Synthesis, antimicrobial activity and toxicity to nematodes of cyclam derivatives.
The antimicrobial activity and toxicity to nematodes of the cyclam salt [H2{H2(4-CF3PhCH2)2Cyclam}](CH3COO)2⋅(CH3COOH)2were evaluated. Estimated minimum inhibitory concentrations (MICs) of 9, 261 and 15 µg/mL were obtained for Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus, respectively. For selected Candida spp., the estimated MICs obtained ranged from 32 µg/mL to 63 µg/mL. Bactericidal activity was demonstrated but the compound was not reliably fungicidal. Concentrations of the cyclam salt up to 32 µg/mL did not significantly affect survival of the nematode Caenorhabditis elegans; however, concentrations equal or above this value significantly affected nematode survival in a dose-dependent manner.
Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisbon, Portugal.
Luis G
LG
Alves
Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisbon, Portugal.
Pedro F
PF
Pinheiro
iBB-Instituto de Bioengenharia e Biociências, Departamento de Bioengenharia, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, Torre Sul, Piso 6, 1049-001 Lisbon, Portugal.
Joana R
JR
Feliciano
Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisbon, Portugal; iBB-Instituto de Bioengenharia e Biociências, Departamento de Bioengenharia, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, Torre Sul, Piso 6, 1049-001 Lisbon, Portugal.
Diana P
DP
Dâmaso
iBB-Instituto de Bioengenharia e Biociências, Departamento de Bioengenharia, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, Torre Sul, Piso 6, 1049-001 Lisbon, Portugal. Electronic address: jorgeleitao@tecnico.ulisboa.pt.
Jorge H
JH
Leitão
Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisbon, Portugal. Electronic address: ana.martins@tecnico.ulisboa.pt.
Ana M
AM
Martins
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000935:Antifungal Agents / Q000494:pharmacology; D000969:Antinematodal Agents / Q000494:pharmacology*; D017173:Caenorhabditis elegans / Q000187:drug effects*; D002175:Candida / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D021261:Parasitic Sensitivity Tests; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000969:Antinematodal Agents; D006571:Heterocyclic Compounds; C024560:cyclam
Antimicrobial activity; Cyclam salts; Nematode; Tetraazamacrocycles; Toxicity