Synthesis, molecular docking with COX 1 and II enzyme, ADMET screening and in vivo anti-inflammatory activity of oxadiazole, thiadiazole and triazole analogs of felbinac
المؤلفون المشاركون
Abd al-Salam, Aftab Ahmad
Husayn, Asif
Munawwir Imam, S.
Basha, Sayyid Husayn
Khan, Shah Alam
المصدر
Journal of Saudi Chemical Society
العدد
المجلد 22، العدد 4 (31 مايو/أيار 2018)، ص ص. 469-484، 16ص.
الناشر
تاريخ النشر
2018-05-31
دولة النشر
السعودية
عدد الصفحات
16
التخصصات الرئيسية
الملخص EN
Based on the core structure of Felbinac drug, three series (4a–d, 5a–d and 6a–n) of five membered heterocyclic derivatives containing three heteroatoms were designed and synthesized starting from Felbinac.
In the rational design of the target molecules, the biphenyl ring along with the methylene bridge of felbinac was retained while the carboxyl group was substituted with biologically active substituents like 1,2,4-triazole, 1,3,4-thiadiazole and 1,3,4-oxadiazole, with an intent to obtain novel, better and safer anti-inflammatory agents with improved efficacy.
The prepared molecules were then investigated for their anti-inflammatory, ulcerogenicity and analgesic activity in experimental animals.
The tested compounds exhibited varying degrees of inflammatory activity (25.21–72.87%), analgesic activity (27.50–65.24%) and severity index on gastric mucosa in the range of 0.20–0.80 in comparison to positive control felbinac (62.44%, 68.70% and 1.5, respectively).
Among all the prepared compounds, 2-(biphenyl-4-ylmethyl)-5-(4-chlorophenyl)-1,3,4-oxa diazole (6c) emerged as the most potent NSAID compound exhibiting the highest antiinflammatory activity (72.87% inhibition) and analgesic activity (65.24%) along with the least
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Khan, Shah Alam& Munawwir Imam, S.& Abd al-Salam, Aftab Ahmad& Basha, Sayyid Husayn& Husayn, Asif. 2018. Synthesis, molecular docking with COX 1 and II enzyme, ADMET screening and in vivo anti-inflammatory activity of oxadiazole, thiadiazole and triazole analogs of felbinac. Journal of Saudi Chemical Society،Vol. 22, no. 4, pp.469-484.
https://search.emarefa.net/detail/BIM-835400
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Khan, Shah Alam…[et al.]. Synthesis, molecular docking with COX 1 and II enzyme, ADMET screening and in vivo anti-inflammatory activity of oxadiazole, thiadiazole and triazole analogs of felbinac. Journal of Saudi Chemical Society Vol. 22, no. 4 (May. 2018), pp.469-484.
https://search.emarefa.net/detail/BIM-835400
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Khan, Shah Alam& Munawwir Imam, S.& Abd al-Salam, Aftab Ahmad& Basha, Sayyid Husayn& Husayn, Asif. Synthesis, molecular docking with COX 1 and II enzyme, ADMET screening and in vivo anti-inflammatory activity of oxadiazole, thiadiazole and triazole analogs of felbinac. Journal of Saudi Chemical Society. 2018. Vol. 22, no. 4, pp.469-484.
https://search.emarefa.net/detail/BIM-835400
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references : p. 483
رقم السجل
BIM-835400
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
تقوم هذه الخدمة بالتحقق من التشابه أو الانتحال في الأبحاث والمقالات العلمية والأطروحات الجامعية والكتب والأبحاث باللغة العربية، وتحديد درجة التشابه أو أصالة الأعمال البحثية وحماية ملكيتها الفكرية. تعرف اكثر