قدمت سعادة الدكتورة هند نجاح في قسم الكيمياء محاضرة علمية بعنوان :
Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine
Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent
وذلك يوم الثلاثاء 8-6-1438 على الساعة 9:30 في قاعة رقم 1C-225 بمبنى كلية العلوم.
وقد حضر الندوة بعض أعضاء هيئة التدريس بالقسم، وكانت لمشاركتهم الأثر الأكبر في الإستفادة العلمية وإثراء النقاش حول تصنيع المركبات العضوية وفعاليتها البيولوجية وتصنيع الأدوية..
ملخص المحاضرة :
A series of novel pyrazole-5-carboxylate containing N-triazole derivatives has been synthesized; different heterocyclic amines Ethyl 4-amino-1-(4-(substituted) butyl))-3-(4-chlorophenyl)-1H-pyrazole-5-carboxylate and (E)-Ethyl 4-amino-1-(4-( substituted)but-2-en-1-yl)-3-(4-chlorophenyl)-1H-pyrazole-5-carboxylate. pyrazolo[4,3-d]pyrimidine containing sulfa drugs and oxypyrazolo[4,3-d] pyrimidine derivatives 3-(4-Chlorophenyl)-5-methyl-7-oxybutyl)-isoindoline-1,3-dioxo-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin & 3-(4-Chlorophenyl)-5-methyl-7-(prop-2-en-1-yloxy)-1H-pyrazolo[4,3-d]pyrimidine & 3-(4-Chlorophenyl)-7-(ethynyloxy)-5-methyl-1H-pyrazolo[4,3-d]pyrimidine has been synthesized.
The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. All compounds have been screened for their in vitro antimicrobial activity against three gram-positive and gram-negative bacteria as well as three fungi. The results revealed that compounds N-(2,6-Dimethoxypyrimidin-4-yl)-4-3-(4-chlorophenyl)-7-oxo-6-[3-(3-phenylthioureido)-6,7-dihydro-1Hpyrazolo[4,3-d]pyrimidine-5-ylamino)benzenesulfonamide and oxypyrazolo[4,3-d] pyrimidine derivatives 3-(4-Chlorophenyl)-5-methyl-7-oxybutyl)-isoindoline-1,3-dioxo-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin had more potent antibacterial activity against all bacterial strains than reference drug Cefotaxime. Moreover compounds 4-Amino-3-(4-chlorophenyl)-1-[2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl]-1H-pyrazole-5-carboxylic acid & Ethyl 4-amino-1-(4-(4-methylpiperazin-1-yl)butyl)-3-(4-chlorophenyl)-1H-pyrazole-5-carboxy-late showed excellent antifungal activities against Aspergillus niger and Candida albicans in low inhibitory concentrations but slightly less than the reference drug miconazole against Aspergillus flavus.