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New imidazolidinic bioisosters: potential candidates for antischistosomal drugs
Pitta, Maira G. R; Silva, Andréa C. A; Al Neves, Juliana Kelle; Silva, Poliana G; Irmão, João I; Malagueño, Elizabeth; Santana, José V; Lima, Maria C. A; Galdino, Suely L; Pitta, Ivan R; Albuquerque, Mônica C. P. A.
Afiliação
  • Pitta, Maira G. R; Universidade Federal de Pernambuco. Departamento de Antibióticos. Recife. BR
  • Silva, Andréa C. A; Universidade Federal de Pernambuco. Departamento de Antibióticos. Recife. BR
  • Al Neves, Juliana Kelle; Universidade Federal de Pernambuco. Departamento de Antibióticos. Recife. BR
  • Silva, Poliana G; Universidade Federal de Pernambuco. Departamento de Antibióticos. Recife. BR
  • Irmão, João I; Universidade Federal de Pernambuco. Departamento de Medicina Tropical. Recife. BR
  • Malagueño, Elizabeth; Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife. BR
  • Santana, José V; Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife. BR
  • Lima, Maria C. A; Universidade Federal de Pernambuco. Departamento de Antibióticos. Recife. BR
  • Galdino, Suely L; Universidade Federal de Pernambuco. Departamento de Antibióticos. Recife. BR
  • Pitta, Ivan R; Universidade Federal de Pernambuco. Departamento de Antibióticos. Recife. BR
  • Albuquerque, Mônica C. P. A; Universidade Federal de Pernambuco. Departamento de Medicina Tropical. Recife. BR
Mem. Inst. Oswaldo Cruz ; 101(supl.1): 313-316, Oct. 2006. tab, graf
Article em En | LILACS | ID: lil-441265
Biblioteca responsável: BR1.1
ABSTRACT
The emergence of strains of Schistosoma resistant to praziquantel has drawn attention to the search for new schistosomacide drugs. Imidazolidinic derivatives have performed outstandingly against adult S. mansoni worms when evaluated in vitro. The molecular modification of imidazolidine by way of bioisosteric replacement gives rise to variations in its biological response. This study verifies the potential of substituent groups in the derivatives (Z)3-benzyl-5-(2-fluoro-benzylidene)-imidazolidine-2,4-dione NE4, 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin -2-ona PT5, 3-benzyl-5-(3-fluoro-benzylidene)-1-methyl-2-thioxo-imidazolidin-4-one JT53; 3-benzyl-1-methyl-5-(4-methyl-benzylidene)-2-thioxo-imidazolidin-4-one JT63; 3-benzyl-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo -imidazolidin-4-one JT68; 3-(4-chloro-benzyl)-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo-imidazolidin-4-one JT69; 3-(4-phenyl-benzyl)-1-methyl-5-(4-methoxi-benzylidene)-2-thioxo-imidazolidin-4-one JT72 by determining the viability in vitro of adult S. mansoni worms in the presence of these derivatives. The susceptibility of the worms obtained from mice and kept in culture in the presence of different concentrations was determined by way of schistosomacide kinetic, observed every 24 h over a period of eight days. The results show that the worms were more sensitive to the PT5 derivative at a concentration of 58 æM which killed 100 percent of the worms after 24 h of contact, also giving rise to alterations in the tegument surface of the worms with the formation of bubbles and peeling. These observations suggest a strong electronic contribution of the arylazo grouping in the biological response.
Assuntos
Texto completo: 1 Base de dados: LILACS Assunto principal: Schistosoma mansoni / Esquistossomicidas / Imidazolidinas Limite: Animals Idioma: En Revista: Mem. Inst. Oswaldo Cruz Assunto da revista: MEDICINA TROPICAL / PARASITOLOGIA Ano de publicação: 2006 Tipo de documento: Article País de afiliação: Brasil
Texto completo: 1 Base de dados: LILACS Assunto principal: Schistosoma mansoni / Esquistossomicidas / Imidazolidinas Limite: Animals Idioma: En Revista: Mem. Inst. Oswaldo Cruz Assunto da revista: MEDICINA TROPICAL / PARASITOLOGIA Ano de publicação: 2006 Tipo de documento: Article País de afiliação: Brasil