New 2-aminopyrimidine derivatives and their antitrypanosomal and antiplasmodial activities

doi:10.1007/s00706-020-02674-7

Paper

New 2-aminopyrimidine derivatives and their antitrypanosomal and antiplasmodial activities

Published Sep 1, 2020 · Michael Hoffelner, Usama Hassan, W. Seebacher

Monatshefte für Chemie - Chemical Monthly

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Abstract

AbstractNovel 2-aminopyrimidine derivatives were prepared from acyclic starting materials, benzylidene acetones and ammonium thiocyanates, via 5 steps, including ring closure, aromatization, S-methylation, oxidation to methylsulfonyl compounds, and formation of guanidines with suitable amines. The prepared compounds differ from each other by the substitutions of their amino group and of their phenyl ring. The 2-aminopyrimidines were tested by use of microplate assays for their in vitro activities against a causative organism of sleeping sickness, Trypanosoma brucei rhodesiense, as well as against a causative organism of malaria, Plasmodium falciparum NF54. Their cytotoxic properties were determined with L-6 cells (rat skeletal myoblasts). Some of the compounds exhibited quite good antitrypanosomal activity, and others showed excellent antiplasmodial activity. The influence of the structural modifications on these activities is discussed.Graphic abstract

In Vitro Study

Study Snapshot

New 2-aminopyrimidine derivatives show promising antitrypanosomal and antiplasmodial activities, with structural modifications influencing these activities.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

New 2-aminopyrimidine derivatives and their antitrypanosomal and antiplasmodial activities

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References

New derivatives of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities

New 3-azabicyclo[3.2.2]nonanes derivatives show promising antiplasmodial activity against Plasmodium falciparum and Trypanosoma brucei rhodesiense, with potential for in vivo testing against Plasmodium berghei.

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Dihydroartemisinin-piperaquine treatment failure in malaria is high in the eastern Greater Mekong subregion due to increasing drug resistance, requiring urgent accelerated elimination efforts.

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Antimicrobial resistance is emerging in six neglected tropical diseases, highlighting the need for strengthened monitoring and surveillance systems to detect and mitigate its global spread.

Synthesis of 5-enamine-4-thiazolidinone derivatives with trypanocidal and anticancer activity.

Novel 5-enamine-4-thiazolidinone derivatives show both trypanocidal and anticancer activity, with activity type and level depending on the enamine fragment in the C5 position of the thiazolidinone core.

Design, Synthesis, and Structure-Activity Relationship of Tetrahydropyrido[4,3-d]pyrimidine Derivatives as Potent Smoothened Antagonists with in Vivo Activity.

Tetrahydropyrido[4,3-d]pyrimidine derivatives show potential as potent smoothened antagonists for treating medulloblastoma and other Hh pathway related malignancies with improved potency and efficacy compared to vismodegib.

Citations

Pyrrole–Aminopyrimidine Ensembles: Cycloaddition of Guanidine to Acylethynylpyrroles

This study developed an efficient method for synthesis of pharmaceutically promising pyrrole-aminopyrimidine ensembles (up to 91% yield) by cyclocondensation of acylethynylpyrroles with guanidine nitrate in the KOH/DMSO

MOLECULAR DOCKING AND IN-VITRO ANTIMICROBIAL ACTIVTY OF SOME NOVEL AMINOPYRIMIDINE DERIVATIVES

Novel aminopyrimidine derivatives AD3 and AD4 show significant antimicrobial activity against both gram positive and gram negative bacteria.