Design and synthesis of 4-Aminoquinoline-isoindoline-dione-isoniazid triads as potential anti-mycobacterials

Autor: Oluwakemi Ebenezer, Laurent Kremer, Parvesh Singh, Anu Rani, Paul Awolade, Françoise Roquet-Banères, Vipan Kumar, Matt D. Johansen, Sumanjit
Přispěvatelé: Guru Nanak Dev University, Punjab, Institut de Recherche en Infectiologie de Montpellier (IRIM), Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), University of KwaZulu-Natal [Durban, Afrique du Sud] (UKZN), Kremer, Laurent, University of KwaZulu-Natal (UKZN)
Jazyk: angličtina
Rok vydání: 2020
Předmět:
Indoles
Cytotoxicity
[SDV]Life Sciences [q-bio]
Clinical Biochemistry
Antitubercular Agents
Pharmaceutical Science
4-aminoquinoline-isoindoline-dione-isoniazid
Biochemistry
chemistry.chemical_compound
Drug Discovery
0303 health sciences
Molecular Structure
Isoniazid
Quinoline
Molecular docking vipan kumar
3. Good health
[SDV] Life Sciences [q-bio]
[SDV.MP]Life Sciences [q-bio]/Microbiology and Parasitology
Oluwakemi Ebenezer
Aminoquinolines
Molecular Medicine
medicine.drug
Matt D Johansen
Stereochemistry
Paul Awolade
Microbial Sensitivity Tests
Structure-Activity Relationship
03 medical and health sciences
Laurent Kremer
medicine
Molecular Biology
[SDV.MP] Life Sciences [q-bio]/Microbiology and Parasitology
030304 developmental biology
Dose-Response Relationship
Drug
030306 microbiology
Organic Chemistry
Mycobacterium tuberculosis
Isoindoline
Parvesh Singh
Structural framework
Anu Rani
Françoise Roquet-Banères
chemistry
Antimycobacterial activity
Drug Design
4-Aminoquinoline
Vero cell
Selectivity index
Sumanjit sumanjit
Conjugate
Zdroj: Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, 2020, 30 (22), pp.127576. ⟨10.1016/j.bmcl.2020.127576⟩
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2020, 30 (22), pp.127576. ⟨10.1016/j.bmcl.2020.127576⟩
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2020.127576⟩
Popis: International audience; A series of 4-aminoquinoline-isoindoline-dione-isoniazid triads were synthesized and assessed for their anti-mycobacterial activities and cytotoxicity. Most of the synthesized compounds exhibited promising activities against the mc26230 strain of M. tuberculosis with MIC in the range of 3.125-12.5 µg/mL and were non-cytotoxic against Vero cells. The conjugates lacking either isoniazid or quinoline core in their structural framework failed to inhibit the growth of M. tuberculosis; thus, further strengthening the proposed design of triads in the present study.
Databáze: OpenAIRE
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