In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal act... more In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal activities of new heterocyclic compounds bearing sulfadiazine moiety. Among the synthesized compounds, arylidine (3f) displayed significant antibacterial activity against S.pneumoniae (IC50, 22.46µg/mL, comparable to ampicillin IC50 value, 22.76 µg/mL),whereas, 2-pyridone (4f)showed the highest antifungal activity against G.candidum (IC50,8.63µg/mL, comparable to amphotericin B,IC50, 11.63 µg/mL).Its antibacterial activity against S.pneumoniae was (IC50,13.84 µg/mL, comparable to ampicillin, IC50, 22.76µg/mL) and E.coli (IC50,29.89 µg/mL, comparable to gentamycin ,IC50,29.42µg/mL) respectively.On the other hand 2-imino chromene (5a) displayed significant antibacterial activities against S.pneumoniae (IC50,19.84µg/mL, comparable to ampicillin , IC50, 22.76 µg/mL) and exhibited antifungal activity against G.candidum (IC50,12.63 µg/mL, comparable to amphotericin B, IC50 , 11.63 µg/mL) respecti...
Development of new antimicrobial agents is our target to overcome drug resistance problems. In th... more Development of new antimicrobial agents is our target to overcome drug resistance problems. In the present work, new chromenopyridone III-V, thiazole VI, hydrazoneVIIa-e, isoxazoleIX, pyrazole X, pyrazolopyrimidineXI and pyridazine XII derivatives containingsulfadiazine moiety were prepared and examined for their in-vitro antimicrobial activities. Among the synthesized compounds, the hydrazones VIIa,VIIc and pyrazoleX displayed significant antibacterial Docking results were in agreement with the biological evaluation results, and the newly synthesized compounds could act by the inhibition of microbial DHPS enzyme. The results provide important information for the futur design of more potent antimicrobial agents.
In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal act... more In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal activities of new heterocyclic compounds bearing sulfadiazine moiety. Among the synthesized compounds, arylidine (3f) displayed significant antibacterial activity against S.pneumoniae (IC50, 22.46µg/mL, comparable to ampicillin IC50 value, 22.76 µg/mL),whereas, 2-pyridone (4f)showed the highest antifungal activity against G.candidum (IC50,8.63µg/mL, comparable to amphotericin B,IC50, 11.63 µg/mL).Its antibacterial activity against S.pneumoniae was (IC50,13.84 µg/mL, comparable to ampicillin, IC50, 22.76µg/mL) and E.coli (IC50,29.89 µg/mL, comparable to gentamycin ,IC50,29.42µg/mL) respectively.On the other hand 2-imino chromene (5a) displayed significant antibacterial activities against S.pneumoniae (IC50,19.84µg/mL, comparable to ampicillin , IC50, 22.76 µg/mL) and exhibited antifungal activity against G.candidum (IC50,12.63 µg/mL, comparable to amphotericin B, IC50 , 11.63 µg/mL) respectively.In general,all of the synthesized compounds exhibited better antimicrobial activities than sulfadiazine. Molecular docking studies indicated that the newly synthesized compounds could occupy both p-aminobenzoic acid (PABA) and pterin binding pockets of the dihydropteroate synthase (DHPS), suggesting that the target compounds could act by the inhibition of microbial DHPS enzyme.These derivatives contain sulfonamide moiety as well as heterocyclic moiety that increase the lipophilic characters of the synthesized compounds hence enhance its absorption.
In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal act... more In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal activities of new heterocyclic compounds bearing sulfadiazine moiety. Among the synthesized compounds, arylidine (3f) displayed significant antibacterial activity against S.pneumoniae (IC50, 22.46µg/mL, comparable to ampicillin IC50 value, 22.76 µg/mL),whereas, 2-pyridone (4f)showed the highest antifungal activity against G.candidum (IC50,8.63µg/mL, comparable to amphotericin B,IC50, 11.63 µg/mL).Its antibacterial activity against S.pneumoniae was (IC50,13.84 µg/mL, comparable to ampicillin, IC50, 22.76µg/mL) and E.coli (IC50,29.89 µg/mL, comparable to gentamycin ,IC50,29.42µg/mL) respectively.On the other hand 2-imino chromene (5a) displayed significant antibacterial activities against S.pneumoniae (IC50,19.84µg/mL, comparable to ampicillin , IC50, 22.76 µg/mL) and exhibited antifungal activity against G.candidum (IC50,12.63 µg/mL, comparable to amphotericin B, IC50 , 11.63 µg/mL) respecti...
Development of new antimicrobial agents is our target to overcome drug resistance problems. In th... more Development of new antimicrobial agents is our target to overcome drug resistance problems. In the present work, new chromenopyridone III-V, thiazole VI, hydrazoneVIIa-e, isoxazoleIX, pyrazole X, pyrazolopyrimidineXI and pyridazine XII derivatives containingsulfadiazine moiety were prepared and examined for their in-vitro antimicrobial activities. Among the synthesized compounds, the hydrazones VIIa,VIIc and pyrazoleX displayed significant antibacterial Docking results were in agreement with the biological evaluation results, and the newly synthesized compounds could act by the inhibition of microbial DHPS enzyme. The results provide important information for the futur design of more potent antimicrobial agents.
In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal act... more In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal activities of new heterocyclic compounds bearing sulfadiazine moiety. Among the synthesized compounds, arylidine (3f) displayed significant antibacterial activity against S.pneumoniae (IC50, 22.46µg/mL, comparable to ampicillin IC50 value, 22.76 µg/mL),whereas, 2-pyridone (4f)showed the highest antifungal activity against G.candidum (IC50,8.63µg/mL, comparable to amphotericin B,IC50, 11.63 µg/mL).Its antibacterial activity against S.pneumoniae was (IC50,13.84 µg/mL, comparable to ampicillin, IC50, 22.76µg/mL) and E.coli (IC50,29.89 µg/mL, comparable to gentamycin ,IC50,29.42µg/mL) respectively.On the other hand 2-imino chromene (5a) displayed significant antibacterial activities against S.pneumoniae (IC50,19.84µg/mL, comparable to ampicillin , IC50, 22.76 µg/mL) and exhibited antifungal activity against G.candidum (IC50,12.63 µg/mL, comparable to amphotericin B, IC50 , 11.63 µg/mL) respectively.In general,all of the synthesized compounds exhibited better antimicrobial activities than sulfadiazine. Molecular docking studies indicated that the newly synthesized compounds could occupy both p-aminobenzoic acid (PABA) and pterin binding pockets of the dihydropteroate synthase (DHPS), suggesting that the target compounds could act by the inhibition of microbial DHPS enzyme.These derivatives contain sulfonamide moiety as well as heterocyclic moiety that increase the lipophilic characters of the synthesized compounds hence enhance its absorption.
Uploads
Papers by aml sabry