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Synthesis, pharmacological evaluation and docking studies of new sulindac analogues.
Romeiro, Nelilma C; Leite, Ramon D F; Lima, Lidia M; Cardozo, Suzana V S; de Miranda, Ana L P; Fraga, Carlos A M; Barreiro, Eliezer J.
Afiliación
  • Romeiro NC; Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio), Faculdade de Farmácia, Universidade Federal do Rio de Janeiro (UFRJ), Rio de Janeiro, PO Box 68023, RJ 21944-970, Brazil.
Eur J Med Chem ; 44(5): 1959-71, 2009 May.
Article en En | MEDLINE | ID: mdl-19144452
ABSTRACT
This paper describes the synthesis, pharmacological evaluation and docking studies of a series of new sulindac analogues. Overall, the designed compounds revealed good, in vivo, antinociceptive activity and satisfactory anti-inflammatory profile. Flexible molecular docking with COX-1/COX-2 has shown putative binding modes of the designed compounds while the theoretical evaluation of cell permeability based on Lipinski's rule of five has helped rationalize the biological results.
Asunto(s)

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Sulindac / Antiinflamatorios no Esteroideos Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2009 Tipo del documento: Article País de afiliación: Brasil

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Sulindac / Antiinflamatorios no Esteroideos Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2009 Tipo del documento: Article País de afiliación: Brasil