Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00034
Abstract: A novel diazaspiro[3.4]octane series was identified from a Plasmodium falciparum whole-cell high-throughput screening campaign. Hits displayed activity against multiple stages of the parasite lifecycle, which together with a novel sp3-rich scaffold provided an attractive starting… read more here.
Keywords: diazaspiro octane; chemistry; plasmodium falciparum; multiple stages ... See more keywords
A Two-Step Kinugasa/Conia-Ene-Type Sequential Reaction for Asymmetric Synthesis of 8-Methylene -2,6-diazaspiro [3.4]octane-1,5-diones
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DOI: 10.1039/d4qo01388c
Abstract: 2,6-Diazaspiro[3.4]octane-1,3-dione, integrating -lactam and -lactam into one structure, is an important skeleton found in many bioactive molecules. This article describes a simple and practical synthesis of 8-methylene-2,6-diazaspiro[3.4]octane-1,5-diones from N-(prop-2-yn-1-yl)propiolamides... read more here.
Keywords: diazaspiro; synthesis methylene; methylene diazaspiro; octane diones ... See more keywords
Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead
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DOI: 10.3390/molecules28062529
Abstract: A small set of twelve compounds of a nitrofuran carboxamide chemotype was elaborated from a readily available 2,6-diazaspiro[3.4]octane building block, exploring diverse variants of the molecular periphery, including various azole substituents. The in vitro inhibitory… read more here.
Keywords: exploration around; diazaspiro octane; antitubercular lead; periphery exploration ... See more keywords