Simple, convenient, and green synthetic protocols have been developed for the one pot synthesis of 2,3-disubstituted quinazolin-4(3H)-ones and 2-styryl-3-substituted quinazolin-4(3H)-ones under catalyst and solvent free conditions.

Human defensins play multiple roles in innate immunity including direct antimicrobial killing and immunomodulatory activity. They have three disulfide bridges which contribute to the stability of three anti-parallel β-strands. The exact role of disulfide bridges and canonical β-structure in the antimicrobial action is not yet fully understood. In this study, we have explored the antimicrobial activity of human β-defensin 4 (HBD4) analogs that differ in the number and connectivity of disulfide bridges. The cysteine framework was similar to the disulfide bridges present in μ-conotoxins, an unrelated class of peptide toxins. All the analogs possessed enhanced antimicrobial potency as compared to native HBD4. Among the analogs, the single disulfide bridged peptide showed maximum potency. However, there were no marked differences in the secondary structure of the analogs. Subtle variations were observed in the localization and membrane interaction of the analogs with bacteria and Candida albicans, suggesting a role for disulfide bridges in modulating their antimicrobial action. All analogs accumulated in the cytosol where they can bind to anionic molecules such as nucleic acids which would affect several cellular processes leading to cell death. Our study strongly suggests that native disulfide bridges or the canonical β-strands in defensins have not evolved for maximal activity but they play important roles in determining their antimicrobial potency.

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Purpose Fruits and vegetables, being good source of energy, health promoting and protecting compounds with unique taste and flavor, are attracting consumers since ages. These horticultural produces start deterioration just after harvest; therefore, their proper storage is must during transportation and storage to retain maximum quality parameters and for good market value. Best storage conditions are required to prevent growth of micro flora and to maintain the nutritional values of harvested produce. Retailers and processors in every corner of world want to move toward the cheaper ways to increase the shelf life and texture of horticultural crops for better consumer preference. The purpose of this paper is to make consumers and researchers aware about different post harvest malpractices in fresh fruits and vegetables. Design/methodology/approach Lot of chemicals like colors, artificial ripening agents, sweeteners and waxes are applied on surface of horticulture produce to siphon off money from consumers, and these have adverse health effects directly or indirectly. Various regulatory agencies have launched various programs, acts and laws for monitoring and avoiding such unhealthy ways. Regulatory bodies launched training programs also for the food handlers and consumers to ensure the food safety from farm to fork. Findings This paper will throw light on different malpractices followed by retailers to manipulate the quality which causes adverse health effects and to create consumer awareness regarding such malpractices. Originality/value The paper emphasizes on current malpractices followed by retailers to mislead the consumers about fruits’ and vegetable’ quality by using sweeteners, colors and other chemical. On prolonged consumption, such substances lead to major health issues such as attention disorder.

According to Hinduism, the main religion of India, the end-of-life (EOL) deals with good and bad death. The WHO definition of palliative care stresses on improving not only the quality of life of patients facing incurable diseases but also their families by providing relief from the pain and suffering that includes the psychosocial and spiritual needs as well. The Indian Society of Palliative Care has been doing a commendable work and appreciable efforts are being done by the Kerala model of delivering the EOL care. The spiritual, ethical issues and ethical challenges raised when the patients are in terminal phase are also reviewed keeping in mind the socio-cultural norms. The Indian Penal Code (IPC) has lacunae, which hamper the physicians from taking proper decision in the EOL care. Some of the sections like IPC 309 are defunct and need to be changed. The Indian Society for Critical Care Medicine has developed a position statement on the patient management of the terminally ill patient in the Intensive Care Unit (ICU) which states that the society should move from the paternalistic model to the share based decision model of the West when deciding the fate of such patients. The literature review on the Indian research on palliative care shows very little emphatic results and the medical under graduates show illiteracy. To strengthen it Medical Council of India has included the palliative care in its curriculum by starting a PG course. Literature review revealed that more research from Indian perspective should be done in this area. This article studies the core issues of developing palliative care in Indian setting keeping in mind the ethical, spiritual and legal issues.

Human β-defensins (HBDs) are cationic antimicrobial peptides constrained by three disulfide bridges. They have diverse range of functions in the innate immune response. It is of interest to investigate whether linear analogs of defensins can be generated, which possess antimicrobial activity. In this study, we have designed linear peptides with potent antimicrobial activity from an inactive peptide spanning the N-terminus of HBD4. Our results show that l-arginine to d-arginine substitution imparts considerable antimicrobial activity against both bacteria and Candida albicans. Increase in hydrophobicity by fatty acylation of the peptides with myristic acid further enhances their potency. In the presence of high concentrations of salt, antimicrobial activity of the myristoylated peptide with l-arginine is attenuated relatively to a lesser extent as compared with the linear active peptide with d-arginine. Substitution of cysteine with the hydrophobic helix-promoting amino acid α-aminoisobutyric acid favors candidacidal activity but not antibacterial activity. The mechanism of killing by d-arginine substituted unacylated analog involves transient interaction with the bacterial membrane followed by translocation into the cytoplasm without membrane permeabilization. Accumulation of peptides in the cytoplasm can affect various cellular processes that lead to cell death. However, the peptide causes membrane permeabilization in case of C. albicans. Myristoylation results in greater interaction of the peptide chain with the microbial cell surface and causes membrane permeabilization. Results described in the study demonstrate that it is possible to generate highly active linear analogs of defensins by selective introduction of d-amino acids and fatty acids, which could be attractive candidates for development as therapeutic agents.

A series of disubstituted 4(3H) quinazolines were designed for potential application in tumors. Firstly, N-benzoyl anthranilic acid is formed, which undergoes cyclization in the presence of pyridine. Subsequently, nucleophilic attack by semicarbazide on the carbonyl carbon gives 2-substituted 3-carbamido 4(3H) quinazolones, which gives final compound with appropriate substitution. The final as well as intermediate products were confirmed by NMR, FT-IR, and mass spectrometry. In vitro toxicity was performed with different cell lines and showed that the connection of hydrophilic styryl to quinazoline moiety increases its efficacy.