Publications by authors named "N S De"

Peripheral ameloblastoma is a rare, benign, slow-growing odontogenic neoplasm prevalent in the mandible. It originates from the odontogenic epithelium and its remnants, and its histological characteristics are identical to those of intraosseous ameloblastoma. It is less aggressive and invasive than its intraosseous variety, with a low recurrence rate.

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Article Synopsis
  • Drug resistance is making existing antimalarials ineffective, highlighting the urgent need for new treatments.
  • Researchers identified a promising new chemotype, cyclopropyl carboxamide, through screening a library of compounds, leading to the development of a strong candidate, WJM280, which is effective against malaria without harming human cells.
  • Further studies revealed that resistant parasites have mutations in the cytochrome b gene, confirming it as the drug target, but improving the compound's stability and effectiveness in mouse models still needs to be addressed.
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Fascioliasis, only foodborne trematodiasis of worldwide distribution, is caused by and , liver flukes transmitted by freshwater snails. Southern and southeastern Asia is an emerging hot spot of , despite its hitherto less involvement in human infection. In Vietnam, increasing cases have been reported since 1995, whereas only sixteen throughout 1800-1994.

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The emergence of resistance against current antimalarial treatments has necessitated the need for the development of novel antimalarial chemotypes. Toward this goal, we recently optimised the antimalarial activity of the dihydroquinazolinone scaffold and showed it targeted PfATP4. Here, we deconstruct the lactam moiety of the tricyclic dihydroquinazolinone scaffold and investigate the structure-activity relationship of the truncated scaffold.

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To contribute to the global effort to develop new antimalarial therapies, we previously disclosed initial findings on the optimization of the dihydroquinazolinone-3-carboxamide class that targets PfATP4. Here we report on refining the aqueous solubility and metabolic stability to improve the pharmacokinetic profile and consequently in vivo efficacy. We show that the incorporation of heterocycle systems in the 8-position of the scaffold was found to provide the greatest attainable balance between parasite activity, aqueous solubility, and metabolic stability.

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