Anti-tubercular agents. Part 5: Synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners
In an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzothiadiazine 1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxa...
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| Veröffentlicht in: | European journal of medicinal chemistry 2010-10, Vol.45 (10), p.4545-4553 |
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| container_title | European journal of medicinal chemistry |
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| creator | Kamal, Ahmed Shetti, Rajesh V.C.R.N.C. Azeeza, Shaik Ahmed, S. Kaleem Swapna, P. Reddy, A. Malla Khan, Inshad Ali Sharma, Sandeep Abdullah, Sheikh Tasduq |
| description | In an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzothiadiazine 1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxacin and amphotericin as positive controls. Further, to understand structural requirements for exploring the structure activity relationship of BTDs, cytotoxicity and
in vivo study of recently reported potent molecule
4 (MIC = 1 μg/mL) is also discussed.
A new series of benzothiadiazine 1,1-dioxide based congeners was synthesized and evaluated against
Mycobacterium tuberculosis, Gram-positive, Gram-negative bacteria and fungi. Further,
in vivo activity of earlier potent molecule of this series is also discussed.
[Display omitted] |
| doi_str_mv | 10.1016/j.ejmech.2010.07.015 |
| format | Article |
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in vivo study of recently reported potent molecule
4 (MIC = 1 μg/mL) is also discussed.
A new series of benzothiadiazine 1,1-dioxide based congeners was synthesized and evaluated against
Mycobacterium tuberculosis, Gram-positive, Gram-negative bacteria and fungi. Further,
in vivo activity of earlier potent molecule of this series is also discussed.
[Display omitted]</description><identifier>ISSN: 0223-5234</identifier><identifier>EISSN: 1768-3254</identifier><identifier>DOI: 10.1016/j.ejmech.2010.07.015</identifier><identifier>PMID: 20705368</identifier><identifier>CODEN: EJMCA5</identifier><language>eng</language><publisher>Kidlington: Elsevier Masson SAS</publisher><subject>Animals ; Anti-tubercular agents ; Antibacterial agents ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antitubercular Agents - chemical synthesis ; Antitubercular Agents - chemistry ; Antitubercular Agents - pharmacology ; Antitubercular Agents - therapeutic use ; Bacteria - drug effects ; Benzothiadiazine 1,1-dioxides ; Benzothiadiazines - chemical synthesis ; Benzothiadiazines - chemistry ; Benzothiadiazines - pharmacology ; Benzothiadiazines - therapeutic use ; Biological and medical sciences ; Cell Line ; Cell Survival - drug effects ; Female ; Fungi - drug effects ; Humans ; M. tuberculosis ; MDR-and XDR-TB ; Medical sciences ; Mice ; Mice, Inbred BALB C ; Microbial Sensitivity Tests ; Mycobacterium tuberculosis - drug effects ; Pharmacology. Drug treatments ; Tuberculosis - drug therapy</subject><ispartof>European journal of medicinal chemistry, 2010-10, Vol.45 (10), p.4545-4553</ispartof><rights>2010 Elsevier Masson SAS</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2010 Elsevier Masson SAS. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c391t-cce43e345bdb8f5e2976b219ae3f94fb0e243f972450d6bad8d85d907865ae6a3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0223523410004952$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65534</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=23214429$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20705368$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kamal, Ahmed</creatorcontrib><creatorcontrib>Shetti, Rajesh V.C.R.N.C.</creatorcontrib><creatorcontrib>Azeeza, Shaik</creatorcontrib><creatorcontrib>Ahmed, S. Kaleem</creatorcontrib><creatorcontrib>Swapna, P.</creatorcontrib><creatorcontrib>Reddy, A. Malla</creatorcontrib><creatorcontrib>Khan, Inshad Ali</creatorcontrib><creatorcontrib>Sharma, Sandeep</creatorcontrib><creatorcontrib>Abdullah, Sheikh Tasduq</creatorcontrib><title>Anti-tubercular agents. Part 5: Synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners</title><title>European journal of medicinal chemistry</title><addtitle>Eur J Med Chem</addtitle><description>In an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzothiadiazine 1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxacin and amphotericin as positive controls. Further, to understand structural requirements for exploring the structure activity relationship of BTDs, cytotoxicity and
in vivo study of recently reported potent molecule
4 (MIC = 1 μg/mL) is also discussed.
A new series of benzothiadiazine 1,1-dioxide based congeners was synthesized and evaluated against
Mycobacterium tuberculosis, Gram-positive, Gram-negative bacteria and fungi. Further,
in vivo activity of earlier potent molecule of this series is also discussed.
[Display omitted]</description><subject>Animals</subject><subject>Anti-tubercular agents</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antitubercular Agents - chemical synthesis</subject><subject>Antitubercular Agents - chemistry</subject><subject>Antitubercular Agents - pharmacology</subject><subject>Antitubercular Agents - therapeutic use</subject><subject>Bacteria - drug effects</subject><subject>Benzothiadiazine 1,1-dioxides</subject><subject>Benzothiadiazines - chemical synthesis</subject><subject>Benzothiadiazines - chemistry</subject><subject>Benzothiadiazines - pharmacology</subject><subject>Benzothiadiazines - therapeutic use</subject><subject>Biological and medical sciences</subject><subject>Cell Line</subject><subject>Cell Survival - drug effects</subject><subject>Female</subject><subject>Fungi - drug effects</subject><subject>Humans</subject><subject>M. tuberculosis</subject><subject>MDR-and XDR-TB</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred BALB C</subject><subject>Microbial Sensitivity Tests</subject><subject>Mycobacterium tuberculosis - drug effects</subject><subject>Pharmacology. Drug treatments</subject><subject>Tuberculosis - drug therapy</subject><issn>0223-5234</issn><issn>1768-3254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kF1rFTEQhhdR7Gn1H4jkRrzprvncDy-EUvyCgoJ6HSbJbE8Oe5KaZIvtrzflHPXOqxmG550ZnqZ5wWjHKOvf7Drc7dFuO07riA4dZepRs2FDP7aCK_m42VDORau4kCfNac47SqnqKX3anHA6UCX6cdPki1B8W1aDya4LJALXGEruyFdIhai35NtdKFvMPhMIjhgfl3jtLSwEb2FZofgYSJyJwXAfy9aD83DvAxJ2zlrn4y_vkBjI6IiNoe7GlJ81T2ZYMj4_1rPmx4f33y8_tVdfPn6-vLhqrZhYaa1FKVBIZZwZZ4V8GnrD2QQo5knOhiKXtRu4VNT1BtzoRuUmOoy9AuxBnDWvD3tvUvy5Yi5677PFZYGAcc16UJIywUZZSXkgbYo5J5z1TfJ7SHeaUf1gW-_0wbZ-sK3poKvtGnt5PLCaPbq_oT96K_DqCECuzuYEwfr8jxOcScmnyr07cFh13HpMOluPwaLzCW3RLvr_f_Ibc9KgRA</recordid><startdate>20101001</startdate><enddate>20101001</enddate><creator>Kamal, Ahmed</creator><creator>Shetti, Rajesh V.C.R.N.C.</creator><creator>Azeeza, Shaik</creator><creator>Ahmed, S. Kaleem</creator><creator>Swapna, P.</creator><creator>Reddy, A. Malla</creator><creator>Khan, Inshad Ali</creator><creator>Sharma, Sandeep</creator><creator>Abdullah, Sheikh Tasduq</creator><general>Elsevier Masson SAS</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>20101001</creationdate><title>Anti-tubercular agents. Part 5: Synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners</title><author>Kamal, Ahmed ; Shetti, Rajesh V.C.R.N.C. ; Azeeza, Shaik ; Ahmed, S. Kaleem ; Swapna, P. ; Reddy, A. 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Antiparasitic agents</topic><topic>Antitubercular Agents - chemical synthesis</topic><topic>Antitubercular Agents - chemistry</topic><topic>Antitubercular Agents - pharmacology</topic><topic>Antitubercular Agents - therapeutic use</topic><topic>Bacteria - drug effects</topic><topic>Benzothiadiazine 1,1-dioxides</topic><topic>Benzothiadiazines - chemical synthesis</topic><topic>Benzothiadiazines - chemistry</topic><topic>Benzothiadiazines - pharmacology</topic><topic>Benzothiadiazines - therapeutic use</topic><topic>Biological and medical sciences</topic><topic>Cell Line</topic><topic>Cell Survival - drug effects</topic><topic>Female</topic><topic>Fungi - drug effects</topic><topic>Humans</topic><topic>M. tuberculosis</topic><topic>MDR-and XDR-TB</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred BALB C</topic><topic>Microbial Sensitivity Tests</topic><topic>Mycobacterium tuberculosis - drug effects</topic><topic>Pharmacology. 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Part 5: Synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners</atitle><jtitle>European journal of medicinal chemistry</jtitle><addtitle>Eur J Med Chem</addtitle><date>2010-10-01</date><risdate>2010</risdate><volume>45</volume><issue>10</issue><spage>4545</spage><epage>4553</epage><pages>4545-4553</pages><issn>0223-5234</issn><eissn>1768-3254</eissn><coden>EJMCA5</coden><abstract>In an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzothiadiazine 1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxacin and amphotericin as positive controls. Further, to understand structural requirements for exploring the structure activity relationship of BTDs, cytotoxicity and
in vivo study of recently reported potent molecule
4 (MIC = 1 μg/mL) is also discussed.
A new series of benzothiadiazine 1,1-dioxide based congeners was synthesized and evaluated against
Mycobacterium tuberculosis, Gram-positive, Gram-negative bacteria and fungi. Further,
in vivo activity of earlier potent molecule of this series is also discussed.
[Display omitted]</abstract><cop>Kidlington</cop><pub>Elsevier Masson SAS</pub><pmid>20705368</pmid><doi>10.1016/j.ejmech.2010.07.015</doi><tpages>9</tpages></addata></record> |
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| ispartof | European journal of medicinal chemistry, 2010-10, Vol.45 (10), p.4545-4553 |
| issn | 0223-5234 1768-3254 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Anti-tubercular agents Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Antitubercular Agents - chemical synthesis Antitubercular Agents - chemistry Antitubercular Agents - pharmacology Antitubercular Agents - therapeutic use Bacteria - drug effects Benzothiadiazine 1,1-dioxides Benzothiadiazines - chemical synthesis Benzothiadiazines - chemistry Benzothiadiazines - pharmacology Benzothiadiazines - therapeutic use Biological and medical sciences Cell Line Cell Survival - drug effects Female Fungi - drug effects Humans M. tuberculosis MDR-and XDR-TB Medical sciences Mice Mice, Inbred BALB C Microbial Sensitivity Tests Mycobacterium tuberculosis - drug effects Pharmacology. Drug treatments Tuberculosis - drug therapy |
| title | Anti-tubercular agents. Part 5: Synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners |
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