Synthesis of acetamidosulfonamide derivatives with antioxidative and QSAR studies

A series of sixteen acetamidosulfonamide derivatives (1-16) have been synthesized and investigated for their antioxidant (radical scavenging and superoxide dismutase (SOD)) and antimicrobial activities. Most compounds exhibited antioxidant activities in which compound 15 displayed the most potent ra...

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Bibliographic Details
Main Authors: Apilak Worachartcheewan, Somchai Pisutjaroenpong, Ratchanok Pingaew, Supaluk Prachayasittikul, Suphakit Siriwong, Somsak Ruchirawat, Virapong Prachayasittikul
Format: Article
Language:English
Published: IfADo - Leibniz Research Centre for Working Environment and Human Factors, Dortmund 2022-02-01
Series:EXCLI Journal : Experimental and Clinical Sciences
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Online Access:https://www.excli.de/index.php/excli/article/view/4590
Description
Summary:A series of sixteen acetamidosulfonamide derivatives (1-16) have been synthesized and investigated for their antioxidant (radical scavenging and superoxide dismutase (SOD)) and antimicrobial activities. Most compounds exhibited antioxidant activities in which compound 15 displayed the most potent radical scavenging and SOD activities. Quantitative structure-activity relationship (QSAR) has been studied using multiple linear regression. The constructed QSAR models displayed high correlation coefficient (Q2/Loo-CV= 0.9708 and 0.8753 for RSA and SOD activities, respectively), but low root mean square error (RMSELOO-CV = 0.5105 and 1.3571 for RSA and SOD activities, respectively). The structure-activity relationship showed that an ethylene group connected to pyridine ring provided significant antioxidant activities. The QSAR models give insight into the rational designed of eighty new sulfonamides with various electron donating and withdrawing groups. The top five new designed sulfonamides with nitro group are potential antioxidants to be further developed for medicinal applications.
ISSN:1611-2156