:6.52 μM; Ki: 3.58 μM) and the weakest one was 1‐Naphtol (IC50:16.55 μM; Ki: 14.4 μM) among these pesticides. It was also found that the strongest inhibitor for the hCA II enzyme was coumatetralil (IC50:5.06 μM; Ki: 1.62 μM) and the weakest one was Dimethachlor (IC50 14.6 μM; Ki: 8.44 μM).

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