1424360-89-3

Upstream product

• 1424360-80-4 (E)-[4-(1-benzyl-3-methylcarbamoylallylcarbamoyl)-4-tert-butoxycarbonylaminobutylamino]acetic acid benzyl ester 
• 1424360-77-9 (E)-4-(5-(((benzyloxy)carbonyl)amino)-2-((tert-butoxycarbonyl)amino)pentanamido)-5-phenylpent-2-enoic acid 
• 1424360-76-8 (E)-ethyl 4-(5-(((benzyloxy)carbonyl)amino)-2-((tert-butoxycarbonyl)amino)pentanamido)-5-phenylpent-2-enoate 
• 244033-75-8 (S)-(+)-trans-5-phenyl-4-amino-2-pentenoic acid ethyl ester 
• 124818-94-6 ethyl (2E,4S)-4-[(tert-butoxycarbonyl)amino]-5-phenylpent-2-enoate 
• 1424360-96-2 (E)-benzyl (4-amino-5-((5-(methylamino)-5-oxo-1-phenylpent-3-en-2-yl)amino)-5-oxopentyl)carbamate 
• 100-52-7 benzaldehyde 

Relevant academic research and scientific papers

Composition comprising an ALLN derivative as an active ingredient for preventing and treating malaria infection

The present invention relates to an anti-malarial composition containing an ALLN (N-acetyl-L-Leucyl-Lleucyl-L-norleucinal) derivative compound as an active ingredient, wherein a compound of the present invention can be used as a pharmaceutical composition for preventing and treating a malaria infection containing the ALLN derivative compound as an active ingredient.

Anti-malarial activity of new N-acetyl-l-leucyl-l-leucyl-l-norleucinal (ALLN) derivatives against Plasmodium falciparum

Malaria is the most common of the parasitic diseases in tropical and subtropical regions. Adverse side effects of anti-malarial drugs have precluded them as a potential clinical drug. In this study, novel derivatives of N-acetyl-l-leucyl-l-leucyl-l-norleucinal (ALLN) based on a variety of dipeptidyl α,β-unsaturated amides containing lysine as a part were synthesized and evaluated. Lower toxicity was achieved by reducing or eliminating the tendency of forming chemically reactive and toxic intermediates and metabolites. The synthesized compounds were evaluated for anti-malarial efficacy against Plasmodium falciparum and cytotoxicity in human epitheloid carcinoma cervix (HeLa cells) by estimating the therapeutic index (TI). N-Methyl amide with N′-Boc protection among them exhibited strong anti-malarial activity and N-methyl amide with N′-m-methylbenzyl amide showed excellent anti-malarial activity with much lower toxicity than the ALLN. Therefore, the two chemicals, as well as the underlying design rationale, could be useful in the discovery and development of new anti-malarial drugs.