Ahmed A. J. Mahmood; Mohammed A. Al-Iraqi; Faris T. Abachi
Abstract
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 ...
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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.
Faris T. Abachi; Khadeeja Younus; Inas Hazim
Abstract
Objective: The molecular characterization of some bioactive compounds in ginger interest because of their various pharmacological activities. To the best of our knowledge, we are isolate hydrocarbon (low molecular weight), alcohol, phenol, acid, ester from nonpolar (oil) and polar (ethanol) extracts ...
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Objective: The molecular characterization of some bioactive compounds in ginger interest because of their various pharmacological activities. To the best of our knowledge, we are isolate hydrocarbon (low molecular weight), alcohol, phenol, acid, ester from nonpolar (oil) and polar (ethanol) extracts using gas chromatography-mass spectrometry [GC-MS] technique. Methods: Gas chromatography-mass spectrometry (GC-MS) analysis of the oil and ethanol extracts of ginger was carried out by using a GC-MS equipment. Results: The GC-MS analysis has revealed the existence of different bioactive chemical compounds in the oil & ethanolic extracts of ginger. The major compounds of oil extract are beta-elemene (0.27%), curcumen (3.12%), zingerberene (10.86%) , bisabolene(3.75) , elemol(1.14%), germacrene( 0.23%) , 7-epi trans sesquisabinene (1.82%), zingerberone (35.92%), ethyl palmitate (0.53%), pardol(3.97%). A total of 53 compounds identified representing of total ginger oil extract. While, the major compounds of ethanolic extract are elmene (0.51%), zingerbiene (4.43%), alloaromadentrene (0.42%), curcumene(21.83%), gama cadienene(3.24%)8-epi-.gama.-eudesmol( 0.34). A total of 50 compounds identified representing 99.98% of total ginger ethanolic extract. Conclusion: In this study, successful identification some of important bioactive compounds using GC-MS technique.
Ahmed A. Mahmood; Mohammed A. Al-Iraqi; Faris T. Abachi
Abstract
Objective:To evaluate the role of fluorine atom in modern drug synthesis. Methods: Different types of fluorinated were prepared, antimicrobials, antivirals, F-NSAIDs, peptides and protein synthesis. Results: Recent developments and future prospects of fluorine in medicinal chemistry and chemical ...
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Objective:To evaluate the role of fluorine atom in modern drug synthesis. Methods: Different types of fluorinated were prepared, antimicrobials, antivirals, F-NSAIDs, peptides and protein synthesis. Results: Recent developments and future prospects of fluorine in medicinal chemistry and chemical biology. The extraordinary potential of fluorine - containing biologically relevant molecules in antimicrobial or antivirial agents, or peptide or protein chemistry, medicinal chemistry, chemical biology, pharmacology, and drug discovery as well as diagnostic and therapeutic applications, was recognized by researchers who are not in the traditional fluorine chemistry field, and thus the new wave of fluorine chemistry has been rapidly expanding its biomedical frontiers. Conclusion: This review how to list of fluorinated drugs( Antimicrobial agents , anticancer agents, Antiviral agents, and study their physicochemical properties of fluorine drugs.