Academic Journal
2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties
| العنوان: | 2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties |
|---|---|
| المؤلفون: | Charoensutthivarakul, Sitthivut, David Hong, W., Leung, Suet C., Gibbons, Peter D., Bedingfield, Paul, Nixon, Gemma L., Lawrenson, Alexandre S., Berry, Neil G., Ward, Steve, Biagini, Giancarlo, O'Neill, Paul |
| المصدر: | MedChemComm, Vol 6, Issue 7, pp. 1252-1259. |
| بيانات النشر: | Royal Society of Chemistry |
| سنة النشر: | 2015 |
| المجموعة: | LSTM Online Archive (Liverpool School of Tropical Medicine) |
| مصطلحات موضوعية: | QV 256 Antimalarials, QW 52 Physiology and chemistry of microorganisms. Metabolism, QX 135 Plasmodia, WC 750 Malaria |
| الوصف: | A series of 2-pyridylquinolones has been prepared in 5–7 steps and through lead optimisation, antimalarial activity as low as 12 nM against Plasmodium falciparum (Pf) has been achieved. Compared with previous analogues in this series, selected molecules have improved solubility, a reduced potential for off-target toxicity and improved metabolic stability profiles. Docking studies performed with a homology model of the Pfbc1 complex target demonstrate a key role for the Tyr16 residues in the recognition of highly active quinolone based inhibitors |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | text |
| اللغة: | English |
| Relation: | https://archive.lstmed.ac.uk/7845/1/MedChemComm_2-Pyridylquinolone%20Antimalarials.pdf; Charoensutthivarakul, Sitthivut, David Hong, W., Leung, Suet C., Gibbons, Peter D., Bedingfield, Paul, Nixon, Gemma L., Lawrenson, Alexandre S., Berry, Neil G., Ward, Steve orcid:0000-0003-2331-3192 , Biagini, Giancarlo orcid:0000-0001-6356-6595 and O'Neill, Paul (2015) '2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties'. MedChemComm, Vol 6, Issue 7, pp. 1252-1259. |
| الاتاحة: | https://archive.lstmed.ac.uk/7845/ http://pubs.rsc.org/en/Journals/JournalIssues/MD#!recentarticles&adv https://archive.lstmed.ac.uk/7845/1/MedChemComm_2-Pyridylquinolone%20Antimalarials.pdf |
| Rights: | cc_by_4 |
| رقم الانضمام: | edsbas.E8778E02 |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |