Synthesis, Evolution Anticancer and Microbial Activity of Some 1,3,4-Oxadiazoles Analogues | ||||
| The Egyptian Journal of Hospital Medicine | ||||
| Article 109, Volume 89, Issue 2, October 2022, Page 6803-6808 PDF (684.56 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ejhm.2022.270823 | ||||
 View on SCiNiTO | ||||
| Authors | ||||
Esraa Mohammed Jawad Mohsen  ; Israa Sami Hadi
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| Abstract | ||||
| Introduction: The need to develop anti-cancer drugs and the increasing bacteria resistance towered many antibiotics have made researchers more interested in testing the ability of synthetic derivatives to inhibit different types of microorganisms, although studying the cytotoxicity effect on various species of cancer cells. Aim: synthesis methyl nicotinate derivatives and evolution their anti-microbial and anti-cancer ability. Material and methods: a series of 1,3,4-oxadiazole heterocyclic compounds were synthesized, a nicotinoyl hydrazine was synthesized by refluxed methyl nicotinate and hydrazine hydrate. a good yield of Schiff bases was isolated by a reaction equimolar quantity of nicotinoyl hydrazine with several aromatic aldehydes. Up on Schiff bases acylation, heterocyclic compounds were collected, and synthetic derivatives were identified using Infra-Red (IR), Hydrogen Nuclear Magnetic Resonance (1HNMR). The methyl thiazolyl tetrazolium (MTT) Method was used for the Evolution of anti-cancer activity. Well diffusion method over agar was used to determine antibacterial activity, gram-positive and gram-negative bacteria were used to test the strength of inhibition for synthesis derivatives. Results: a white solid of nicotinoyl hydrazine was isolated, different Schiff bases were separated in a high yield, and 1,3,4-oxadiazole analogues were collected. The inhibition values of the prepared derivatives towards bacterial growth were measured. Cytotoxicity was an accounted for Schiff bases and 1,3,4-oxadiazole analogues. Conclusion: Three oxadiazole heterocyclic compounds show moderate activity. In contrast, two showed excellent inhibition toward cancer cell and bacteria growth greatly depending on the type and position of substituent groups in different hetero cyclic compounds. | ||||
| Keywords | ||||
| 1; 3; 4-Oxadiazole; Schiff bases acylation; Methyl nicotinoyl hydrazine | ||||
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