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Thalassemia is a genetic disease that significantly affects human health. The common treatment of thalassemia is the regular injection of red blood cell, which is associated with the accumulation of iron in different tissues of the body, and makes chelation therapy necessary. Deferiprone and deferoxamine are broadly used as iron chelating agents in the vast majority of thalassemia cases. In this study, an efficient method for the synthesis of deferiprone was used by reacting maltol with methylamine in a mixture of water and ethanol as solvent. The structure of deferiprone was assigned using different spectroscopic techniques such as IR, 1H-NMR, and 13C-NMR. The advantages of this pathway are simple, practical, one-pot cascade, mild condition and high yield. The statistics of the Ministry of Health of Iran show the growing trend of deferiprone drug consumption in the country. Therefore, the domestic preparation of this drug can help the pharmaceutical industry in order to reduce costs and make it available for target patients. [ABSTRACT FROM AUTHOR]

A new class of 3‐hydroxypyridine‐4‐one derivatives was synthesized and screened against several Gram‐positive and Gram‐negative bacteria, as well as two species of fungi. Among these synthesized compounds, the substituted derivatives with ortho‐ and para‐nitro and para‐methoxy groups showed the highest antibacterial activities against S. aureus and E. coli species with MIC value of 32 μg/mL, which were more potent compared to ampicillin as a reference drug. Furthermore, the substituted derivatives with ortho‐methoxy, ortho‐, para‐chloride, ortho‐, and para‐hydroxy groups exhibited MIC values of 64 μg/mL against S. aureus and E. coli species. In addition, the synthesized compounds were evaluated for their antifungal activities against C. albicans and A. niger strains. The best antifungal activity was observed for compounds with ortho‐methoxy, ortho‐hydroxy, and para‐methyl substitutions against A. niger species with MIC values of 64 μg/mL. The analysis of the antimicrobial results revealed that the type and position of the phenyl ring substituents greatly influence the antimicrobial activities of the synthesized compounds. Subsequently, molecular docking studies on E. coli species were performed to predict the interaction mode of these compounds in the active site of the receptor. Also, in silico ADME profile outputs showed that the compounds comply with the rule of five. [ABSTRACT FROM AUTHOR]

In recent years, resistance to conventional antimicrobial drugs has become a serious concern in the clinic. Hence, the discovery of novel and effective antimicrobial agents with improved properties is of great value. In this study, the antibacterial and anticandidal activities of some imidazole, benzimidazole and benztriazole derivatives (C1-C8) against several species of Gram-positive and Gram-negative bacteria, including Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli and Salmonella typhi as well as one species of fungi including Candida albicans, were evaluated using Clinical & Laboratory Standards Institute (CLSI) method. Antimicrobial evaluation revealed that among the tested compounds, imidazole derivative (C5) indicated the highest activity against bacterial strains and Candida albicans. It was found that compound C5 is more potent than ampicillin against S. aureus strain (MIC =2-16 µg/mL) and possessed excellent anticandidal activity (MIC =1 µg/mL) which was comparable to Amphotericin B as the positive control. In addition, cytotoxic activity of the tested compounds was investigated using MTT assay. The results of MTT assay demonstrated that the toxicity of the tested compounds was less than 35%. [ABSTRACT FROM AUTHOR]

Sustainable development is one of the important subjects of our world. It means supporting the needs of current populations without dangerous effects on the resources of future generations. This subject finds its vital role in different sciences and is an effort based on sustainable development goals (SDG), defined by the United Nations (in United Nations General Assembly) in 2015. In this paper, two parks, Qeytariyeh park and Niyavaran park located in Northern Tehran, Iran, were studied according to SDG. The study was designed specifically around goal 11 of United Nations General Assembly and the application of sustainable development in cities. After a literature review of research, the parks were examined to trace their success as a public space according to the SDG. Qualitative methods were used to investigate field observations and conduct personal interviews with daily visitors of the parks (selected randomly with small control over demographics of gender and age). The aim of this paper is to find out the extent that these parks are successful public spaces according to sustainable development standards. According to the analysis, considering the high percentage of positive answers in each part of the study, both cases are considered as successful sustainable public spaces. However, in most components of the study, Qeytariyeh scored marginally higher than Niyavaran. The primary concerns in each study were the ability of women to engage in physical activities and the low employment rates due to parks and surrounding businesses. These concerns should be considered for park design, maintenance, and future improvements. In conclusion, we have proposed solutions to strengthen the success of the parks as sustainable public spaces. [ABSTRACT FROM AUTHOR]

Viral infections are a great threat to human health. Currently, there are no effective vaccines and antiviral drugs against the majority of viral diseases, suggesting the need to develop novel and effective antiviral agents. Since the intracellular delivery of antiviral agents, particularly the impermeable molecules, such as peptides, proteins, and nucleic acids, are essential to exert their therapeutic effects, using a delivery system is highly required. Among various delivery systems, cell-penetrating peptides (CPPs), a group of short peptides with the unique ability of crossing cell membrane, offer great potential for the intracellular delivery of various biologically active cargoes. The results of numerous in vitro and in vivo studies with CPP conjugates demonstrate their promise as therapeutic agents in various medical fields including antiviral therapy. The CPP-mediated delivery of various antiviral agents including peptides, proteins, nucleic acids, and nanocarriers have been associated with therapeutic efficacy both in vitro and in vivo. This review describes various aspects of viruses including their biology, pathogenesis, and therapy and briefly discusses the concept of CPP and its potential in drug delivery. Particularly, it will highlight a variety of CPP applications in the management of viral infections. [Display omitted] [ABSTRACT FROM AUTHOR]

Introduction: Drug resistance to existing antimicrobial drugs has become a serious threat to human health, which highlights the need to develop new antimicrobial agents., Method: In this study, a new set of 3-hydroxypyridine-4-one derivatives (6a-j) was synthesized, and the antimicrobial effects of these derivatives were evaluated against a variety of microorganisms using the microdilution method. The antimicrobial evaluation indicated that compound 6c, with an electron-donating group -OCH3 at the meta position of the phenyl ring, was the most active compound against S. aureus and E. coli species with an MIC value of 32 μg/mL. Compound 6c was more potent than ampicillin as a reference drug., Result: The in vitro antifungal results showed that the studied derivatives had moderate effects (MIC = 128-512 μg/mL) against C. albicans and A. niger species. The molecular modeling studies revealed the possible mechanism and suitable interactions of these derivatives with the target protein., Conclusion: The obtained biological results offer valuable insights into the design of more effective antimicrobial agents., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: Azoles are the famous and widespread scaffold in the pharmaceutical industry due to their wide range of activities, high efficacy, good tolerability, and oral availability. Furthermore, azole derivatives have attracted attention as potent antimicrobial agents., Introduction: The purpose of this review is to provide an overview of pharmacological aspects of the main scaffolds of azoles, including imidazole, benzimidazole, triazole, and tetrazole, which possess antimicrobial activity, reported from 2016 to 2020, as well as all of our publication in this field. In addition, we discuss the relationship between structure and activity and molecular docking studies of the azole derivatives to provide critical features and valuable information for the synthesis of novel azole compounds with desirable biological activities. The presented structures in this review have been tested against several bacteria and fungi, such as E. coli and C. albicans, which have been common in all of these studies., Results: A comparison of the reported MIC for tested compounds showed fluconazole base structures as the most active antifungal agents, and triazole derivatives bearing nitrophenyl and coumarin moieties to have the most dominant antibacterial activity., Conclusion: Triazole and imidazole scaffolds are more important for designing antimicrobial compounds than other azole derivatives, like benzimidazole or tetrazole. All the most active compounds were observed to fulfill the Lipinski rule., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)