Synthesis, Characterization, Molecular Docking, ADMET Study, and Antimicrobial Evaluation of New Mannich Bases of Isatin–Thiazole Imine Bases

Marwa Hashim Al-Musawi; May Mohammed Jawad Al-Mudhafar

doi:10.54133/ajms.v6i2.835

المؤلفون

Marwa Hashim Al-Musawi Department of Pharmaceutical Chemistry, College of Pharmacy, University of Baghdad, Baghdad, Iraq https://orcid.org/0009-0005-5516-0014
May Mohammed Jawad Al-Mudhafar Department of Pharmaceutical Chemistry, College of Pharmacy, University of Baghdad, Baghdad, Iraq https://orcid.org/0000-0002-9747-3140

DOI:

https://doi.org/10.54133/ajms.v6i2.835

الكلمات المفتاحية:

2-امينوثيازول ، الفعالية المضادة للميكروبات، ايزاتين ، قواعد مانك.

الملخص

يوجد جزيء الايزاتين في العديد من المواد الطبيعية ، مثل النباتات ، ويستخدم لتحضيرمركبات ذات أنشطة بيولوجية مختلفة. تم تصنيع سلسلة من قواعد شيف مانيك المشتقة من الإيزاتين في هذا البحث. أولا ، تم تحضير قواعد مانيك (2a-e) عن طريق تفاعل الإيزاتين مع الفورمالديهايد والأمينات الثانوية المختلفة (المورفولين ، البيبيريدين ، البيروليدين ، ثنائي إيثيل أمين ،وN -مثيل انيلين) بشكل منفصل. ثانيا ، تمت معالجة قواعد مانك;هذه مع 2-أمينوثيازول للحصول على المركبات النهائية المطلوبة (3a-e) وقد تم توصيف المركبات الجديدة على أساس بياناتها الطيفية(FT-IR) ،.(1H- NMR) تم فحص كل هذه المشتقات لنشاطها المضاد للميكروبات ضد اثنين من البكتيريا إيجابية الجرام. وهي "المكورات العنقودية الذهبية و Bacillus licheniformis" ، واثنين من البكتيريا سالبة الجرام. "الإشريكية القولونية و “Acinetobacter baumannii"، ونوع واحد من الفطريات المسماة: "المبيضات البيض". أظهرت النتائج ان معظم المركبات لها فعالية مضادة للميكروبات كبيرة والأكثر نشاطا هو المركب(3e) . وتم إجراء الالتحام الجزيئي للمركبات المركبة النهائية ثم مقارنتها بالأدوية القياسية (سيبروفلوكساسين وفلوكونازول) . سجل الالتحام الجزيئي درجات إرساء أعلى للمشتق النهائي (3e) مقارنة بالفلوكونازول بالإضافة إلى تسجيل درجات إرساء أعلى للمشتق النهائي (3d و (3e مقارنة بالسيبروفلوكساسين. بالأضافة الى ذلك تم دراسة حركية الدواء لمعرفة هل المركبات المحضرة ممكن اعطاؤها عن طريق الفم، وطريقة الأمتصاص والأنتشار ودرجة سميتها ضمن الضوابط المسموح بها طبيا.

التنزيلات

بيانات التنزيل غير متوفرة بعد.

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