A new class of nifuroxazide analogues: Synthesis of 5-nitrothiophene derivatives with antimicrobial activity against multidrug-resistant Staphylococcus aureus
“…1 There is a real need for discovery of new compounds endowed with antimicrobial activity, possibly acting through mechanisms of actions, which are distinct from those of well known classes of antimicrobial agents to which many clinically relevant pathogens are now resistant. 2 Hydrazide analogues also possess other biological activities like anticonvulsant, 3 antidepressant, 4 anti-inflammatory, 5 antimalarial, 6 antimycobacterial, 7 anticancer 8 and antimicrobial [9][10][11][12] activities. QSAR is one of the oldest and most widely used methods in computational drug design.…”
Development of new antimicrobial agents is increasingly important due to the resistance of microbes to the known antimicrobial drugs. In the present work substituted benzoic acid hydrazides (1-10) were condensed with substituted aromatic and heteroaromatic aldehydes to yield the target products (11)(12)(13)(14)(15)(16)(17)(18)(19)(20). The synthesized compounds were tested in vitro for their antimicrobial activity against Gram positive, Gram negative bacterial and fungal species. The QSAR analysis applied to determine the correlation of antimicrobial activity of substituted hydrazide derivatives with their physicochemical properties indicated the importance of electronic parameters, dipole moment (µ) and energy of lowest unoccupied molecular orbital (LUMO) in describing antibacterial and antifungal activity respectively.
“…1 There is a real need for discovery of new compounds endowed with antimicrobial activity, possibly acting through mechanisms of actions, which are distinct from those of well known classes of antimicrobial agents to which many clinically relevant pathogens are now resistant. 2 Hydrazide analogues also possess other biological activities like anticonvulsant, 3 antidepressant, 4 anti-inflammatory, 5 antimalarial, 6 antimycobacterial, 7 anticancer 8 and antimicrobial [9][10][11][12] activities. QSAR is one of the oldest and most widely used methods in computational drug design.…”
Development of new antimicrobial agents is increasingly important due to the resistance of microbes to the known antimicrobial drugs. In the present work substituted benzoic acid hydrazides (1-10) were condensed with substituted aromatic and heteroaromatic aldehydes to yield the target products (11)(12)(13)(14)(15)(16)(17)(18)(19)(20). The synthesized compounds were tested in vitro for their antimicrobial activity against Gram positive, Gram negative bacterial and fungal species. The QSAR analysis applied to determine the correlation of antimicrobial activity of substituted hydrazide derivatives with their physicochemical properties indicated the importance of electronic parameters, dipole moment (µ) and energy of lowest unoccupied molecular orbital (LUMO) in describing antibacterial and antifungal activity respectively.
“…Several hydrazidehydrazone derivatives have shown antimicrobial, antiviral, antimalarial, anticonvulsant, antiinflammatory, antituberculosis, antitumor, antiplatelet aggregation, antileishmanial, analgesic and antimalarial properties [4][5][6][7][8][9][10][11][12]. Furthermore, various substituted pyridines were recorded to exhibit antibacterial, anti-inflammatory and antitumor activity [13][14][15].…”
“…Structurally, a Schiff's base (also known as imine or azomethine) is a nitrogen analogue of an aldehyde or ketone in which the carbonyl group has been replaced by an imine or azomethine group. Schiff's bases of pyrazole aldehydes and aromatic amines exhibit a wide range of biological activities such as antifungal [1], antibacterial [2] and antitubercular [3] etc. The biological significance of this class of compounds impelled us to continue working on the synthesis of new schiff's bases of pyrazole derivatives.…”
Results: Compounds 3a,3b,3d,3j,3l,4d,4e,4j,4l,4m,5e,5g,5h,5n exhibited excellent to good antibacterial activity as compared to reference drugs.
Conclusion
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