Keywords : Schiff base
Iraqi Journal of Pharmacy,
2021, Volume 18, Issue 2, Pages 180-193
Objectives: Green chemistry is the field that implies instruments and procedures, by which it offers significant environmental and financial benefits above traditional synthetic methods. The modern attention in green chemistry has pretended an additional need for organic synthesis in which different reaction environments must locate, which decreases the use of toxic organic solvents or toxic chemicals.
These green methods must enhance the selectivity, shorten reaction time, and make the products isolation simpler than the ordinary routes. In the 19th century, Hugo Schiff recorded the first synthesis of Schiff bases (imines). A Schiff base is considered as an aldehyde with a C=N group (azomethine group) in steed of the C=O group, It is normally produced by condensation of primary amines with aldehydes. Schiff bases entertain many important biologically and pharmaceutical activities and they are distinguished for their pharmacological action and wide-range applications in the food industry.
This study tries to focus on the green synthetic methods used for Schiff bases synthesis, in order to find the best technique that offers higher yields in shorter time within eco-friendly environment.
Conclusions: The review considered many green synthetics techniques, from which the microwaves irradiation method is considered to be the best followed by the ultrasonic, natural acids utilizing and grinding methods.
Design, synthesis, and evaluation the anti-β-lactamase activity of new sulphathiazole-derived monobactam compounds
Iraqi Journal of Pharmacy,
2020, Volume 17, Issue 1, Pages 19-36
Objectives: β-Lactams are the most successful antibiotics for the management of infectious diseases. Unfortunately, the bacterial production of β-lactamase that hydrolyzes the β-lactam ring can inactivate these drugs. The use of β-lactamase inhibitors like (clavulanic acid) in combination with the β-lactams may reduce this inactivation. The prevalent β-lactamase phenotype is the TEM-1 of class A released by Gram-positive and Gram-negative bacteria.
Methods: The docking study with TEM-1 β-lactamase lead to synthesize of new 5 monobactam compounds as the acid chloride derivatives reacted with the Schiff bases compound forming the monobactam ring. The final 5 synthesized compounds were characterized using physical and spectroscopic methods and tested biologically by evaluating their MIC values against 4 strains of β-lactamase Gram-positive and Gram-negative bacteria. The results were compared with those acquired from using clavulanic acid as a co-inhibiter with amoxicillin against the tested bacteria.
Results: The results revealed that 2 synthesized compounds showed an anti β-lactamase effect resemble to that of clavulanic acid.
Conclusion: As conclusion; the β-lactamase active pocket prefers hydrophobic substituents, as the synthesized products with these groups appeared to have the highest affinity.