The non-toxic inorganic antimicrobial agents iodine (I2) and copper (Cu) are interesting alternatives for biocidal applications. Iodine is broad-spectrum antimicrobial agent but its use is overshadowed by compound instability, uncontrolled iodine release and short-term effectiveness. These disadvantages can be reduced by forming complex-stabilized, polymeric polyiodides. In a facile, in-vitro synthesis we prepared the copper-pentaiodide complex [Cu(H2O)6(12-crown-4)5]I6 ´ 2I2, investigated its structure and antimicrobial properties. The chemical structure of the compound has been verified. We used agar well and disc-diffusion method assays against nine microbial reference strains in comparison to common antibiotics. The stable complex revealed excellent inhibition zones against C. albicans WDCM 00054, and strong antibacterial activities against several pathogens. [Cu(H2O)6(12-crown-4)5]I6 ´ 2I2 is a strong antimicrobial agent with an interesting crystal structure consisting of complexes located on an inversion center and surrounded by six 12-crown-4 molecules forming a cationic substructure. The six 12-crown-4 molecules form hydrogen bonds with the central Cu(H2O)6 . The anionic substructure is a halogen bonded polymer which is formed by formal I5− repetition units. The topology of this chain-type polyiodide is unique. The I5− repetition units can be understood as a triodide anion connected to two iodine molecules.
Our previous work identified isoxazole-based chalcones and their dihydropyrazole derivatives as two important five-membered heterocycles having antitubercular activity. Hence, in the present study, we biologically evaluated 30 compounds, including 15 isoxazole ring-containing chalcones (17–31) and 15 dihydropyrazoles (32–46) derived from these chalcones for their antimicrobial, antioxidant, and anticancer activities. Chalcones exhibited superior antibacterial and antioxidant activities compared to dihydropyrazoles. Among the chalcones, compound 28 showed potent antibacterial (MIC = 1 µg/mL) and antioxidant activities (IC50 = 5 ± 1 µg/mL). Dihydropyrazoles, on the contrary, demonstrated remarkable antifungal and anticancer activities. Compound 46 (IC50 = 2 ± 1 µg/mL) showed excellent antifungal activity whereas two other dihydropyrazoles 45 (IC50 = 2 ± 1 µg/mL) and 39 (IC50 = 4 ± 1 µg/mL) exhibited potential anticancer activity. The compounds were also tested for their toxicity on normal human cell lines (LO2) and were found to be nontoxic. The active compounds that have emerged out of this study are potential lead molecules for the development of novel drugs against infectious diseases, oxidative stress, and cancer.
Nano-sized metals have been introduced as a promising solution for microbial resistance to antimicrobial agents. Silver nanoparticles (AgNPs) have been proven to possess good antimicrobial activity. Green synthesis of AgNPs has been reported as safe, low cost and ecofriendly. This methodology uses extracts originating from different plants to reduce silver ions from AgNO 3 into nano-sized particles. In this study, extracts of several plants including ginger, garlic, capsicum and their mixtures were successfully used to produce AgNPs. Numerous spectroscopic, light scattering and microscopic techniques were employed to characterize the synthesized AgNPs. Agar well diffusion assay was performed to investigate the antimicrobial activity of AgNPs. The biosynthesized AgNPs have spherical shape with a size range of 20-70 nm. Garlic extract, pure or in mixture with ginger extract, generated AgNPs of the smallest size. The presence of the plant-origin capping agents surrounding AgNPs was proven by Fourier-transform infrared spectroscopy. The AgNPs, at a concentration of 50 µg/mL, demonstrated potent antimicrobial activity against Staphyloccocus aureus, Escherichia coli and Candida albicans as indicated by the zones of inhibitions. Our results revealed that AgNPs having potent antimicrobial activity could be prepared using different pure plant extracts and their mixtures.
Carbon nitride-catalyzed photocatalytic strategies for the oxidation of alcohols, reduction of nitro compounds, coupling reactions, and synthesis of esters, phenols, and sulfoxides have been summarized.
A bstract Background: E-commerce of medicines has been extensively spread worldwide. Many reasons influence consumers to purchase their medical needs through the Internet, including low cost, availability, accessibility, and time saving. However, most of these medicines are substandard and counterfeit. Aim: To assess the perception of people in the UAE about purchasing medicines from online sources and to evaluate the quality of furosemide tablets from two different sources including illegal online source. Materials and Methods: A cross-sectional study was conducted on 528 participants in the UAE. The questionnaire included three parts to assess the public perception and experience toward purchasing medicines from online sources. Furosemide tablets, purchased from the UAE market and an illegal online source, were physically and chemically studied to assess their quality according to the British Pharmacopoeia (2018). Results: The survey results revealed that less than 10% of participants have purchased their medicines from online sources and mostly they were nonprescription products (78%). Most common motives for online purchasing were either unavailability in the local pharmacies (43%) or lower cost compared to that in local market (43%). The opinion of participants toward purchasing of online medicines was negative. On the other hand, the experimental analysis showed that online furosemide had failed to pass the chemical assay test (91.0% ± 0.8), which makes it a substandard product. Conclusion: This study showed that few consumers had considered purchasing pharmaceutical products from online sources as a feasible way to save money and time. However, most of them were in doubt about their quality, which encourages health-care providers to guide patients to government-supported websites if required. The study also showed that the quality of online medicines is questionable, indicating that these products are not equally effective as the medicines purchased from a local pharmacy.
Despite the availability of many drugs to treat infectious diseases, the problems like narrow antimicrobial spectrum, drug resistance, hypersensitivities and systemic toxicities are hampering their clinical utility. Based on the above facts, in the present study, we designed, synthesized and evaluated the antibacterial and antifungal activity of novel fluorinated compounds comprising of chalcones bearing trifluoromethyl (A1–A10) and trifluoromethoxy (B1–B10) substituents. The compounds were characterized by spectroscopic techniques and evaluated for their antimicrobial activity against four pathogenic Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Escherichia coli and Bacillus subtilis) bacterial and fungal (Candida albicans and Aspergillus niger) strains. In this study, the compounds with trifluoromethoxy group were more effective than those with trifluoromethyl group. Among the 20 fluorinated chalcones, compound A3/B3 bearing an indole ring attached to the olefinic carbon have been proved to possess the most antimicrobial activity compared to the standard drugs without showing cytotoxicity on human normal liver cell line (L02). Further, the minimum inhibitory concentration (MIC) for A3/B3 was determined by serial tube dilution method and showed potential activity. These results would provide promising access to future study about the development of novel agents against bacterial and fungal infections.
Infectious diseases caused by fungi and mycobacteria pose an important problem for humankind. Similarly, cancer is one of the leading causes of death globally. Therefore, there is an urgent need for the development of novel agents to combat the deadly problems of cancer, tuberculosis, and also fungal infections. Hence, in the present study, we designed, synthesized, and characterized 30 compounds including 15 chalcones (2–16) and 15 dihydropyrazoles (17–31) containing dichlorophenyl moiety and also screened these compounds for their antifungal, antitubercular, and antiproliferative activities. Among these compounds, the dihydropyrazoles showed excellent antifungal and antitubercular activities whereas the chalcones exhibited promising antiproliferative activity. Among the dihydropyrazoles, compound 31 containing 2-thienyl moiety showed promising antifungal activity (MIC 5.35 µM), whereas compounds 22 and 24 containing 2,4-difluorophenyl and 4-trifluoromethyl scaffolds revealed significant antitubercular activity with the MICs of 3.96 and 3.67 µM, respectively. Compound 16 containing 2-thienyl moiety in the chalcone series showed the highest anti-proliferative activity with an IC50 value of 17 ± 1 µM. The most active compounds identified through this study could be considered as starting points in the development of drugs with potential antifungal, antitubercular, and antiproliferative activities.
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