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Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Jun 01; Vol. 41, pp. 127978. Date of Electronic Publication: 2021 Mar 22. - Publication Year :
- 2021
-
Abstract
- A series of novel thiazole-containing amides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent and selective PfFPPS/GGPPS inhibitors with good in vitro ADME profiles. The most promising candidate molecules were progressed to mouse in vivo PK studies and demonstrated adequate free drug exposure to warrant further investigation.<br /> (Copyright © 2021 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antimalarials chemical synthesis
Antimalarials chemistry
Diphosphonates chemical synthesis
Diphosphonates chemistry
Dose-Response Relationship, Drug
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Farnesyltranstransferase metabolism
Geranyltranstransferase metabolism
Molecular Structure
Parasitic Sensitivity Tests
Plasmodium falciparum enzymology
Structure-Activity Relationship
Antimalarials pharmacology
Diphosphonates pharmacology
Enzyme Inhibitors pharmacology
Farnesyltranstransferase antagonists & inhibitors
Geranyltranstransferase antagonists & inhibitors
Plasmodium falciparum drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 41
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 33766764
- Full Text :
- https://doi.org/10.1016/j.bmcl.2021.127978