B. Bindu, A. Manikandan, S. Jeevitha, Joe Jacob Kunju, S. Vijayalakshmi
{"title":"Imidazolidine-Based Aspartate Inhibitors for Candida Infections","authors":"B. Bindu, A. Manikandan, S. Jeevitha, Joe Jacob Kunju, S. Vijayalakshmi","doi":"10.1002/ddr.70074","DOIUrl":null,"url":null,"abstract":"<div>\n \n <p>The fungal infection gradually poses a life threat to mankind, candidiasis caused by Candida sp. is one among them. We describe the aspartate protease inhibition potentials of 12 sulfonyl-containing imidazolidines (<b>5a-l</b>) anti-candidal agents. <i>Candida Albicans</i> secretes aspartic proteases (Saps), one of its most important virulent agents. These hydrolytic enzymes are critical for both fungal physiological processes and host-fungus interactions. Compounds <b>5a-l</b> were examined for their fungal aspartate protease inhibition apart from their anti-candida activity. These findings were equipped and validated in silico using molecular docking and in vitro enzyme inhibition assays. The study found that imidazolidine derivatives inhibited aspartic protease and exhibited anti-candida action. Conclusively, imidazolidines <b>5g, 5h,</b> and <b>5j</b> were perceived as the most potent anti-candida compounds and are presently being evaluated for their preclinical studies.</p>\n </div>","PeriodicalId":11291,"journal":{"name":"Drug Development Research","volume":"86 2","pages":""},"PeriodicalIF":3.5000,"publicationDate":"2025-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Development Research","FirstCategoryId":"3","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/ddr.70074","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
The fungal infection gradually poses a life threat to mankind, candidiasis caused by Candida sp. is one among them. We describe the aspartate protease inhibition potentials of 12 sulfonyl-containing imidazolidines (5a-l) anti-candidal agents. Candida Albicans secretes aspartic proteases (Saps), one of its most important virulent agents. These hydrolytic enzymes are critical for both fungal physiological processes and host-fungus interactions. Compounds 5a-l were examined for their fungal aspartate protease inhibition apart from their anti-candida activity. These findings were equipped and validated in silico using molecular docking and in vitro enzyme inhibition assays. The study found that imidazolidine derivatives inhibited aspartic protease and exhibited anti-candida action. Conclusively, imidazolidines 5g, 5h, and 5j were perceived as the most potent anti-candida compounds and are presently being evaluated for their preclinical studies.
期刊介绍:
Drug Development Research focuses on research topics related to the discovery and development of new therapeutic entities. The journal publishes original research articles on medicinal chemistry, pharmacology, biotechnology and biopharmaceuticals, toxicology, and drug delivery, formulation, and pharmacokinetics. The journal welcomes manuscripts on new compounds and technologies in all areas focused on human therapeutics, as well as global management, health care policy, and regulatory issues involving the drug discovery and development process. In addition to full-length articles, Drug Development Research publishes Brief Reports on important and timely new research findings, as well as in-depth review articles. The journal also features periodic special thematic issues devoted to specific compound classes, new technologies, and broad aspects of drug discovery and development.