Author(s): Nedaa A. Hameed A. Rahim, Sumayah Saadi Abbas, Sahar B. Aljuboori, Ammar A Razzak Mahmood

Email(s): nedaarahim@yahoo.com

DOI: 10.52711/0974-360X.2021.00715   

Address: Nedaa A. Hameed A. Rahim1, Sumayah Saadi Abbas1, Sahar B. Aljuboori2, Ammar A Razzak Mahmood1*
1College of Pharmacy, Dept. of Pharmaceutical Chemistry, Baghdad, University Baghdad-Bab-Almudam- 10001, Iraq.
2College of Al-Rafiden University- Dept. of Pharmacy-Baghdad-Iraq.
*Corresponding Author

Published In:   Volume - 14,      Issue - 8,     Year - 2021


ABSTRACT:
Objective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the preparation compounds. The synthesized derivatives against (Gram positive bacteria GPB) (Bacillus subtilis) and two (Gram-negative bacteria GNB) (Klebsiella pneumoniae and Escherichia coli) and (one fungal species Candida albicans), have been evaluated to their antibacterial activity in vitro. all results showed which most of them have good antibacterial activity, while their antifungal activity revealed that compounds displayed slight antifungal activity. The synthesized Benzoxazole derivatives were docked using, glucosamine 6-phosphate synthase as a ligand. Conclusion: The antimicrobial activity indicates that compounds (4), (7) and (8) have more potent antibacterial activity than the compounds (5) and (6). Molecular docking study revealed that compounds (7) and (8), with bulky phenyl groups are essential to block the active centers of (GluN-6-Ps) amino acids synthase in the bacteria.


Cite this article:
Nedaa A. Hameed A. Rahim, Sumayah Saadi Abbas, Sahar B. Aljuboori, Ammar A Razzak Mahmood. Synthesis, Antimicrobial evaluation and Docking study of new Schiff bases of benzo[d]oxazol-5-amine derivatives. Research Journal of Pharmacy and Technology. 2021; 14(8):4129-6. doi: 10.52711/0974-360X.2021.00715

Cite(Electronic):
Nedaa A. Hameed A. Rahim, Sumayah Saadi Abbas, Sahar B. Aljuboori, Ammar A Razzak Mahmood. Synthesis, Antimicrobial evaluation and Docking study of new Schiff bases of benzo[d]oxazol-5-amine derivatives. Research Journal of Pharmacy and Technology. 2021; 14(8):4129-6. doi: 10.52711/0974-360X.2021.00715   Available on: https://rjptonline.org/AbstractView.aspx?PID=2021-14-8-21


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