Tuberculostatic Activity of 2-Amino-6-Chloropurine Derivatives
Studies of the antimycobacterial activity of 2-amino-6-chloropurine and its N-acyl derivatives against laboratory ( Mycobacterium tuberculosis H37Rv, M. avium, M. terrae ) and clinical Mycobacterium tuberculosis strains (MDR-TB) identified compounds with high tuberculostatic activity (MIC from 0.35...
Gespeichert in:
| Veröffentlicht in: | Pharmaceutical chemistry journal 2017-12, Vol.51 (9), p.769-772 |
|---|---|
| Hauptverfasser: | , , , , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 772 |
|---|---|
| container_issue | 9 |
| container_start_page | 769 |
| container_title | Pharmaceutical chemistry journal |
| container_volume | 51 |
| creator | Krasnov, V. P. Vigorov, A. Yu Gruzdev, D. A. Levit, G. L. Kravchenko, M. A. Skornyakov, S. N. Bekker, O. B. Maslov, D. A. Danilenko, V. N. Charushin, V. N. |
| description | Studies of the antimycobacterial activity of 2-amino-6-chloropurine and its N-acyl derivatives against laboratory (
Mycobacterium tuberculosis
H37Rv,
M. avium, M. terrae
) and clinical
Mycobacterium tuberculosis
strains (MDR-TB) identified compounds with high tuberculostatic activity (MIC from 0.35 – 1.5 μg/ml). The cytotoxic activities of the compounds with antimycobacterial activity against human embryo fibroblasts were studied in the MTT test, which showed that the study compounds were essentially nontoxic (IC
50
> 50 μM). Further chemical modification may yield compounds with potential for creating drugs for the treatment of tuberculosis. With the aim of identifying the possible mechanism of the tuberculostatic activity, the ability of the study compounds to inhibit mycobacterial serine-threonine protein kinases (STPK) was assessed. The tuberculostatic activity of 2-amino-6-chloropurine derivatives was not linked with their inhibition of STPK. |
| doi_str_mv | 10.1007/s11094-017-1690-4 |
| format | Article |
| fullrecord | <record><control><sourceid>gale_cross</sourceid><recordid>TN_cdi_gale_infotracmisc_A517939699</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><galeid>A517939699</galeid><sourcerecordid>A517939699</sourcerecordid><originalsourceid>FETCH-LOGICAL-c355t-a8f171c9b4c11721991318ed623cc253417a452b62c75156a1eab367d4421ca33</originalsourceid><addsrcrecordid>eNp9kMtKAzEUQIMoWKsf4G7AdWpuHpNmIwz1CQU3FdyFTJqpKZ1JSWYK_XtTxo0gksWFcM6FexC6BTIDQuR9AiCKYwISQ6kI5mdoAkIyrAiDczQhRAEGQT4v0VVKW0KyxegEPayG2kU77ELqTe9tUdneH3x_LEJTUFy1vgu4xIuvXYhhP0TfueLRRX_I8MGla3TRmF1yNz9zij6en1aLV7x8f3lbVEtsmRA9NvMGJFhVcwsgKSgFDOZuXVJmLRWMgzRc0LqkVgoQpQFnalbKNecUrGFsiu7GvRuzc9p3Teijsa1PVlcCpGKqVCpTsz-o_Nau9TZ0rvH5_5cAo2BjSCm6Ru-jb008aiD61FWPXXXuqk9dNc8OHZ2U2W7jot6GIXb5-n-kb-mPeDI</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Tuberculostatic Activity of 2-Amino-6-Chloropurine Derivatives</title><source>SpringerLink Journals</source><creator>Krasnov, V. P. ; Vigorov, A. Yu ; Gruzdev, D. A. ; Levit, G. L. ; Kravchenko, M. A. ; Skornyakov, S. N. ; Bekker, O. B. ; Maslov, D. A. ; Danilenko, V. N. ; Charushin, V. N.</creator><creatorcontrib>Krasnov, V. P. ; Vigorov, A. Yu ; Gruzdev, D. A. ; Levit, G. L. ; Kravchenko, M. A. ; Skornyakov, S. N. ; Bekker, O. B. ; Maslov, D. A. ; Danilenko, V. N. ; Charushin, V. N.</creatorcontrib><description>Studies of the antimycobacterial activity of 2-amino-6-chloropurine and its N-acyl derivatives against laboratory (
Mycobacterium tuberculosis
H37Rv,
M. avium, M. terrae
) and clinical
Mycobacterium tuberculosis
strains (MDR-TB) identified compounds with high tuberculostatic activity (MIC from 0.35 – 1.5 μg/ml). The cytotoxic activities of the compounds with antimycobacterial activity against human embryo fibroblasts were studied in the MTT test, which showed that the study compounds were essentially nontoxic (IC
50
> 50 μM). Further chemical modification may yield compounds with potential for creating drugs for the treatment of tuberculosis. With the aim of identifying the possible mechanism of the tuberculostatic activity, the ability of the study compounds to inhibit mycobacterial serine-threonine protein kinases (STPK) was assessed. The tuberculostatic activity of 2-amino-6-chloropurine derivatives was not linked with their inhibition of STPK.</description><identifier>ISSN: 0091-150X</identifier><identifier>EISSN: 1573-9031</identifier><identifier>DOI: 10.1007/s11094-017-1690-4</identifier><language>eng</language><publisher>New York: Springer US</publisher><subject>Antitubercular agents ; Care and treatment ; Medicine ; Organic Chemistry ; Pharmacology/Toxicology ; Pharmacy ; Tuberculosis</subject><ispartof>Pharmaceutical chemistry journal, 2017-12, Vol.51 (9), p.769-772</ispartof><rights>Springer Science+Business Media, LLC, part of Springer Nature 2017</rights><rights>COPYRIGHT 2017 Springer</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c355t-a8f171c9b4c11721991318ed623cc253417a452b62c75156a1eab367d4421ca33</citedby><cites>FETCH-LOGICAL-c355t-a8f171c9b4c11721991318ed623cc253417a452b62c75156a1eab367d4421ca33</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s11094-017-1690-4$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s11094-017-1690-4$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,776,780,27901,27902,41464,42533,51294</link.rule.ids></links><search><creatorcontrib>Krasnov, V. P.</creatorcontrib><creatorcontrib>Vigorov, A. Yu</creatorcontrib><creatorcontrib>Gruzdev, D. A.</creatorcontrib><creatorcontrib>Levit, G. L.</creatorcontrib><creatorcontrib>Kravchenko, M. A.</creatorcontrib><creatorcontrib>Skornyakov, S. N.</creatorcontrib><creatorcontrib>Bekker, O. B.</creatorcontrib><creatorcontrib>Maslov, D. A.</creatorcontrib><creatorcontrib>Danilenko, V. N.</creatorcontrib><creatorcontrib>Charushin, V. N.</creatorcontrib><title>Tuberculostatic Activity of 2-Amino-6-Chloropurine Derivatives</title><title>Pharmaceutical chemistry journal</title><addtitle>Pharm Chem J</addtitle><description>Studies of the antimycobacterial activity of 2-amino-6-chloropurine and its N-acyl derivatives against laboratory (
Mycobacterium tuberculosis
H37Rv,
M. avium, M. terrae
) and clinical
Mycobacterium tuberculosis
strains (MDR-TB) identified compounds with high tuberculostatic activity (MIC from 0.35 – 1.5 μg/ml). The cytotoxic activities of the compounds with antimycobacterial activity against human embryo fibroblasts were studied in the MTT test, which showed that the study compounds were essentially nontoxic (IC
50
> 50 μM). Further chemical modification may yield compounds with potential for creating drugs for the treatment of tuberculosis. With the aim of identifying the possible mechanism of the tuberculostatic activity, the ability of the study compounds to inhibit mycobacterial serine-threonine protein kinases (STPK) was assessed. The tuberculostatic activity of 2-amino-6-chloropurine derivatives was not linked with their inhibition of STPK.</description><subject>Antitubercular agents</subject><subject>Care and treatment</subject><subject>Medicine</subject><subject>Organic Chemistry</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Tuberculosis</subject><issn>0091-150X</issn><issn>1573-9031</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><recordid>eNp9kMtKAzEUQIMoWKsf4G7AdWpuHpNmIwz1CQU3FdyFTJqpKZ1JSWYK_XtTxo0gksWFcM6FexC6BTIDQuR9AiCKYwISQ6kI5mdoAkIyrAiDczQhRAEGQT4v0VVKW0KyxegEPayG2kU77ELqTe9tUdneH3x_LEJTUFy1vgu4xIuvXYhhP0TfueLRRX_I8MGla3TRmF1yNz9zij6en1aLV7x8f3lbVEtsmRA9NvMGJFhVcwsgKSgFDOZuXVJmLRWMgzRc0LqkVgoQpQFnalbKNecUrGFsiu7GvRuzc9p3Teijsa1PVlcCpGKqVCpTsz-o_Nau9TZ0rvH5_5cAo2BjSCm6Ru-jb008aiD61FWPXXXuqk9dNc8OHZ2U2W7jot6GIXb5-n-kb-mPeDI</recordid><startdate>20171201</startdate><enddate>20171201</enddate><creator>Krasnov, V. P.</creator><creator>Vigorov, A. Yu</creator><creator>Gruzdev, D. A.</creator><creator>Levit, G. L.</creator><creator>Kravchenko, M. A.</creator><creator>Skornyakov, S. N.</creator><creator>Bekker, O. B.</creator><creator>Maslov, D. A.</creator><creator>Danilenko, V. N.</creator><creator>Charushin, V. N.</creator><general>Springer US</general><general>Springer</general><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20171201</creationdate><title>Tuberculostatic Activity of 2-Amino-6-Chloropurine Derivatives</title><author>Krasnov, V. P. ; Vigorov, A. Yu ; Gruzdev, D. A. ; Levit, G. L. ; Kravchenko, M. A. ; Skornyakov, S. N. ; Bekker, O. B. ; Maslov, D. A. ; Danilenko, V. N. ; Charushin, V. N.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c355t-a8f171c9b4c11721991318ed623cc253417a452b62c75156a1eab367d4421ca33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Antitubercular agents</topic><topic>Care and treatment</topic><topic>Medicine</topic><topic>Organic Chemistry</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Tuberculosis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Krasnov, V. P.</creatorcontrib><creatorcontrib>Vigorov, A. Yu</creatorcontrib><creatorcontrib>Gruzdev, D. A.</creatorcontrib><creatorcontrib>Levit, G. L.</creatorcontrib><creatorcontrib>Kravchenko, M. A.</creatorcontrib><creatorcontrib>Skornyakov, S. N.</creatorcontrib><creatorcontrib>Bekker, O. B.</creatorcontrib><creatorcontrib>Maslov, D. A.</creatorcontrib><creatorcontrib>Danilenko, V. N.</creatorcontrib><creatorcontrib>Charushin, V. N.</creatorcontrib><collection>CrossRef</collection><jtitle>Pharmaceutical chemistry journal</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Krasnov, V. P.</au><au>Vigorov, A. Yu</au><au>Gruzdev, D. A.</au><au>Levit, G. L.</au><au>Kravchenko, M. A.</au><au>Skornyakov, S. N.</au><au>Bekker, O. B.</au><au>Maslov, D. A.</au><au>Danilenko, V. N.</au><au>Charushin, V. N.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Tuberculostatic Activity of 2-Amino-6-Chloropurine Derivatives</atitle><jtitle>Pharmaceutical chemistry journal</jtitle><stitle>Pharm Chem J</stitle><date>2017-12-01</date><risdate>2017</risdate><volume>51</volume><issue>9</issue><spage>769</spage><epage>772</epage><pages>769-772</pages><issn>0091-150X</issn><eissn>1573-9031</eissn><abstract>Studies of the antimycobacterial activity of 2-amino-6-chloropurine and its N-acyl derivatives against laboratory (
Mycobacterium tuberculosis
H37Rv,
M. avium, M. terrae
) and clinical
Mycobacterium tuberculosis
strains (MDR-TB) identified compounds with high tuberculostatic activity (MIC from 0.35 – 1.5 μg/ml). The cytotoxic activities of the compounds with antimycobacterial activity against human embryo fibroblasts were studied in the MTT test, which showed that the study compounds were essentially nontoxic (IC
50
> 50 μM). Further chemical modification may yield compounds with potential for creating drugs for the treatment of tuberculosis. With the aim of identifying the possible mechanism of the tuberculostatic activity, the ability of the study compounds to inhibit mycobacterial serine-threonine protein kinases (STPK) was assessed. The tuberculostatic activity of 2-amino-6-chloropurine derivatives was not linked with their inhibition of STPK.</abstract><cop>New York</cop><pub>Springer US</pub><doi>10.1007/s11094-017-1690-4</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0091-150X |
| ispartof | Pharmaceutical chemistry journal, 2017-12, Vol.51 (9), p.769-772 |
| issn | 0091-150X 1573-9031 |
| language | eng |
| recordid | cdi_gale_infotracmisc_A517939699 |
| source | SpringerLink Journals |
| subjects | Antitubercular agents Care and treatment Medicine Organic Chemistry Pharmacology/Toxicology Pharmacy Tuberculosis |
| title | Tuberculostatic Activity of 2-Amino-6-Chloropurine Derivatives |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-15T09%3A46%3A54IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-gale_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Tuberculostatic%20Activity%20of%202-Amino-6-Chloropurine%20Derivatives&rft.jtitle=Pharmaceutical%20chemistry%20journal&rft.au=Krasnov,%20V.%20P.&rft.date=2017-12-01&rft.volume=51&rft.issue=9&rft.spage=769&rft.epage=772&rft.pages=769-772&rft.issn=0091-150X&rft.eissn=1573-9031&rft_id=info:doi/10.1007/s11094-017-1690-4&rft_dat=%3Cgale_cross%3EA517939699%3C/gale_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rft_galeid=A517939699&rfr_iscdi=true |