Evolution of anti-HIV drug candidates. Part 1: From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU)
Stemming from work on a previous clinical candidate, loviride, and other α-APA derivatives, a new series of potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been synthesized. The ITU analogues, which contain a unique diarylated imidoyl thiourea, are very active in inhibiting both...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2001-09, Vol.11 (17), p.2225-2228 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Ludovici, Donald W. Kukla, Michael J. Grous, Philip G. Krishnan, Suma Andries, Koen de Béthune, Marie-Pierre Azijn, Hilde Pauwels, Rudi De Clercq, Erik Arnold, Edward Janssen, Paul A.J. |
| description | Stemming from work on a previous clinical candidate, loviride, and other α-APA derivatives, a new series of potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been synthesized. The ITU analogues, which contain a unique diarylated imidoyl thiourea, are very active in inhibiting both wild-type and clinically important mutant strains of HIV-1.
Synthetic work around a previous NNRTI clinical candidate (loviride) has led to diarylated imidoyl thioureas (ITUs) that are very active against both the wild-type and mutant strains of the HIV-1 virus. |
| doi_str_mv | 10.1016/S0960-894X(01)00410-3 |
| format | Article |
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Synthetic work around a previous NNRTI clinical candidate (loviride) has led to diarylated imidoyl thioureas (ITUs) that are very active against both the wild-type and mutant strains of the HIV-1 virus.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/S0960-894X(01)00410-3</identifier><identifier>PMID: 11527703</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Acetamides - chemistry ; Acetamides - pharmacology ; Acetophenones - pharmacology ; Aniline Compounds - chemistry ; Anti-HIV Agents - chemical synthesis ; Anti-HIV Agents - chemistry ; Anti-HIV Agents - pharmacology ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiviral agents ; Biological and medical sciences ; Drug Design ; Drug Evaluation, Preclinical ; Drug Stability ; HIV Reverse Transcriptase - antagonists & inhibitors ; HIV Reverse Transcriptase - drug effects ; HIV Reverse Transcriptase - genetics ; HIV-1 - drug effects ; Imines - chemistry ; Imines - pharmacology ; Medical sciences ; Pharmacology. Drug treatments ; Structure-Activity Relationship ; Thiourea - analogs & derivatives ; Thiourea - chemistry ; Thiourea - pharmacology</subject><ispartof>Bioorganic & medicinal chemistry letters, 2001-09, Vol.11 (17), p.2225-2228</ispartof><rights>2001 Elsevier Science Ltd</rights><rights>2001 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c392t-ab1b9044d30b4e337a68a2f241bdb87c0939af8b35c6dcb773f08346eea779d43</citedby><cites>FETCH-LOGICAL-c392t-ab1b9044d30b4e337a68a2f241bdb87c0939af8b35c6dcb773f08346eea779d43</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X01004103$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1114767$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11527703$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ludovici, Donald W.</creatorcontrib><creatorcontrib>Kukla, Michael J.</creatorcontrib><creatorcontrib>Grous, Philip G.</creatorcontrib><creatorcontrib>Krishnan, Suma</creatorcontrib><creatorcontrib>Andries, Koen</creatorcontrib><creatorcontrib>de Béthune, Marie-Pierre</creatorcontrib><creatorcontrib>Azijn, Hilde</creatorcontrib><creatorcontrib>Pauwels, Rudi</creatorcontrib><creatorcontrib>De Clercq, Erik</creatorcontrib><creatorcontrib>Arnold, Edward</creatorcontrib><creatorcontrib>Janssen, Paul A.J.</creatorcontrib><title>Evolution of anti-HIV drug candidates. Part 1: From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU)</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Stemming from work on a previous clinical candidate, loviride, and other α-APA derivatives, a new series of potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been synthesized. The ITU analogues, which contain a unique diarylated imidoyl thiourea, are very active in inhibiting both wild-type and clinically important mutant strains of HIV-1.
Synthetic work around a previous NNRTI clinical candidate (loviride) has led to diarylated imidoyl thioureas (ITUs) that are very active against both the wild-type and mutant strains of the HIV-1 virus.</description><subject>Acetamides - chemistry</subject><subject>Acetamides - pharmacology</subject><subject>Acetophenones - pharmacology</subject><subject>Aniline Compounds - chemistry</subject><subject>Anti-HIV Agents - chemical synthesis</subject><subject>Anti-HIV Agents - chemistry</subject><subject>Anti-HIV Agents - pharmacology</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiviral agents</subject><subject>Biological and medical sciences</subject><subject>Drug Design</subject><subject>Drug Evaluation, Preclinical</subject><subject>Drug Stability</subject><subject>HIV Reverse Transcriptase - antagonists & inhibitors</subject><subject>HIV Reverse Transcriptase - drug effects</subject><subject>HIV Reverse Transcriptase - genetics</subject><subject>HIV-1 - drug effects</subject><subject>Imines - chemistry</subject><subject>Imines - pharmacology</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Structure-Activity Relationship</subject><subject>Thiourea - analogs & derivatives</subject><subject>Thiourea - chemistry</subject><subject>Thiourea - pharmacology</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM9qGzEQh0Vpadwkj9CiQyn2YVPJkle7vRQTksYQaCB_6E3MSrONyq7kSNqAHysvkmfqOjZtbz0NzHwz8-Mj5D1nJ5zx8vM1q0tWVLX8MWV8xpjkrBCvyITLUhZCssVrMvmDHJB3Kf1ijEsm5VtywPlirhQTE7I-ewzdkF3wNLQUfHbFxeqO2jj8pAa8dRYyphN6BTFT_oWex9DT56di6V3nfFjfo990YDBD7yzS6XZ0tZzRHKgbO2HT0XzvwhAR6HR1czs7Im9a6BIe7-shuT0_uzm9KC6_f1udLi8LI-p5LqDhTT2GtYI1EoVQUFYwb-eSN7aplGG1qKGtGrEwpTWNUqJllZAlIihVWykOyafd3XUMDwOmrHuXDHYdeAxD0opzIZVQI7jYgSaGlCK2eh1dD3GjOdNb1fpFtd561IzrF9VajHsf9g-Gpkf7d2vvdgQ-7gFIBro2gjcu_cNxqcrt_687DEcbjw6jTsahN2hdRJO1De4_SX4Dfv6bCg</recordid><startdate>20010903</startdate><enddate>20010903</enddate><creator>Ludovici, Donald W.</creator><creator>Kukla, Michael J.</creator><creator>Grous, Philip G.</creator><creator>Krishnan, Suma</creator><creator>Andries, Koen</creator><creator>de Béthune, Marie-Pierre</creator><creator>Azijn, Hilde</creator><creator>Pauwels, Rudi</creator><creator>De Clercq, Erik</creator><creator>Arnold, Edward</creator><creator>Janssen, Paul A.J.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><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>7X8</scope></search><sort><creationdate>20010903</creationdate><title>Evolution of anti-HIV drug candidates. Part 1: From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU)</title><author>Ludovici, Donald W. ; Kukla, Michael J. ; Grous, Philip G. ; Krishnan, Suma ; Andries, Koen ; de Béthune, Marie-Pierre ; Azijn, Hilde ; Pauwels, Rudi ; De Clercq, Erik ; Arnold, Edward ; Janssen, Paul A.J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c392t-ab1b9044d30b4e337a68a2f241bdb87c0939af8b35c6dcb773f08346eea779d43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Acetamides - chemistry</topic><topic>Acetamides - pharmacology</topic><topic>Acetophenones - pharmacology</topic><topic>Aniline Compounds - chemistry</topic><topic>Anti-HIV Agents - chemical synthesis</topic><topic>Anti-HIV Agents - chemistry</topic><topic>Anti-HIV Agents - pharmacology</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antiviral agents</topic><topic>Biological and medical sciences</topic><topic>Drug Design</topic><topic>Drug Evaluation, Preclinical</topic><topic>Drug Stability</topic><topic>HIV Reverse Transcriptase - antagonists & inhibitors</topic><topic>HIV Reverse Transcriptase - drug effects</topic><topic>HIV Reverse Transcriptase - genetics</topic><topic>HIV-1 - drug effects</topic><topic>Imines - chemistry</topic><topic>Imines - pharmacology</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Structure-Activity Relationship</topic><topic>Thiourea - analogs & derivatives</topic><topic>Thiourea - chemistry</topic><topic>Thiourea - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ludovici, Donald W.</creatorcontrib><creatorcontrib>Kukla, Michael J.</creatorcontrib><creatorcontrib>Grous, Philip G.</creatorcontrib><creatorcontrib>Krishnan, Suma</creatorcontrib><creatorcontrib>Andries, Koen</creatorcontrib><creatorcontrib>de Béthune, Marie-Pierre</creatorcontrib><creatorcontrib>Azijn, Hilde</creatorcontrib><creatorcontrib>Pauwels, Rudi</creatorcontrib><creatorcontrib>De Clercq, Erik</creatorcontrib><creatorcontrib>Arnold, Edward</creatorcontrib><creatorcontrib>Janssen, Paul A.J.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ludovici, Donald W.</au><au>Kukla, Michael J.</au><au>Grous, Philip G.</au><au>Krishnan, Suma</au><au>Andries, Koen</au><au>de Béthune, Marie-Pierre</au><au>Azijn, Hilde</au><au>Pauwels, Rudi</au><au>De Clercq, Erik</au><au>Arnold, Edward</au><au>Janssen, Paul A.J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evolution of anti-HIV drug candidates. 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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2001-09, Vol.11 (17), p.2225-2228 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Acetamides - chemistry Acetamides - pharmacology Acetophenones - pharmacology Aniline Compounds - chemistry Anti-HIV Agents - chemical synthesis Anti-HIV Agents - chemistry Anti-HIV Agents - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Biological and medical sciences Drug Design Drug Evaluation, Preclinical Drug Stability HIV Reverse Transcriptase - antagonists & inhibitors HIV Reverse Transcriptase - drug effects HIV Reverse Transcriptase - genetics HIV-1 - drug effects Imines - chemistry Imines - pharmacology Medical sciences Pharmacology. Drug treatments Structure-Activity Relationship Thiourea - analogs & derivatives Thiourea - chemistry Thiourea - pharmacology |
| title | Evolution of anti-HIV drug candidates. Part 1: From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU) |
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