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Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives.
Kamel, Moumen S; Belal, Amany; Aboelez, Moustafa O; Shokr, E Kh; Abdel-Ghany, H; Mansour, Hany S; Shawky, Ahmed M; El-Remaily, Mahmoud Abd El Aleem Ali Ali.
Afiliação
  • Kamel MS; Chemistry Department, Faculty of Science, Sohag University, Sohag 82524, Egypt.
  • Belal A; Department of Pharmaceutical Chemistry, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia.
  • Aboelez MO; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sohag University, Sohag 82524, Egypt.
  • Shokr EK; Physics Department, Faculty of Science, Sohag University, Sohag 82524, Egypt.
  • Abdel-Ghany H; Chemistry Department, Faculty of Science, Sohag University, Sohag 82524, Egypt.
  • Mansour HS; Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.
  • Shawky AM; Science and Technology Unit (STU), Umm Al-Qura University, Makkah 21955, Saudi Arabia.
  • El-Remaily MAEAAA; Chemistry Department, Faculty of Science, Sohag University, Sohag 82524, Egypt.
Molecules ; 27(7)2022 Mar 23.
Article em En | MEDLINE | ID: mdl-35408463
ABSTRACT
Novel pyrrolo [2,3-b] pyrrole derivatives were synthesized and their hypolipidemic activity was assessed in hyperlipidemic rats. The chemical structures of the new derivatives were confirmed through spectral analysis. Compounds 5 and 6 were revealed to be the most effective hypolipidemic agents, with considerable hypocholesterolemic and hypotriglyceridemic effects. They appear to be promising candidates for creating new powerful derivatives with anti-atherosclerotic and hypolipidemic properties. As for antimicrobial activity, some of the tested compounds showed moderate activity against Pseudomonas aeruginosa compound 2 revealed an MIC value of 50 µg/mL, compared to 25 µg/mL for ciprofloxacin. Compound 3 showed good antimicrobial activity against Staphylococcus aureus, comparable to ciprofloxacin, and roughly half the activity of ampicillin, according to MIC values. Compound 2 has an MIC approximately 25% of that of clotrimazole against Candida albicans. Compound 2 also showed the highest antioxidant activity with 59% inhibition of radical scavenging activity. Additionally, the cytotoxic activity of these new derivatives 1-7 was investigated and most of them showed good anticancer activity against the three tested cell lines.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirróis / Anti-Infecciosos Limite: Animals Idioma: En Ano de publicação: 2022 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirróis / Anti-Infecciosos Limite: Animals Idioma: En Ano de publicação: 2022 Tipo de documento: Article