This work presents the successful synthesis of a library of novel peptidomimetics via Ugi multicomponent reaction. Most of these peptidomimetics contain differently substituted aminocoumarin; 7-amino-4-methylcoumarin and 7-amino-4-(trifluoromethyl) coumarin. Inspired by the biological properties of coumarin derivatives and peptidomimetics, we proposed the synthesis of coumarin incorporated peptidomimetics. We studied the potential of synthesized compounds as antimicrobial drugs on model E. coli bacterial strains (k12 and R2–R4). To highlight the importance of coumarin in antimicrobial resistance, we also synthesized the structurally similar peptidomimetics, using benzylamine. Preliminary cellular studies suggest that the compounds with coumarin derivatives have more potential as antimicrobial agents compared to the compounds without coumarin. We also analyzed the effect of aldehyde, free acid group and ester group on the course of their antimicrobial properties.
An efficient method for the synthesis of functionalized peptidomimetics via multicomponent Ugi reaction has been developed. The application of trifluoroethanol (TFE) as a reaction medium provided desired products with good yields. Further, using the developed cyclisation reaction, the obtained peptidomimetics were transformed into the cyclic analogues (diketopiperazines, DKPs). The goal of the performed studies was to revised and compare whether the structure of the obtained structurally flexible acyclic peptidomimetics and their rigid cycling analogue DKPs affect antimicrobial activity. We studied the potential of synthesized peptidomimetics, both cyclic and acyclic, as antimicrobial drugs on model E. coli bacteria strains (k12, R2–R4). The biological assays reveal that DKPs hold more potential as antimicrobial drugs compared to open chain Ugi peptidomimetics. We believe that it can be due to the rigid cyclic structure of DKPs which promotes the membrane penetration in the cell of studied pathogens. The obtained data clearly indicate the high antibiotic potential of synthesized diketopiperazine derivatives over tested antibiotics.
Prisons have become a world of their own, and women are its new citizens. There have been many studies on incarcerated as a result of the growing numbers of women in prisons, and feminist studies. The on-going reconstruction of literature on this subject has given rise to a new question as to whether we should consider women in prisons, as victims in need of protection, or has this narrative changed? Even with the development of international and municipal legal instruments and agencies for the protection of incarcerated women, there have been various instances where women are victimized in prisons. Both India and Indonesia are part of different international treaties and enacted several laws but lack a systemized prison system to ensure their overall protection. This paper unfolds as follows: The first section delves into the conceptual development of the sexual rights of women in the international sphere, focusing specifically on women in prisons. Subsequently, the second section analyzes in detail various studies, article, and news reports on the subject of sexually abusive treatment of women inmates offering a brief overview of the concerns in India and Indonesia. The methodology adopted for this paper is primarily doctrinal, for the comparative analyses of the rights available to women inmates under various national and international legal instruments.
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