الفهرس 
IntroductionOnly 14 pages are availabe for public view
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Abstract
Incorporation of benzocaine and other pharmacophores could affect the biological activities of synthesized compounds in different ways. The Antibacterial properties were evaluated against gram positive and negative bacteria to get some potent derivatives against positive strains more than the negative ones. The thiophene derivatives especially 30b recorded the best inhibition to bacterial growth in contract to thiazole derivatives. Triazine and arylidene displayed good results while some of hydrazone and pyridones showed no activity. For pyrazole derivatives, pyrazolopyrmidine 40 was the best core with inhibition equal to 66.6% against S.aureus species. Furthermore, MOE docking was implemented to one of the highest antibacterial compound 30b and 40 stimulated their interaction with four infected S. aureus proteins with promising docking score. Evaluation DNA-binding assay for some of benzocaine derivatives to highlight thiol 28 and thiophene 30b as the potent cores. QSAR studies was performed to match the experimental result to highlight the thiophene 30b as a potent DNA-binding compound. Then anti-oxidant activities was accomplished via different methodologies as DPPH & ABTS methods to outcome thiazolidine 26, pyrazole derivative 32 and pyrazolopyrimidinone 47 which are considered as the best antioxidant compounds. It is hoped that this effective strategy will be used for developing even more potent compounds in medicinal chemistry. Furthermore, five potent compounds recorded antitumor activity on Hep-G2 carcinoma using Doxorubicin as a positive control. The more potent compound was chloroacetamide derivative 51 with IC50 equal 3.6 mg/ml. The other compounds followed the order 48>40>37>32 with IC50 equal 17.7, 24.4, 37 and 41mg/ml. Interestingly, Liplinski rule were in acomplete agreement with potent compounds.