تفاصيل الوثيقة

نوع الوثيقة : مقال في مجلة دورية 
عنوان الوثيقة :
Azole antimicrobial pharmacophore-based tetrazoles: Synthesis and biological evaluation as potential antimicrobial and anticonvulsant agents
Azole antimicrobial pharmacophore-based tetrazoles: Synthesis and biological evaluation as potential antimicrobial and anticonvulsant agents
 
الموضوع : كيمياء 
لغة الوثيقة : الانجليزية 
المستخلص : The azole pharmacophore is still considered a viable lead structure for the synthesis of more efficacious and broad spectrum antimicrobial agents. Potential antibacterial and antifungal activities are encountered with some tetrazoles. Therefore, this study presents the synthesis and antimicrobial evaluation of a new series of substituted tetrazoles that are structurally related to the famous antimicrobial azole pharmacophore. A detailed discussion of the structural elucidation of some of the newly synthesized compounds is also described. Antimicrobial evaluation revealed that twenty compounds were able to display variable growth inhibitory effects on the tested Gram positive and Gram negative bacteria with special efficacy against the Gram positive strains. Meanwhile, six compounds exhibited moderate antifungal activity against Candida albicans and Aspergillus fumigatus. Structurally, the antibacterial activity was encountered with tetrazoles containing a phenyl substituent, while the obtained antifungal activity was confined to the benzyl variants. Compounds 16, 18, 24 and 27 were proved to be the most active antibacterial members within this study with a considerable broad spectrum against all the Gram positive and negative strains tested. A distinctive anti-Gram positive activity was displayed by compound 18 against Staphylococcus aureus that was equipotent to ampicillin (MIC 6.25 μg/mL). On the other hand, twelve compounds were selected to be screened for their preliminary anticonvulsant activity against subcutaneous metrazole (ScMet) and maximal electroshock (MES) induced seizures in mice. The results revealed that five compounds namely; 3, 5, 13, 21, and 24 were able to display noticeable anticonvulsant activity in both tests at 100 mg/kg dose level. Compounds 5 and 21 were proved to be the most active anticonvulsant members in this study with special high activity in the ScMet assay (% protection: 100% and 80%, respectively 
ردمد : 0960-894X 
اسم الدورية : Bioorganic and Medicinal Chemistry 
المجلد : 17 
العدد : 6 
سنة النشر : 2009 هـ
2009 م 
عدد الصفحات : 12 
نوع المقالة : مقالة علمية 
تاريخ الاضافة على الموقع : Tuesday, October 13, 2009 

الباحثون

اسم الباحث (عربي)اسم الباحث (انجليزي)نوع الباحثالمرتبة العلميةالبريد الالكتروني
شريف أحمد رستمRostom, S.A.Fباحثدكتوراهsherifrostom@yahoo.com
Ashour, H.M.A.Ashour, H.M.A.باحثدكتوراه 
Razik, H.A.A.ERazik, H.A.A.Eباحثدكتوراه 
Fattah, A.E.F.H.A.E.Fattah, A.E.F.H.A.E.باحثدكتوراه 
El-Din, N.N.El-Din, N.N.باحثدكتوراه 

الملفات

اسم الملفالنوعالوصف
 23428.pdf pdfAbstract

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