scholarly journals Synthesis and Structure–Activity Relationships of Phosphonic Arginine Mimetics as Inhibitors of the M1 and M17 Aminopeptidases from Plasmodium falciparum

2013 ◽  
Vol 56 (12) ◽  
pp. 5213-5217 ◽  
Author(s):  
Komagal Kannan Sivaraman ◽  
Alessandro Paiardini ◽  
Marcin Sieńczyk ◽  
Chiara Ruggeri ◽  
Christine A. Oellig ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Arginine Mimetics

scholarly journals Structure-Activity Relationships for Inhibition of Cysteine Protease Activity and Development of Plasmodium falciparum by Peptidyl Vinyl Sulfones

2003 ◽  
Vol 47 (1) ◽  
pp. 154-160 ◽  
Author(s):  
Bhaskar R. Shenai ◽  
Belinda J. Lee ◽  
Alejandro Alvarez-Hernandez ◽  
Pek Y. Chong ◽  
Cory D. Emal ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Cysteine Protease ◽  
Cysteine Proteases ◽  
Parasite Development ◽  
Vinyl Sulfone ◽  
Cysteine Protease Inhibitors ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Sulfonate Ester

ABSTRACT The Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3 appear to be required for hemoglobin hydrolysis by intraerythrocytic malaria parasites. Previous studies showed that peptidyl vinyl sulfone inhibitors of falcipain-2 blocked the development of P. falciparum in culture and exerted antimalarial effects in vivo. We now report the structure-activity relationships for inhibition of falcipain-2, falcipain-3, and parasite development by 39 new vinyl sulfone, vinyl sulfonate ester, and vinyl sulfonamide cysteine protease inhibitors. Levels of inhibition of falcipain-2 and falcipain-3 were generally similar, and many potent compounds were identified. Optimal antimalarial compounds, which inhibited P. falciparum development at low nanomolar concentrations, were phenyl vinyl sulfones, vinyl sulfonate esters, and vinyl sulfonamides with P2 leucine moieties. Our results identify independent structural correlates of falcipain inhibition and antiparasitic activity and suggest that peptidyl vinyl sulfones have promise as antimalarial agents.

Antiplasmodial Bis-Indole Alkaloids from the Bark of Flindersia pimenteliana

Planta Medica ◽  
2019 ◽  
Vol 86 (01) ◽  
pp. 19-25 ◽  
Author(s):  
Luke P. Robertson ◽  
Leonardo Lucantoni ◽  
Vicky M. Avery ◽  
Anthony R. Carroll
Keyword(s):  
Plasmodium Falciparum ◽  
Spectroscopic Data ◽  
Indole Alkaloids ◽  
2D Nmr ◽  
Antiplasmodial Activity ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Ic50 Values ◽  
Significant Attention

AbstractThree new (1–3) and 2 known (4–5) bis-indole alkaloids were identified from the bark of Flindersia pimenteliana (Rutaceae). The structures of 1–3 were elucidated on the basis of their (+)-HRESESIMS and 2D NMR spectroscopic data. Antiplasmodial activity for 1–3 against chloroquine sensitive (3D7) and chloroquine-resistant (Dd2) Plasmodium falciparum is also reported, with IC50 values ranging from 0.96 to 2.41 µg/mL. These results expand our knowledge of the structure-activity relationships of potently antiplasmodial isoborreverine-type alkaloids, the bioactivity of which have recently attracted significant attention in the literature.

scholarly journals Synthesis, characterization, and anti-plasmodial activity of 2,6-substituted benzothiazole derivatives

2016 ◽  
Vol 11 (2) ◽  
pp. 321 ◽  
Author(s):  
Gnanavel Sadhasivam ◽  
Kannan Kulanthai ◽  
Sowmiya Rajamani ◽  
Pachiappan Perumal
Keyword(s):  
Plasmodium Falciparum ◽  
Giemsa Stain ◽  
Structure Activity Relationships ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Structure Activity ◽  
Ft Ir ◽  
C Nmr

<p class="Abstract">Six compounds of benzothiazole derivatives were synthesized, and structures were confirmed by FT-IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR and LC-MS. The resulting compounds were evaluated for anti-plasmodial activity against <em>Plasmodium falciparum</em> by Giemsa stain. Among them the compounds 3b and 4 showed potent anti-plasmodial activity against <em>P. falciparum</em>. The com-pounds 3a, 5a, 5b also showed moderate anti-plasmodial activity. The structure-activity relationships of benzothiazole derivatives also discussed which were useful for exploring and developing benzothiazole derivatives as novel anti-malarial drugs.</p><p> </p>

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