دورية أكاديمية
Novel quinoline-piperazine hybrids: the design, synthesis and evaluation of antibacterial and antituberculosis properties.
| العنوان: | Novel quinoline-piperazine hybrids: the design, synthesis and evaluation of antibacterial and antituberculosis properties. |
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| المؤلفون: | Gnanavelu K; Anthem Biosciences Pvt. Ltd. #49, Bommasandra Industrial Area, Bommasandra Bangalore 560099 Karnataka India sumesh.e@anthembio.com.; School of Bio-Sciences and Technology, Vellore Institute of Technology Vellore Tamil Nadu 632014 India., K S VK; Anthem Biosciences Pvt. Ltd. #49, Bommasandra Industrial Area, Bommasandra Bangalore 560099 Karnataka India sumesh.e@anthembio.com., Eswaran S; Anthem Biosciences Pvt. Ltd. #49, Bommasandra Industrial Area, Bommasandra Bangalore 560099 Karnataka India sumesh.e@anthembio.com., Sivashanmugam K; School of Bio-Sciences and Technology, Vellore Institute of Technology Vellore Tamil Nadu 632014 India. |
| المصدر: | RSC medicinal chemistry [RSC Med Chem] 2022 Nov 01; Vol. 14 (1), pp. 183-189. Date of Electronic Publication: 2022 Nov 01 (Print Publication: 2023). |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 101759460 Publication Model: eCollection Cited Medium: Internet ISSN: 2632-8682 (Electronic) Linking ISSN: 26328682 NLM ISO Abbreviation: RSC Med Chem Subsets: PubMed not MEDLINE |
| أسماء مطبوعة: | Original Publication: Cambridge : Royal Society of Chemistry, [2020]- |
| مستخلص: | A communicable disease such as tuberculosis (TB), which takes ∼10 million lives worldwide every year, is one of the major concerns for future generations. The intake of multiple antibiotics is increasing because of the emergence of multiple drug-resistant TB (MDR-TB) to pathogens which do not respond to the first-line TB drugs. Even though numerous drugs are available on the market, there is a huge need for MDR-TB drugs. Herein, our emphasis was to synthesise a series of 2,4,6-substituted quinoline conjugated piperazine coupled sulfonamides, as well as amides, and to study and evaluate their in vitro antibacterial activity against both susceptible and resistant pathogens of Gram-positive and Gram-negative bacteria. Furthermore, their antituberculosis activity was assessed against non-virulent, virulent and MDR pathogens. Few compounds displayed inhibitory activity against bacterial growth, but two compounds displayed significant inhibitory activity against all the TB strains (lowest MIC of 10g is 0.07 μM and 11e is 1.1 μM), which are more effective than other 1st line and 2nd line TB drugs. These two compounds are less cytotoxic, and could be developed as antibiotics or MDR-TB drugs by improving their hydrophilicity. Competing Interests: There are no conflicts to declare. (This journal is © The Royal Society of Chemistry.) |
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| تواريخ الأحداث: | Date Created: 20230210 Latest Revision: 20231102 |
| رمز التحديث: | 20231215 |
| مُعرف محوري في PubMed: | PMC9890665 |
| DOI: | 10.1039/d2md00260d |
| PMID: | 36760744 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 2632-8682 |
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| DOI: | 10.1039/d2md00260d |