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Liposome-Based Delivery of Therapeutic Agents
Published in Emmanuel Opara, Controlled Drug Delivery Systems, 2020
Eneida de Paula, Juliana Damasceno Oliveira, Fernando Freitas de Lima, Lígia Nunes de Morais Ribeiro
The broadest spectrum agents of antifungal therapy worldwide in the last 50 years have been the polyene compounds (e.g. amphotericin, nystatin, hamycin, dermostatin, etc.). Amphotericin B (AMB) is the gold standard antifungal drug, but its use is still associated with severe adverse effects (mainly impairment of nephron function by cumulative doses, besides fever, chills, myalgia, and thrombophlebitis), low clinical response, and high mortality rates. Another class of antifungal, the azoles, include ketoconazole, fluconazole, and itraconazole (launched in the 80s), and later the second-generation triazoles voriconazole, ravuconazole, and posaconazole. Their good activity against molds brought some help to the antifungal therapy, although some of them are mostly used as topical agents. Allylamines, such as butenafine and naftifine, are the third class of antimycotic agents that are able to inhibit squalene epoxidase, restraining the synthesis of ergosterol.143 In the beginning of the 21st century, another class of drugs, the echinocandins–noncompetitive inhibitors of β-1-3-glucan synthase, blocking the synthesis of the fungal cell wall – appeared as a promise for the candidiasis and aspergillosis treatment.144,145
DFT computational insights into structural, electronic and spectroscopic parameters of 2-(2-Hydrazineyl)thiazole derivatives: a concise theoretical and experimental approach
Published in Journal of Sulfur Chemistry, 2021
Vishnu A. Adole, Thansing B. Pawar, Bapu S. Jagdale
The thiazole structure is a vital pharmacophore in the domain of science; in light of its omnipresence in a variety of biological properties [1–5]. The hydrazinylthiazolyl core is one of the significant pharmacological scaffolds which have produced a profound interest in medicinal and industrial researchers. The astounding pharmacological profile of hydrazinylthiazolyl derivatives includes antitubercular, antimalarial, anti-inflammatory, antitumor, antiproliferative, antioxidant, and antimicrobial activity [6–13]. Besides, numerous thiazole hybrids have been identified as potential antibacterial [14–16], anticancer [17,18], anti-inflammatory [19], anti-tubercular [20], antioxidant [21], analgesic [21,22], antidiabetic [23,24], anti-Alzheimer agents [25,26]. The remarkable examples which show diverse biological activities are depicted in Figure 1. For instance, ravuconazole inhibits 14alpha demethylase prompting lysis of the fungal cell wall and responsible for fungal cell death [27,28]. Niridazole is used to cure schistosomiasis (helminthic disease) caused by some flatworms of the genus Schistosoma [29]. Thiamine injections are used to prevent or cure vitamin B1 deficiency [30,31]. Thiabendazole drug is being used for the treatment of infections caused by worms, for example, threadworm [32,33]. Aztreonam is an antibiotic and principally used to treat diseases brought about by gram-negative bacteria, for example, Pseudomonas aeruginosa [34,35]. Ravuconazole is used to treat fungal infections and therefore act as an antimicrobial agent [36,37]. Voreloxin has a double anti-cancer activity that combines DNA intercalation and the suppression of topoisomerase II action [38,39]. Appropriately, it seems, by all accounts, to be exceedingly appealing to study the previously synthesized 2-(2-hydrazinyl) thiazole derivatives [40] of biological intrigue from a computational investigation point of view.