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Abstract
In order to overcome the challenges of microbial resistance as well as to improve the effectiveness and selectivity of chemotherapeutic agents against cancer, a novel series of 4-(4-bromophenyl)-thiazol-2-amine derivatives was synthesized and its molecular structures were confirmed by physicochemical and spectral characteristics. The synthesized compounds were further evaluated for their in vitro antimicrobial activity using turbidimetric method and anticancer activity against oestrogen receptor positive human breast adenocarcinoma cancer cell line (MCF7) by Sulforhodamine B (SRB) assay. The antimicrobial activity results revealed that compound p2, p3, p4 and p6 exhibited promising antimicrobial activity that are comparable to standard norfloxacin (antibacterial) and fluconazole (antifungal). Anticancer screening results demonstrated that compound p2 was found to be the most active one against cancer cell line when compared to the rest of the compounds and comparable to the standard drug (5-fluorouracil). The molecular docking study demonstrated that compounds, p2, p3, p4 and p6 displayed good docking score within binding pocket of the selected PDB ID (1JIJ, 4WMZ and 3ERT) and showed promising ADME properties.
Highlights
In recent years, epidemiological studies confirmed the significant negative impact of infections caused by pathogenic bacteria and fungi against human health
Research is focused towards new antimicrobial agents with expansion of bioactivity of existing drugs and with novel target so as to address the problem of resistance [2]
Chemistry Synthesis of intermediate and target derivatives (p1–p10) were carried out as per the reactions outlined in Scheme 1
Summary
Epidemiological studies confirmed the significant negative impact of infections caused by pathogenic bacteria and fungi against human health. Large-scale surveillance revealed increasing incidence of drug-resistance that had compromised the efficacy of antimicrobial therapy. The increased emergence of multidrug-resistant pathogenic bacteria has called for exploration of alternative drug therapies [1]. Research is focused towards new antimicrobial agents with expansion of bioactivity of existing drugs and with novel target so as to address the problem of resistance [2]. In this era, cancer remains as one of the most serious clinical problems and the second primary cause of deaths worldwide.
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