دورية أكاديمية
Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors.
| العنوان: | Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors. |
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| المؤلفون: | Axford LC; Biota Holdings Ltd, 10/585 Blackburn Road, Notting Hill, Victoria 3168, Australia. Electronic address: l.offermann@biota.com.au., Agarwal PK, Anderson KH, Andrau LN, Atherall J, Barker S, Bennett JM, Blair M, Collins I, Czaplewski LG, Davies DT, Gannon CT, Kumar D, Lancett P, Logan A, Lunniss CJ, Mitchell DR, Offermann DA, Palmer JT, Palmer N, Pitt GR, Pommier S, Price D, Narasinga Rao B, Saxena R, Shukla T, Singh AK, Singh M, Srivastava A, Steele C, Stokes NR, Thomaides-Brears HB, Tyndall EM, Watson D, Haydon DJ |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Dec 15; Vol. 23 (24), pp. 6598-603. Date of Electronic Publication: 2013 Nov 04. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Drug Design*, Benzothiazoles/*chemistry , Benzothiazoles/*pharmacology , DNA Topoisomerase IV/*antagonists & inhibitors , Isonipecotic Acids/*chemistry , Topoisomerase II Inhibitors/*chemical synthesis , Topoisomerase II Inhibitors/*pharmacology, Animals ; Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/pharmacokinetics ; Anti-Bacterial Agents/pharmacology ; Benzothiazoles/chemical synthesis ; DNA Gyrase/chemistry ; DNA Gyrase/metabolism ; DNA Topoisomerase IV/metabolism ; Enterococcus faecalis/drug effects ; Enterococcus faecalis/enzymology ; Enzyme Activation/drug effects ; Haemophilus influenzae/drug effects ; Haemophilus influenzae/enzymology ; Half-Life ; Mice ; Microbial Sensitivity Tests ; Rats ; Staphylococcus aureus/drug effects ; Staphylococcus aureus/enzymology ; Streptococcus pyogenes/drug effects ; Streptococcus pyogenes/enzymology ; Topoisomerase II Inhibitors/chemistry ; Topoisomerase II Inhibitors/pharmacokinetics |
| مستخلص: | The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described. Antibacterial properties have been demonstrated by activity against DNA gyrase ATPase and potent activity against Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes and Haemophilus influenzae. Further refinements to the scaffold designed to enhance drug-likeness included analogues bearing an α-substituent to the carboxylic acid group, resulting in excellent solubility and favourable pharmacokinetic properties. (Copyright © 2013 Elsevier Ltd. All rights reserved.) |
| فهرسة مساهمة: | Keywords: Antibacterial; DNA gyrase; Topoisomerase |
| المشرفين على المادة: | 0 (Anti-Bacterial Agents) 0 (Benzothiazoles) 0 (Isonipecotic Acids) 0 (Topoisomerase II Inhibitors) EC 5.99.1.- (DNA Topoisomerase IV) EC 5.99.1.3 (DNA Gyrase) G5BW2593EP (benzothiazole) |
| تواريخ الأحداث: | Date Created: 20131119 Date Completed: 20140725 Latest Revision: 20131202 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1016/j.bmcl.2013.10.058 |
| PMID: | 24239017 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3405 |
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| DOI: | 10.1016/j.bmcl.2013.10.058 |