الفهرس | Only 14 pages are availabe for public view |
Abstract Resistance toantibioticsis an increasing problem worldwide which is mainly caused byβ-lactamases production.Such enzymes were divided into four classes ”A”, ”B”, ”C”, and” D”. <Also, there are no clinically available drugs capable of inhibiting any of class ”B” (MBLs). < Therefore, there is a crucial need to synthesize such inhibitors.It has been found that sulfur derivatives containing molecules which can coordinate to the zinc ions in the enzyme active site showed promising inhibition against MBLs. Several classes of compounds have been reported as MBL inhibitors, including thiol, thioester, sulfonic acid, 3-mercaptotriazole and thiosemicarbazide derivatives. In the present study, we shed some light on the MBLs inhibition activity of sulfonyl hydrazone, mercaptotriazole and thiosemicarbazide derivativesof pyrazole and quinoline nuclei. After that, some modifications on the parent structure were performed to form thehybrid derivatives. Then, only molecules with high binding affinities and docking score in the computational docking studies were synthesized and further investigatedm for the effect of such molecular variations on their biological activities. |