NDLI: Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies.

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Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies.

Content Provider	Semantic Scholar
Author	Gemma, Sandra Campiani, Giuseppe Butini, Stefania Kukreja, Gagan Coccone, Salvatore Sanna Joshi, Bhupendra Persico, Marco Nacci, Vito A. Fiorini, Isabella Novellino, Ettore Fattorusso, Ernesto Taglialatela-Scafati, Orazio Savini, Luisa Taramelli, Donatella Basilico, Nicoletta Parapini, Silvia Morace, Giulia Yardley, Vanessa Croft, Simon Coletta, Massimiliano Marini, Stefano Fattorusso, Caterina
Copyright Year	2008
Abstract	We describe herein the design, synthesis, biological evaluation, and structure-activity relationship (SAR) studies of an innovative class of antimalarial agents based on a polyaromatic pharmacophore structurally related to clotrimazole and easy to synthesize by low-cost synthetic procedures. SAR studies delineated a number of structural features able to modulate the in vitro and in vivo antimalarial activity. A selected set of antimalarials was further biologically investigated and displayed low in vitro toxicity on a panel of human and murine cell lines. In vitro, the novel compounds proved to be selective for free heme, as demonstrated in the beta-hematin inhibitory activity assay, and did not show inhibitory activity against 14-alpha-lanosterol demethylase (a fungal P450 cytochrome). Compounds 2, 4e, and 4n exhibited in vivo activity against P. chabaudi after oral administration and thus represent promising antimalarial agents for further preclinical development.
File Format	PDF HTM / HTML
DOI	10.1021/jm701247k
PubMed reference number	18278860
Journal	Medline
Volume Number	51
Issue Number	5
Alternate Webpage(s)	https://art.torvergata.it/retrieve/handle/2108/41187/117238/JMedChem2008AMalariaCampiani.pdf
Alternate Webpage(s)	https://doi.org/10.1021/jm701247k
Journal	Journal of medicinal chemistry
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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