دورية أكاديمية
Antitrypanosomal Chloronitrobenzamides.
| العنوان: | Antitrypanosomal Chloronitrobenzamides. |
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| المؤلفون: | Carrillo AK; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States., Kadayat TM; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536-0509, United States., Hwang JY; Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Daejeon, KR 34114, United States., Chen Y; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536-0509, United States., Zhu F; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States., Holbrook G; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States., Gillingwater K; Department of Medical Parasitology & Infection Biology, Swiss Tropical and Public Health Institute, Kreuzstrasse 2, Allschwil 4123, Switzerland., Connelly MC; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States., Yang L; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States., Kaiser M; Department of Medical Parasitology & Infection Biology, Swiss Tropical and Public Health Institute, Kreuzstrasse 2, Allschwil 4123, Switzerland.; Faculty of Science, University of Basel, Petersplatz 1, Basel 4003, Switzerland., Guy RK; Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536-0509, United States. |
| المصدر: | Journal of medicinal chemistry [J Med Chem] 2024 Mar 14; Vol. 67 (5), pp. 3437-3447. Date of Electronic Publication: 2024 Feb 16. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Washington Dc : American Chemical Society Original Publication: [Easton, Pa.] : American Chemical Society, [c1963- |
| مواضيع طبية MeSH: | Trypanosomiasis, African*/drug therapy , Trypanosoma brucei brucei* , Trypanocidal Agents*/toxicity , Trypanocidal Agents*/therapeutic use, Humans ; Animals ; Mice ; Trypanosoma brucei rhodesiense ; Trypanosoma brucei gambiense |
| مستخلص: | Human African trypanosomiasis (HAT), a neglected tropical disease caused by Trypanosoma brucei gambiense ( Tbg ) or Trypanosoma brucei rhodesiense ( Tbr ), remains a significant public health concern with over 55 million people at risk of infection. Current treatments for HAT face the challenges of poor efficacy, drug resistance, and toxicity. This study presents the synthesis and evaluation of chloronitrobenzamides (CNBs) against Trypanosoma species , identifying previously reported compound 52 as a potent and selective orally bioavailable antitrypanosomal agent. 52 was well tolerated in vivo and demonstrated favorable oral pharmacokinetics, maintaining plasma concentrations surpassing the cellular EC |
| المشرفين على المادة: | 0 (Trypanocidal Agents) |
| تواريخ الأحداث: | Date Created: 20240216 Date Completed: 20240315 Latest Revision: 20240315 |
| رمز التحديث: | 20240315 |
| DOI: | 10.1021/acs.jmedchem.3c01680 |
| PMID: | 38363074 |
| قاعدة البيانات: | MEDLINE |
Find this issue from the American Chemical Society | تدمد: | 1520-4804 |
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| DOI: | 10.1021/acs.jmedchem.3c01680 |