Structure–activity relationship studies of new rifamycins containing l -amino acid esters as inhibitors of bacterial RNA polymerases

2016 ◽  
Vol 116 ◽  
pp. 216-221 ◽  
Author(s):  
Dominika Czerwonka ◽  
Joanna Domagalska ◽  
Krystian Pyta ◽  
Marcelina M. Kubicka ◽  
Paulina Pecyna ◽  
...  
Keyword(s):  
Amino Acid ◽  
Structure Activity Relationship ◽  
Rna Polymerases ◽  
Activity Relationship ◽  
Amino Acid Esters ◽  
Structure Activity ◽  
Bacterial Rna ◽  
Acid Esters

scholarly journals Synthesis and leishmanicidal activity of cinnamic acid esters: structure–activity relationship

2013 ◽  
Vol 23 (3) ◽  
pp. 1378-1386 ◽  
Author(s):  
Elver Otero ◽  
Sara M. Robledo ◽  
Santiago Díaz ◽  
Miguel Carda ◽  
Diana Muñoz ◽  
...  
Keyword(s):  
Cinnamic Acid ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Leishmanicidal Activity ◽  
Structure Activity ◽  
Acid Esters

The anti-leishmanial activity of dipeptide esters on Leishmania amazonensis amastigotes

Parasitology ◽  
1990 ◽  
Vol 100 (2) ◽  
pp. 201-207 ◽  
Author(s):  
C. Ramazeilles ◽  
L. Juliano ◽  
J. R. Chagas ◽  
M. Rabinovitch
Keyword(s):  
Amino Acid ◽  
Methyl Esters ◽  
Leishmania Amazonensis ◽  
Amino Acid Esters ◽  
Cysteine Proteinases ◽  
Hydrophobic Amino Acid ◽  
Structure Activity ◽  
Reduction Assay ◽  
Mtt Reduction ◽  
Acid Esters

SUMMARYL-Amino acid esters, such as L-Leu-OMe, kill Leishmania amazonensis amastigotes by a mechanism which appears to involve ester hydrolysis by cysteine proteinases located in the parasite megasomes. We have examined the killing of isolated amastigotes by L-dipeptide esters and derived some structure-activity correlations. Toxicity of the compounds for the parasites was measured by a tetrazolium (MTT) reduction assay. The results show that active dipeptide esters contained at least I hydrophobic amino acid (Leu, Ile, Val, Phe or Trp). The activity of homodipeptide methyl esters depended on the nature of the amino acid, as indicated by the following series: Phe-Phe-OMe < Val-Val-OMe < Leu-Leu-OMe < Trp-Trp-OMe < Ile-Ile-OMe. The nature of the amino acids in Leu-X-OMe and X-Leu-OMe was relatively unimportant when X was Phe, Trp or Val. However, when X was Ala or Gly, Leu-X-OMe was several-fold more active than X-Leu-OMe.

Nematicidal Efficacy of Substituted Phenols, Phenoxyacetic Acid Esters and Hydrazides: a Structure-Activity Relationship Study

Nematologica ◽  
1989 ◽  
Vol 35 (3) ◽  
pp. 366-370 ◽  
Author(s):  
Mangel S. Malik ◽  
Kuldip Singh Dhindsa ◽  
Vijay Pal ◽  
K.K. Verma ◽  
Naresh K. Sangwan ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Phenoxyacetic Acid ◽  
Substituted Phenols ◽  
Structure Activity ◽  
Relationship Study ◽  
Acid Esters
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