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Antibacterial Evaluation, In Silico Characters and Molecular Docking of Schiff Bases Derived from 5-aminopyrazoles.
Hassan, Ashraf S; Askar, Ahmed A; Nossier, Eman S; Naglah, Ahmed M; Moustafa, Gaber O; Al-Omar, Mohamed A.
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  • Hassan AS; Organometallic and Organometalloid Chemistry Department, National Research Centre, Dokki, Cairo 12622, Egypt. ashraf_salmoon@yahoo.com.
  • Askar AA; Botany and Microbiology Department, Faculty of Science (Boys), Al-Azhar University, Cairo 11754, Egypt.
  • Nossier ES; Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11754, Egypt.
  • Naglah AM; Department of Pharmaceutical Chemistry, Drug Exploration and Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. anaglah@ksu.edu.sa.
  • Moustafa GO; Peptide Chemistry Department, National Research Centre, Dokki, Cairo 12622, Egypt. anaglah@ksu.edu.sa.
  • Al-Omar MA; Peptide Chemistry Department, National Research Centre, Dokki, Cairo 12622, Egypt.
Molecules ; 24(17)2019 Aug 28.
Article en En | MEDLINE | ID: mdl-31466322
A series of Schiff bases 14-25 were designed and synthesized for evaluation of their antibacterial properties against multi-drug resistant bacteria (MDRB). The antibacterial activities of Schiff bases 14-25 showed that most of the synthesized compounds displayed a significant antibacterial activity. Assessment of in silico ADMET properties (absorption, distribution, metabolism, excretion and toxicity) of Schiff bases illustrates that all derivatives showed agreement to the Lipinski's rule of five. Further enzymatic assay aided by molecular docking study demonstrated that compound 18 is a potent inhibitor of staphylococcus aureus DNA gyrase and dihydrofolate reductase kinases. This study could be valuable in the discovery of new potent antimicrobial agents.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Bases de Schiff / Staphylococcus aureus / Antibacterianos Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2019 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Suiza
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Bases de Schiff / Staphylococcus aureus / Antibacterianos Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2019 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Suiza