In‐house chemical library repurposing: A case example for Pseudomonas aeruginosa antibiofilm activity and quorum sensing inhibition
Hit, Lead & Candidate Discovery Drug repurposing has become a recent trend in drug development programs, where previously developed drugs are explored for hit and redeveloped into potential therapeutic agents for new diseases. Globally, in any drug development program, a series of molecules are...
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| Veröffentlicht in: | Drug development research 2018-12, Vol.79 (8), p.383-390 |
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| creator | Ravithej Singh, L Tripathi, Vikash C. Raj, Sneha Kumar, Anoop Gupta, Sampa Horam, Soyar Upadhyay, Akanksha Kushwaha, Pragati Arockiaraj, Jesu Sashidhara, Koneni V. Pasupuleti, Mukesh |
| description | Hit, Lead & Candidate Discovery
Drug repurposing has become a recent trend in drug development programs, where previously developed drugs are explored for hit and redeveloped into potential therapeutic agents for new diseases. Globally, in any drug development program, a series of molecules are synthesized and evaluated for the hypothesized activity. Hits are developed into lead molecules or drugs, whereas the negative ones are shelved in the lab with no immediate use. We in this project took the previously sidelined small chemical molecules to the next level of utility, where previously developed in‐house small molecules library are tested for the unexplored biological relevant activity. As biofilm formation and quorum sensing play a vital role in bacterial pathogenesis, we believe that they could be one of the most effective targets for antimicrobial agents. In this study, we report the evaluation of 50 different compounds for anti‐biofilm and anti‐quorum sensing activity against Pseudomonas aeruginosa. Out of the screened compounds, three hydrazine‐carboxamide hybrid derivatives showed promising anti‐biofilm property and inhibition of pyocyanin production without any direct antimicrobial activity and cytotoxicity issues. Hydrazine‐carboxamide hybrids can be a new class and promising leads for further anti‐biofilm and anti‐virulence development against microbial infections. |
| doi_str_mv | 10.1002/ddr.21458 |
| format | Article |
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Drug repurposing has become a recent trend in drug development programs, where previously developed drugs are explored for hit and redeveloped into potential therapeutic agents for new diseases. Globally, in any drug development program, a series of molecules are synthesized and evaluated for the hypothesized activity. Hits are developed into lead molecules or drugs, whereas the negative ones are shelved in the lab with no immediate use. We in this project took the previously sidelined small chemical molecules to the next level of utility, where previously developed in‐house small molecules library are tested for the unexplored biological relevant activity. As biofilm formation and quorum sensing play a vital role in bacterial pathogenesis, we believe that they could be one of the most effective targets for antimicrobial agents. In this study, we report the evaluation of 50 different compounds for anti‐biofilm and anti‐quorum sensing activity against Pseudomonas aeruginosa. Out of the screened compounds, three hydrazine‐carboxamide hybrid derivatives showed promising anti‐biofilm property and inhibition of pyocyanin production without any direct antimicrobial activity and cytotoxicity issues. Hydrazine‐carboxamide hybrids can be a new class and promising leads for further anti‐biofilm and anti‐virulence development against microbial infections.</description><identifier>ISSN: 0272-4391</identifier><identifier>EISSN: 1098-2299</identifier><identifier>DOI: 10.1002/ddr.21458</identifier><identifier>PMID: 30291767</identifier><language>eng</language><publisher>United States: Wiley Subscription Services, Inc</publisher><subject>Anti-Bacterial Agents - pharmacology ; Antiinfectives and antibacterials ; Antimicrobial activity ; Antimicrobial agents ; anti‐biofilm ; Biofilms ; Biofilms - drug effects ; Biofilms - growth & development ; Biological activity ; Cell Line ; Chemical compounds ; chemical repurposing ; Chemical synthesis ; Cytotoxicity ; Detection ; Dose-Response Relationship, Drug ; Drug development ; Drug Repositioning - methods ; Drugs ; Humans ; Hybrids ; Hydrazine ; Hydrazines ; hydrazine‐carboxamide ; Inhibition ; in‐house chemical library ; Microbial Sensitivity Tests - methods ; Microorganisms ; Organic chemistry ; P. aeruginosa ; Pathogenesis ; Pharmacology ; Pseudomonas aeruginosa ; Pseudomonas aeruginosa - drug effects ; Pseudomonas aeruginosa - physiology ; Pyocyanin ; quorum sensing ; Quorum Sensing - drug effects ; Quorum Sensing - physiology ; Small Molecule Libraries - pharmacology ; Toxicity ; Virulence</subject><ispartof>Drug development research, 2018-12, Vol.79 (8), p.383-390</ispartof><rights>2018 Wiley Periodicals, Inc.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3538-ed58b1d7aee0b1e12ac948641cc4c214b7a202e53713cacbc187bd88a27a480c3</citedby><cites>FETCH-LOGICAL-c3538-ed58b1d7aee0b1e12ac948641cc4c214b7a202e53713cacbc187bd88a27a480c3</cites><orcidid>0000-0002-9589-0709 ; 0000-0001-6337-6257 ; 0000-0001-6369-380X</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fddr.21458$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fddr.21458$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1416,27922,27923,45572,45573</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/30291767$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ravithej Singh, L</creatorcontrib><creatorcontrib>Tripathi, Vikash C.</creatorcontrib><creatorcontrib>Raj, Sneha</creatorcontrib><creatorcontrib>Kumar, Anoop</creatorcontrib><creatorcontrib>Gupta, Sampa</creatorcontrib><creatorcontrib>Horam, Soyar</creatorcontrib><creatorcontrib>Upadhyay, Akanksha</creatorcontrib><creatorcontrib>Kushwaha, Pragati</creatorcontrib><creatorcontrib>Arockiaraj, Jesu</creatorcontrib><creatorcontrib>Sashidhara, Koneni V.</creatorcontrib><creatorcontrib>Pasupuleti, Mukesh</creatorcontrib><title>In‐house chemical library repurposing: A case example for Pseudomonas aeruginosa antibiofilm activity and quorum sensing inhibition</title><title>Drug development research</title><addtitle>Drug Dev Res</addtitle><description>Hit, Lead & Candidate Discovery
Drug repurposing has become a recent trend in drug development programs, where previously developed drugs are explored for hit and redeveloped into potential therapeutic agents for new diseases. Globally, in any drug development program, a series of molecules are synthesized and evaluated for the hypothesized activity. Hits are developed into lead molecules or drugs, whereas the negative ones are shelved in the lab with no immediate use. We in this project took the previously sidelined small chemical molecules to the next level of utility, where previously developed in‐house small molecules library are tested for the unexplored biological relevant activity. As biofilm formation and quorum sensing play a vital role in bacterial pathogenesis, we believe that they could be one of the most effective targets for antimicrobial agents. In this study, we report the evaluation of 50 different compounds for anti‐biofilm and anti‐quorum sensing activity against Pseudomonas aeruginosa. Out of the screened compounds, three hydrazine‐carboxamide hybrid derivatives showed promising anti‐biofilm property and inhibition of pyocyanin production without any direct antimicrobial activity and cytotoxicity issues. Hydrazine‐carboxamide hybrids can be a new class and promising leads for further anti‐biofilm and anti‐virulence development against microbial infections.</description><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Antiinfectives and antibacterials</subject><subject>Antimicrobial activity</subject><subject>Antimicrobial agents</subject><subject>anti‐biofilm</subject><subject>Biofilms</subject><subject>Biofilms - drug effects</subject><subject>Biofilms - growth & development</subject><subject>Biological activity</subject><subject>Cell Line</subject><subject>Chemical compounds</subject><subject>chemical repurposing</subject><subject>Chemical synthesis</subject><subject>Cytotoxicity</subject><subject>Detection</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug development</subject><subject>Drug Repositioning - methods</subject><subject>Drugs</subject><subject>Humans</subject><subject>Hybrids</subject><subject>Hydrazine</subject><subject>Hydrazines</subject><subject>hydrazine‐carboxamide</subject><subject>Inhibition</subject><subject>in‐house chemical library</subject><subject>Microbial Sensitivity Tests - methods</subject><subject>Microorganisms</subject><subject>Organic chemistry</subject><subject>P. aeruginosa</subject><subject>Pathogenesis</subject><subject>Pharmacology</subject><subject>Pseudomonas aeruginosa</subject><subject>Pseudomonas aeruginosa - drug effects</subject><subject>Pseudomonas aeruginosa - physiology</subject><subject>Pyocyanin</subject><subject>quorum sensing</subject><subject>Quorum Sensing - drug effects</subject><subject>Quorum Sensing - physiology</subject><subject>Small Molecule Libraries - pharmacology</subject><subject>Toxicity</subject><subject>Virulence</subject><issn>0272-4391</issn><issn>1098-2299</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp10cFKHTEUBuAgLXprXfgCEnDTLkZzksxMxp1oq4LQUtr1kMmc643MJGMysb27brrvM_ZJGnvVhdBVIHz8HP6fkH1gR8AYP-77cMRBlmqLLIA1quC8aV6RBeM1L6RoYIe8ifGWMQCp1DbZEYw3UFf1gvy6cn9-_l75FJGaFY7W6IEOtgs6rGnAKYXJR-tuTugpNToj_KHHaUC69IF-jph6P3qnI9UY0o11Pmqq3Ww765d2GKk2s7238zp_9vQu-ZBGGtE9RFLrVtnN1ru35PVSDxH3Ht9d8u3jh69nl8X1p4urs9PrwohSqAL7UnXQ1xqRdYDAtWmkqiQYI00uoKs1ZxxLUYMw2nQGVN31Smlea6mYEbvk3SZ3Cv4uYZzb0UaDw6Ad5gpaDlApWZVKZHr4gt76FFy-LquykkI0gmX1fqNM8DEGXLZTsGPurgXWPmzT5m3af9tke_CYmLoR-2f5NEYGxxvw3Q64_n9Se37-ZRP5Fxiem8Y</recordid><startdate>201812</startdate><enddate>201812</enddate><creator>Ravithej Singh, L</creator><creator>Tripathi, Vikash C.</creator><creator>Raj, Sneha</creator><creator>Kumar, Anoop</creator><creator>Gupta, Sampa</creator><creator>Horam, Soyar</creator><creator>Upadhyay, Akanksha</creator><creator>Kushwaha, Pragati</creator><creator>Arockiaraj, Jesu</creator><creator>Sashidhara, Koneni V.</creator><creator>Pasupuleti, Mukesh</creator><general>Wiley Subscription Services, Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0002-9589-0709</orcidid><orcidid>https://orcid.org/0000-0001-6337-6257</orcidid><orcidid>https://orcid.org/0000-0001-6369-380X</orcidid></search><sort><creationdate>201812</creationdate><title>In‐house chemical library repurposing: A case example for Pseudomonas aeruginosa antibiofilm activity and quorum sensing inhibition</title><author>Ravithej Singh, L ; Tripathi, Vikash C. ; Raj, Sneha ; Kumar, Anoop ; Gupta, Sampa ; Horam, Soyar ; Upadhyay, Akanksha ; Kushwaha, Pragati ; Arockiaraj, Jesu ; Sashidhara, Koneni V. ; Pasupuleti, Mukesh</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3538-ed58b1d7aee0b1e12ac948641cc4c214b7a202e53713cacbc187bd88a27a480c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>Anti-Bacterial Agents - pharmacology</topic><topic>Antiinfectives and antibacterials</topic><topic>Antimicrobial activity</topic><topic>Antimicrobial agents</topic><topic>anti‐biofilm</topic><topic>Biofilms</topic><topic>Biofilms - drug effects</topic><topic>Biofilms - growth & development</topic><topic>Biological activity</topic><topic>Cell Line</topic><topic>Chemical compounds</topic><topic>chemical repurposing</topic><topic>Chemical synthesis</topic><topic>Cytotoxicity</topic><topic>Detection</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug development</topic><topic>Drug Repositioning - methods</topic><topic>Drugs</topic><topic>Humans</topic><topic>Hybrids</topic><topic>Hydrazine</topic><topic>Hydrazines</topic><topic>hydrazine‐carboxamide</topic><topic>Inhibition</topic><topic>in‐house chemical library</topic><topic>Microbial Sensitivity Tests - methods</topic><topic>Microorganisms</topic><topic>Organic chemistry</topic><topic>P. aeruginosa</topic><topic>Pathogenesis</topic><topic>Pharmacology</topic><topic>Pseudomonas aeruginosa</topic><topic>Pseudomonas aeruginosa - drug effects</topic><topic>Pseudomonas aeruginosa - physiology</topic><topic>Pyocyanin</topic><topic>quorum sensing</topic><topic>Quorum Sensing - drug effects</topic><topic>Quorum Sensing - physiology</topic><topic>Small Molecule Libraries - pharmacology</topic><topic>Toxicity</topic><topic>Virulence</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ravithej Singh, L</creatorcontrib><creatorcontrib>Tripathi, Vikash C.</creatorcontrib><creatorcontrib>Raj, Sneha</creatorcontrib><creatorcontrib>Kumar, Anoop</creatorcontrib><creatorcontrib>Gupta, Sampa</creatorcontrib><creatorcontrib>Horam, Soyar</creatorcontrib><creatorcontrib>Upadhyay, Akanksha</creatorcontrib><creatorcontrib>Kushwaha, Pragati</creatorcontrib><creatorcontrib>Arockiaraj, Jesu</creatorcontrib><creatorcontrib>Sashidhara, Koneni V.</creatorcontrib><creatorcontrib>Pasupuleti, Mukesh</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Toxicology Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Drug development research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ravithej Singh, L</au><au>Tripathi, Vikash C.</au><au>Raj, Sneha</au><au>Kumar, Anoop</au><au>Gupta, Sampa</au><au>Horam, Soyar</au><au>Upadhyay, Akanksha</au><au>Kushwaha, Pragati</au><au>Arockiaraj, Jesu</au><au>Sashidhara, Koneni V.</au><au>Pasupuleti, Mukesh</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In‐house chemical library repurposing: A case example for Pseudomonas aeruginosa antibiofilm activity and quorum sensing inhibition</atitle><jtitle>Drug development research</jtitle><addtitle>Drug Dev Res</addtitle><date>2018-12</date><risdate>2018</risdate><volume>79</volume><issue>8</issue><spage>383</spage><epage>390</epage><pages>383-390</pages><issn>0272-4391</issn><eissn>1098-2299</eissn><abstract>Hit, Lead & Candidate Discovery
Drug repurposing has become a recent trend in drug development programs, where previously developed drugs are explored for hit and redeveloped into potential therapeutic agents for new diseases. Globally, in any drug development program, a series of molecules are synthesized and evaluated for the hypothesized activity. Hits are developed into lead molecules or drugs, whereas the negative ones are shelved in the lab with no immediate use. We in this project took the previously sidelined small chemical molecules to the next level of utility, where previously developed in‐house small molecules library are tested for the unexplored biological relevant activity. As biofilm formation and quorum sensing play a vital role in bacterial pathogenesis, we believe that they could be one of the most effective targets for antimicrobial agents. In this study, we report the evaluation of 50 different compounds for anti‐biofilm and anti‐quorum sensing activity against Pseudomonas aeruginosa. Out of the screened compounds, three hydrazine‐carboxamide hybrid derivatives showed promising anti‐biofilm property and inhibition of pyocyanin production without any direct antimicrobial activity and cytotoxicity issues. Hydrazine‐carboxamide hybrids can be a new class and promising leads for further anti‐biofilm and anti‐virulence development against microbial infections.</abstract><cop>United States</cop><pub>Wiley Subscription Services, Inc</pub><pmid>30291767</pmid><doi>10.1002/ddr.21458</doi><tpages>8</tpages><orcidid>https://orcid.org/0000-0002-9589-0709</orcidid><orcidid>https://orcid.org/0000-0001-6337-6257</orcidid><orcidid>https://orcid.org/0000-0001-6369-380X</orcidid></addata></record> |
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| ispartof | Drug development research, 2018-12, Vol.79 (8), p.383-390 |
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| subjects | Anti-Bacterial Agents - pharmacology Antiinfectives and antibacterials Antimicrobial activity Antimicrobial agents anti‐biofilm Biofilms Biofilms - drug effects Biofilms - growth & development Biological activity Cell Line Chemical compounds chemical repurposing Chemical synthesis Cytotoxicity Detection Dose-Response Relationship, Drug Drug development Drug Repositioning - methods Drugs Humans Hybrids Hydrazine Hydrazines hydrazine‐carboxamide Inhibition in‐house chemical library Microbial Sensitivity Tests - methods Microorganisms Organic chemistry P. aeruginosa Pathogenesis Pharmacology Pseudomonas aeruginosa Pseudomonas aeruginosa - drug effects Pseudomonas aeruginosa - physiology Pyocyanin quorum sensing Quorum Sensing - drug effects Quorum Sensing - physiology Small Molecule Libraries - pharmacology Toxicity Virulence |
| title | In‐house chemical library repurposing: A case example for Pseudomonas aeruginosa antibiofilm activity and quorum sensing inhibition |
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