Synthesis of Novel Bivalent Hydrazino-Thymohydroquinone Analogs Derived from Thymoquinone as Potential Antimicrobial Agents | ||
| Egyptian Journal of Chemistry | ||
| Article 38, Volume 64, Issue 12, December 2021, Pages 7229-7234 PDF (307.99 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2021.74154.3743 | ||
| Authors | ||
| Ahmed H. Abdelazeem* 1; Hany H Arab2; Alaa M. Alqahtani3; Mohamed F. El-Badway4; Yasser Mahmoud Ali Mohamed5 | ||
| 1Department of Medicinal Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt; Department of Pharmaceutical Sciences, College of Pharmacy, Riyadh Elm University, Riyadh 11681, Saudi Arabia. | ||
| 2Department of Pharmacology and Toxicology-Biochemistry division, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia | ||
| 3Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia; | ||
| 4Department of Microbiology and Immunology, Faculty of Pharmacy, University of Sadat City, 32897, Menuofia, Egypt | ||
| 5Photochemistry Department, National Research Center, Dokki, Giza, 12622, Egypt. | ||
| Abstract | ||
| In our previous work, it was reported that thymoquinone (TQ) and some thymohydroquinone (THQ) derivatives were used as precursors for the synthesis of potential anticancer agents. Hence, as a part of our ongoing program in the design of biologically active compounds derived from TQ scaffold we herein investigated the synthesis of homo- and heteronuclear thymol dimers tethered through various linkers such as ethylene, butylene, acetyl and N,N’-acetyl piperazine groups. The newly prepared compounds were examined as antimicrobial agents. Compounds 7 and 8 bearing a piperazine moiety exhibited highest antibacterial activity comparing to TQ, THQ and ampicillin especially against Staphylococcus aureus bacteria with MIC value of 16 µg/mL. All compounds showed moderate antifungal activity against Candida albicans and Aspergillus fumigatus. Together, the new TQ-based bivalent lead might be serving as a promising scaffold for development of novel and potent antimicrobial agents. | ||
| Keywords | ||
| Thymoquinone; Thymohydroquinone; Antimicrobial; Bivalent, Heteronuclear dimer | ||
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