<?xml version="1.0" encoding="UTF-8"?> <!DOCTYPE article PUBLIC "-//NLM//DTD JATS (Z39.96) Journal Publishing DTD v1.2d1 20170631//EN" "JATS-journalpublishing1.dtd"> <ArticleSet> <Article> <Journal> <PublisherName>isfcppharmaspire</PublisherName> <JournalTitle>Pharmaspire</JournalTitle> <PISSN>C</PISSN> <EISSN>o</EISSN> <Volume-Issue>Volume 13, Issue 3</Volume-Issue> <PartNumber/> <IssueTopic>Multidisciplinary</IssueTopic> <IssueLanguage>English</IssueLanguage> <Season>July - September, 2021</Season> <SpecialIssue>N</SpecialIssue> <SupplementaryIssue>N</SupplementaryIssue> <IssueOA>Y</IssueOA> <PubDate> <Year>2022</Year> <Month>06</Month> <Day>7</Day> </PubDate> <ArticleType>Pharmaceutics</ArticleType> <ArticleTitle>Design, synthesis, and antibacterial evaluation of arylidene derivatives of rhodanine-3-hexanoic acid</ArticleTitle> <SubTitle/> <ArticleLanguage>English</ArticleLanguage> <ArticleOA>Y</ArticleOA> <FirstPage>122</FirstPage> <LastPage>127</LastPage> <AuthorList> <Author> <FirstName>Abhishek Kumar</FirstName> <LastName>Yadav</LastName> <AuthorLanguage>English</AuthorLanguage> <Affiliation/> <CorrespondingAuthor>N</CorrespondingAuthor> <ORCID/> <FirstName>Gurpreet</FirstName> <LastName>Singh</LastName> <AuthorLanguage>English</AuthorLanguage> <Affiliation/> <CorrespondingAuthor>Y</CorrespondingAuthor> <ORCID/> <FirstName>Vikramdeep</FirstName> <LastName>Monga</LastName> <AuthorLanguage>English</AuthorLanguage> <Affiliation/> <CorrespondingAuthor>Y</CorrespondingAuthor> <ORCID/> </Author> </AuthorList> <DOI/> <Abstract>Background: Due to the development of resistance to various traditional antibacterial medications, bacterial infections represents a significant problem for healthcare professionals. Thus, there are unsatisfactory medical requirements for new bacteria and bacterial infections. Rationale: Rhodanine derivatives substituted with carboxyalkyl acid moiety have been reported to possess potent antimicrobial activity through a novel mechanism. However, their antibacterial potential has not been completely explored. Results: Therefore, in the present study, series of rhodanine-3-hexanoic acid derivatives bearing hydroxyl substituted benzylidene moiety at the C-5 position of the rhodanine core were synthesized through Knoevenagel condensation of rhodanine-3-hexanoic acid with various hydroxyl substituted aromatic aldehydes. All the compounds were structurally characterized and evaluated in vitro for their antibacterial activity against two Gram-positive and two Gram-negative bacterial strains. Conclusion: Biological data showed that synthesized derivatives exhibited potent to moderate antibacterial activity against the tested bacterial strains. The lead identified in the present study can be further explored for the design of potent antimicrobial agents.</Abstract> <AbstractLanguage>English</AbstractLanguage> <Keywords>2-thiazolidine-4-one, antibacterial activity, antimicrobial activity, rhodanine</Keywords> <URLs> <Abstract>https://isfcppharmaspire.com/ubijournal-v1copy/journals/abstract.php?article_id=13783&title=Design, synthesis, and antibacterial evaluation of arylidene derivatives of rhodanine-3-hexanoic acid</Abstract> </URLs> <References> <ReferencesarticleTitle>References</ReferencesarticleTitle> <ReferencesfirstPage>16</ReferencesfirstPage> <ReferenceslastPage>19</ReferenceslastPage> <References>1. Frieri M, Kumar K, Boutin A. Antibiotic resistance. J Infect Public Health 2017;10:369-78. 2. Velez R, Sloand E. Combating antibiotic resistance, mitigating future threats and ongoing initiatives. J Clin Nurs 2016;25:1886-9. 3. Akova M. Epidemiology of antimicrobial resistance in bloodstream infections. Virulence 2016;7:252-66. 4. Mand;uuml;hlen S, Dersch P. Anti-virulence strategies to target bacterial infections. In: How to Overcome the Antibiotic Crisis. Berlin, Germany: Springer; 2015. p. 147-83. 5. Chellat MF, Ragu z L, Riedl R. Targeting antibiotic resistance. Angew Chem Int Ed Engl 2016;55:6600-26. 6. Jiang H, Zhang WJ, Li PH, Wang J, Dong CJ, Zhang K, et al. Synthesis and biological evaluation of novel carbazole-rhodanine conjugates as topoisomerase II inhibitors. Bioorg Med Chem Lett 2018;28:1320-3. 7. Liu J, Wu Y, Piao H, Zhao X, Zhang W, Wang Y, et al. A comprehensive review on the biological and pharmacological activities of rhodanine based compounds for research and development of drugs. Mini Rev Med Chem 2018; 18:948. 8. Kaminskyy D, Kryshchyshyn A, Lesyk R. Recent developments with rhodanine as a scaffold for drug discovery. Expert Opin Drug Discov 2017; 12:1233. 9. Lesyk RB, Zimenkovsky BS. 4-thiazolidones: Centenarian history, current status and perspectives for modern organic and medicinal chemistry. Curr Org Chem 2004;8:1547-77. 10. Krand;aacute;tkand;yacute; M, Vinand;scaron;ovand;aacute; J, Stolarand;iacute;kovand;aacute; J. Antimicrobial activity of rhodanine-3-acetic acid derivatives. Bioorg Med Chem 2017;25:1839-45. 11. Xu LL, Zheng CJ, Sun LP, Miao J, Piao HR. Synthesis of novel 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties as potential antibacterial agents. Eur J Med Chem 2012;48:174-8. 12. Miao J, Zheng CJ, Sun LP, Song MX, Xu LL, Piao HR. Synthesis and potential antibacterial activity of new rhodanine-3-acetic acid derivatives. Med Chem Res 2013;22:4125-32. 13. Patel BA, Ashby CR Jr., Hardej D, Talele TT. The synthesis and SAR study of phenylalanine-derived (Z)-5-arylmethylidene rhodanines as anti-methicillinresistant Staphylococcus aureus (MRSA) compounds. Bioorg Med Chem Lett 2013;23:5523-7. 14. Arora N, Devi V, Monga V. Antibacterial properties of new 5-substituted derivatives of rhodanine-3-propanoic acid. Pharmaspire 2020;12:6-10. 15. Rattan A. Antimicrobials in Laboratory Medicine. New Delhi: Churchill Livingstone; 2000. p. 85-108.</References> </References> </Journal> </Article> </ArticleSet>