Document Type : Original Article
Authors
1
Department 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.
2
Department of Pharmacology and Toxicology-Biochemistry division, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia
3
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia;
4
Department of Microbiology and Immunology, Faculty of Pharmacy, University of Sadat City, 32897, Menuofia, Egypt
5
Photochemistry 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.
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