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Abstract Diosgenin, a hydrolyzed product of phytosteroid saponin, has widely been studied for its medicinal properties. In an effort to find bioactive molecules, 25 novel thiazole‐fused diosgenin molecules have been synthesized by an efficient reaction protocol. The chemistry involves the Oppenauer oxidation followed by double bond isomerization in a one‐pot reaction, epoxidation, and the reaction of urea derivatives with the epoxyketone to synthesize the target compounds. These novel chimeric compounds were tested for their potential antimicrobial and cytotoxic properties. Antimicrobial studies against a panel of Gram‐positive and Gram‐negative led to the discovery of some of these molecules as narrow‐spectrum antimicrobial agents againstBacillus subtilisbacteria. In preliminary cytotoxicity studies, 2‐fluorophenyl derivative (10) inhibited the growth of several cell lines of the NCI‐60 cell line panels including >93 % inhibition of UO‐31 cell line. Furthermore, the hit antibacterial compounds are non‐toxic to human cancer cell lines, and the cytotoxic compound is not active against the bacterial strains, showing the selective therapeutic potential of the chimeric compounds. 

Verbena officinalis is commonly used in traditional medicine to treat many ailments. Extracts of this plant are therapeutic agents for the potential treatment of different diseases, including colorectal and liver cancers, but have not been explored for their anti-melanoma potential so far. The goal of the current work was to prepare a methanolic extract and fractionate it using hexane, chloroform, ethyl acetate, butanol, and acetone to get semi-purified products. These semi-purified fractions were studied for their potency against melanoma cell lines. The three potent fractions (HA, VO79, and EA3) demonstrated 50% inhibition concentration (IC50) values as low as 2.85 µg/mL against the LOX IMVI cell line. All three fractions showed similar potency in inhibiting the growth of the B16 cells, a murine melanoma cell line. Based on high-resolution mass spectrometry (HRMS) data, for the first time, we report on lupulone A from this plant. LC-MS data also indicated the presence of hedergonic acid, serjanic acid, and other compounds in V. officinalis extracts. 

From a library of compounds, 11 hit antibacterial agents have been identified as potent anti-Gram-positive bacterial agents. These pyrazole derivatives are active against two groups of pathogens, staphylococci and enterococci, with minimum inhibitory concentration (MIC) values as low as 0.78 μg/mL. These potent compounds showed bactericidal action, and some were effective at inhibiting and eradicating Staphylococcus aureus and Enterococcus faecalis biofilms. Real-time biofilm inhibition by the potent compounds was studied, by using Bioscreen C. These lead compounds were also very potent against S. aureus persisters as compared to controls, gentamycin and vancomycin. In multiple passage studies, bacteria developed little resistance to these compounds (no more than 2 × MIC). The plausible mode of action of the lead compounds is the permeabilization of the cell membrane determined by flow cytometry and protein leakage assays. With the detailed antimicrobial studies, both in planktonic and biofilm contexts, some of these potent compounds have the potential for further antimicrobial drug development.