Antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant ESKAPE clinical pathogens
The synthesis of a new class of effective antibiotics and antimicrobial agents with less toxicity is highly desirable due to bacterial resistance to antibiotics has increased dramatically. In this context, molecules that embedding a spiro moiety are attractive from a medicinal chemistry point of vie...
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Elsevier
2024-01-01
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Series: | Journal of King Saud University: Science |
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Online Access: | http://www.sciencedirect.com/science/article/pii/S1018364723004585 |
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author | Natarajan Arumugam Khloud Ibrahim Al-Shemaimari Mohammad Altaf Karuppiah Ponmurugan Dhanaraj Premnath Sinouvassane Djearamane Ling Shing Wong Saminathan Kayarohanam |
author_facet | Natarajan Arumugam Khloud Ibrahim Al-Shemaimari Mohammad Altaf Karuppiah Ponmurugan Dhanaraj Premnath Sinouvassane Djearamane Ling Shing Wong Saminathan Kayarohanam |
author_sort | Natarajan Arumugam |
collection | DOAJ |
description | The synthesis of a new class of effective antibiotics and antimicrobial agents with less toxicity is highly desirable due to bacterial resistance to antibiotics has increased dramatically. In this context, molecules that embedding a spiro moiety are attractive from a medicinal chemistry point of view as these spiro heterocycles show a vital part in the development of delivery systems for antimicrobial therapies. In the present study, the synthesis and antimicrobial evaluation of structurally attractive complex hybrid heterocycles comprising spriooxindolopyrrolidine and indole heterocycles was attained in quantitative yields by cycloaddition strategy. The new class of spirocompouds were unequivocally assigned through spectroscopic analysis and the antimicrobial efficacy were assessed against six microbial pathogens. Among them, compound 4a, bearing chlorine substituted derivative showed significant activity against tested ESKAPE pathogens. The maximum zone of inhibition observed against ESKAPE microbial pathogens causing infectious disease ranged from 6.75 ± 0.40 to 19.75 ± 1.15 mm, with MIC values ranging between 16.00 to > 256.00 µg/ml . |
first_indexed | 2024-03-11T07:33:32Z |
format | Article |
id | doaj.art-0a3e2875a6c243b2b701f21ed9b7e89f |
institution | Directory Open Access Journal |
issn | 1018-3647 |
language | English |
last_indexed | 2024-03-11T07:33:32Z |
publishDate | 2024-01-01 |
publisher | Elsevier |
record_format | Article |
series | Journal of King Saud University: Science |
spelling | doaj.art-0a3e2875a6c243b2b701f21ed9b7e89f2023-11-17T05:25:23ZengElsevierJournal of King Saud University: Science1018-36472024-01-01361102996Antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant ESKAPE clinical pathogensNatarajan Arumugam0Khloud Ibrahim Al-Shemaimari1Mohammad Altaf2Karuppiah Ponmurugan3Dhanaraj Premnath4Sinouvassane Djearamane5Ling Shing Wong6Saminathan Kayarohanam7Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia; Corresponding authors.Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi ArabiaDepartment of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi ArabiaDepartment of Botany and Microbiology, College of Science, P.O. Box 2455, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Biotechnology, Karunya Institute of Technology and Sciences, Coimbatore, Tamil Nadu, IndiaBiomedical Research Unit and Lab Animal Research Centre, Saveetha Dental College, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai 602 105, India; Faculty of Science, Universiti Tunku Abdul Rahman, Jalan Universiti, Bandar Barat, Kampar 31900, Malaysia; Corresponding authors.Faculty of Health and Life Sciences, INTI International University, Nilai 71800, MalaysiaFaculty of Bioeconomics and Health Sciences, Geomatika University Malaysia, Kuala Lumpur 54200, MalaysiaThe synthesis of a new class of effective antibiotics and antimicrobial agents with less toxicity is highly desirable due to bacterial resistance to antibiotics has increased dramatically. In this context, molecules that embedding a spiro moiety are attractive from a medicinal chemistry point of view as these spiro heterocycles show a vital part in the development of delivery systems for antimicrobial therapies. In the present study, the synthesis and antimicrobial evaluation of structurally attractive complex hybrid heterocycles comprising spriooxindolopyrrolidine and indole heterocycles was attained in quantitative yields by cycloaddition strategy. The new class of spirocompouds were unequivocally assigned through spectroscopic analysis and the antimicrobial efficacy were assessed against six microbial pathogens. Among them, compound 4a, bearing chlorine substituted derivative showed significant activity against tested ESKAPE pathogens. The maximum zone of inhibition observed against ESKAPE microbial pathogens causing infectious disease ranged from 6.75 ± 0.40 to 19.75 ± 1.15 mm, with MIC values ranging between 16.00 to > 256.00 µg/ml .http://www.sciencedirect.com/science/article/pii/S1018364723004585Multidrug resistantESKAPE pathogensSpiropyrrolidinesCycloaddition reactionHuman health |
spellingShingle | Natarajan Arumugam Khloud Ibrahim Al-Shemaimari Mohammad Altaf Karuppiah Ponmurugan Dhanaraj Premnath Sinouvassane Djearamane Ling Shing Wong Saminathan Kayarohanam Antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant ESKAPE clinical pathogens Journal of King Saud University: Science Multidrug resistant ESKAPE pathogens Spiropyrrolidines Cycloaddition reaction Human health |
title | Antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant ESKAPE clinical pathogens |
title_full | Antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant ESKAPE clinical pathogens |
title_fullStr | Antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant ESKAPE clinical pathogens |
title_full_unstemmed | Antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant ESKAPE clinical pathogens |
title_short | Antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant ESKAPE clinical pathogens |
title_sort | antimicrobial evaluation of spirooxindolopyrrolidine engrafted indoles against multidrug resistant eskape clinical pathogens |
topic | Multidrug resistant ESKAPE pathogens Spiropyrrolidines Cycloaddition reaction Human health |
url | http://www.sciencedirect.com/science/article/pii/S1018364723004585 |
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