2022
DOI: 10.3390/biom12121903
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Novel Selective and Low-Toxic Inhibitor of LmCPB2.8ΔCTE (CPB) One Important Cysteine Protease for Leishmania Virulence

Abstract: Leishmaniasis is a highly prevalent, yet neglected disease caused by protozoan parasites of the genus Leishmania. In the search for newer, safer, and more effective antileishmanial compounds, we herein present a study of the mode of action in addition to a detailed structural and biological characterization of LQOF-G6 [N-benzoyl-N′-benzyl-N″-(4-tertbutylphenyl)guanidine]. X-ray crystallography and extensive NMR experiments revealed that LQOF-G6 nearly exclusively adopts the Z conformation stabilized by an intr… Show more

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Cited by 10 publications
(22 citation statements)
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“…They have demonstrated a range of biological activities, such as antiinflammatory, 29 antibacterial, antifungal, 30 and antiprotozoal. 13,28,31 They have also been studied in the context of diabetes. 32 Their antiparasitic activity, specifically leishmanicidal, 28 has also been reported.…”
Section: ■ Introductionmentioning
confidence: 99%
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“…They have demonstrated a range of biological activities, such as antiinflammatory, 29 antibacterial, antifungal, 30 and antiprotozoal. 13,28,31 They have also been studied in the context of diabetes. 32 Their antiparasitic activity, specifically leishmanicidal, 28 has also been reported.…”
Section: ■ Introductionmentioning
confidence: 99%
“…33 Furthermore, the guanidine derivative (Z)-N-benzoyl-N′-benzyl-N″-(4-tertbutylphenyl)guanidine (LQOF-G6) targets the Leishmania cysteine protease. 13 Guanidine LQOF-G6 reduced the parasite load in mice infected with L. amazonensis and exhibited low toxicity in organs and cells, 13 indicating its potential as a future therapeutic agent.…”
Section: ■ Introductionmentioning
confidence: 99%
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