Errini Decruse Dhar, A. Yadav, Grace Basumatary
Jul 26, 2021
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Quality indicators
Journal
Parasitology international
Abstract
The control of pinworms mainly relies on use of anthelmintic drugs. At present, there exists only few medications against pinworms, and their repeated use pose a serious risk of resistance development. Therefore, new anti-pinworm drugs are required to overcome the risk of resistance. This study reports the anti-pinworm activity of three novel coumarin-based trisubstituted methanes (TRSMs), i.e., 6-Amino-5-((4-hydroxy-2-oxo-2H-chromen-3-yl)(4-fluoro-phenyl)methyl)-1,3-dimethyl-pyrimidine-2,4(1H,3H)-dione (1), 6-Amino-5-((4-hydroxy-2-oxo-2H-chromen-3-yl)(4-chlor-ophenyl)methyl)-1,3-dimethyl-pyrimidine-2,4(1H,3H)-dione (2) and 6-Amino-5-((4-hydroxy-2-oxo-2H-chromen-3-yl)(4-bromophenyl)methyl)-1,3-dimethyl-pyrimidine-2,4(1H,3H)-dione (3) in Syphacia obvelata-infected mice. The oral acute toxicity of compounds was examined using the OECD guidelines. The findings of this study reveal that TRSM analogues 1 and 2, at a single 80 mg/kg dose given for 5 days, can reduce about 90% of pinworm worm burden in mice, compared to 98% worm reduction shown by 20 mg/kg dose of albendazole, the reference drug, on the 12 day of infection. In particular, the fluoro-and bromo-substituents in the phenyl ring of synthesized derivatives greatly influence the efficacy of candidates. The oral acute toxicity of TRSMs was observed to be greater than 2000 mg/kg body weight for mice. Taken together, our study suggests that studied novel coumarin-based trisubstituted methanes could serve as suitable candidates for the development of new anti-pinworm drugs.