In-vitro Anti-trypanosomal and Cytotoxicity Evaluation of
                                        3-methyl-3,4-dihydroquinazolin-2(1H)-one Derivatives

Jesumoroti, Omobolanle J.; Beteck, Richard M.; Legoabe, Lesetja J.

doi:10.1055/a-1349-1256

Cited by 1 publication

(1 citation statement)

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“…We have previously reported several compound classes exhibiting antitrypanosomal activity, [ 38 , 39 , 40 ] including quinolone-based compounds. [ 41 , 42 ] Our interest in quinolones is motivated by the tractability of this scaffold, and the fact that it can easily be modified at eight different positions to generate novel compounds with diverse biological and physico-chemical properties.…”

Section: Introductionmentioning

confidence: 99%

Tractable Quinolone Hydrazides Exhibiting Sub‐Micromolar and Broad Spectrum Antitrypanosomal Activities

Chirwa,

Francisco,

Dube

et al. 2024

ChemMedChem

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Nagana and Human African Trypanosomiasis (HAT), caused by (sub)species of Trypanosoma, are diseases that impede human and animal health, and economic growth in Africa. The few drugs available have drawbacks including suboptimal efficacy, adverse effects, drug resistance, and difficult routes of administration. New drugs are needed. A series of 20 novel quinolone compounds with affordable synthetic routes was made and evaluated in vitro against Trypanosoma brucei and HEK293 cells. Of the 20 compounds, 12 had sub‐micromolar potencies against the parasite (EC50 values = 0.051‐0.57 µM), and most were non‐toxic to HEK293 cells (CC50 values >5 µM). Two of the most potent compounds presented sub‐micromolar activities against other trypanosome (sub)species (T. cruzi and T. b. rhodesiense). Although aqueous solubility is poor, both compounds possess good logD values (2‐3), and either robust or poor microsomal stability profiles. These varying attributes will be addressed in future reports.

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