تصميم، تخليق، ربط جزيئي وتقييم بيولوجي لمشتقات جديدة من السلفامويل بنتاميدات المستخلصة من الليوسين كعوامل مضادة للميكروبات ومضادة للأكسدة
DOI:
https://doi.org/10.35516/jjps.v17i4.2467الكلمات المفتاحية:
البنتاميدات، الليوسين، السلفوناميدات، مضاد للميكروبات، النشاط المضاد للأكسدة، التخليقالملخص
غالبية الأمراض التي تتوسطها العوامل الميكروبية والإجهاد التأكسدي مقلقة للغاية. تتجلى الحاجة إلى تطوير أدوية جديدة من خلال حقيقة أن مقاومة المضادات الميكروبية في تزايد وأن العديد من الأدوية المضادة للأكسدة الحالية توفر تخفيفًا عرضيًا ضئيلًا فقط. كان الهدف من هذا العمل هو تخليق البنتاميدات السلفامويلية المشتقة من الليوسين ذات الأنشطة المضادة للأكسدة والمضادة للميكروبات. تم تخليق أميدات البنتاناميد السلفامويل القائمة على الليوسين الجديدة وتم استخدام التحليل العنصري، و1H-NMR، و13C-NMR، وFTIR لتوضيح هياكلها. خضعوا لتحقيقات ربط جزيئي بالإضافة إلى تحليلات النشاط المضاد للأكسدة والمضاد للميكروبات في المختبر. المركب 5a (0.60 جم/مل) كان المركب الأكثر نشاطًا ضد Pseudomonas aeroginosa، بينما كان المركب 5f (0.30-0.40 ملغ/مل) هو الأكثر فعالية كمضاد للبكتيريا ضد E. Coli و S. typhi و S. aureus و B. subtilis. المركبات ذات أفضل نشاط مضاد للفطريات ضد C. albican و A. niger، على التوالي، كانت 5g (0.80 ملغ/مل) و 5e (0.50 ملغ/مل). في تقييم النشاط المضاد للأكسدة في المختبر، أظهرت المركبات 5g (1.174µg/ml) و5h (1.172µg/ml) نشاطًا مضادًا للأكسدة مشابهًا لحمض الأسكوربيك (IC50 1.001µg/ml). بالإضافة إلى ذلك، فإن معظم المركبات المستهدفة تتمتع بقدرات قوية نسبيًا مضادة للبكتيريا والفطريات ومضادة للأكسدة، وفقًا لدراسة الربط الجزيئي. نظرًا لأن كل مركب مستهدف امتثل لقواعد ليبينسكي الخمسة، فمن المحتمل أن يتم استخدامه كمرشحين علاجيين لعلاج الأمراض المرتبطة بالإجهاد التأكسدي والعدوى الميكروبية.
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