Novel pyridopyrimidine derivatives as inhibitors of stable toxin a (STa) induced cGMP synthesis.

Tanifum, Eric A; Kots, Alexander Y; Choi, Byung-Kwon; Murad, Ferid; Gilbertson, Scott R

Tanifum, Eric A; Kots, Alexander Y; Choi, Byung-Kwon; Murad, Ferid; Gilbertson, Scott R.

Afiliación

Tanifum EA; Department of Pharmacology and Toxicology, The University of Texas Medical Branch, Galveston, TX 77555-0650, USA.

Bioorg Med Chem Lett ; 19(11): 3067-71, 2009 Jun 01.

Article en En | MEDLINE | ID: mdl-19409779

ABSTRACT

ABSTRACT

A series of pyridopyrimidine derivatives were synthesized and evaluated for their ability to inhibit cyclic nucleotide synthesis in the presence of stable toxin a of Escherichia coli. The structure activity relationships around the basic core structure were examined and examples with better activity and potentially better pharmacological properties are presented.

Asunto(s)

Toxinas Bacterianas/metabolismo; GMP Cíclico/biosíntesis; Enterotoxinas/metabolismo; Pirimidinas/química; Línea Celular Tumoral; Escherichia coli/metabolismo; Proteínas de Escherichia coli; Guanilato Ciclasa/antagonistas & inhibidores; Guanilato Ciclasa/metabolismo; Humanos; Pirimidinas/síntesis química; Pirimidinas/farmacología; Receptores de Enterotoxina; Receptores Acoplados a la Guanilato-Ciclasa; Receptores de Péptidos/antagonistas & inhibidores; Receptores de Péptidos/metabolismo; Relación Estructura-Actividad

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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Pirimidinas / Toxinas Bacterianas / GMP Cíclico / Enterotoxinas Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: Estados Unidos

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