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pyridin-2-yl sulfanyl acid esters and processes for their preparation
专利权人:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
发明人:
BALARAM GHOSH,DILIP CHANDRA BORA,JADAB CHANDRA SARMA,PARUCHURI GANGADHAR RAO,SAKSHI BALWANI
申请号:
BR112013001244
公开号:
BR112013001244A2
申请日:
2011.07.20
申请国别(地区):
BR
年份:
2016
代理人:
摘要:
pyridin-2-yl sulfanyl acid esters and process for their preparation. The present invention relates to pyridin-3-yl sulfanyl acid ester compounds having anti-inflammatory properties. The present invention particularly relates to novel pyridin-2-yl sulfanyl anti-inflammatory heterocyclic acid esters having the structure of formula 1 which have been screened for their anti-inflammatory activity with respect to inhibition of adhesion of neutrophils isolated from the human peripheral blood on the surface of human umbilical vein endothelial cells (huvec) as a result of inhibition of icam-1 cytokine stimulated expression of cell adhesion molecule. rs-z, 3-pentyl (pyridin-2-yl-sulfanyl) -propionic acid compound (structure 1a, r1-1 = h, r2-2 = h, r3- = ch2-2) cooc ~ 5 ~ h ~ 11 ~) has been found to be more effective in inhibiting adhesion of neutrophil and icam-1 and has been found to effectively alleviate inflammation mediated by excessive leukocyte infiltration that induces inflammatory disorders or similar conditions such as injury. pulmonary artery and acute respiratory distress syndrome in mice.ésteres de ácido de piridin-2-il sulfanila e processo para a preparação dos mesmos. a presente invenção refere-se aos compostos de éster de ácido de piridin-3-il sulfanila tendo propriedades anti-inflamatórias. a presente invenção particularmente se refere aos novos ésteres de ácido heterocíclico anti-inflamatórios de piridin-2-il sulfanila tendo a estrutura de fórmula geral 1 que foram analisados quanto a sua atividade anti-inflamatória com respeito à inibição de adesão de neutrófilos, isolados do sangue periférico humano, na superfície de células endoteliais de veia umbilical humana (huvec) como um resultado de inibição da expressão estimulada por citocina de icam-1 de molécula de adesão celular. o composto rs-z, 3-pentil éster de ácido (piridin-2-il-sulfanil)-propiônico (estrutura 1a, r~ 1~ = h, r~ 2~ = h, r~ 3~ = ch~ 2~cooc~ 5~h~ 11~) foi descoberto ser mais eficaz quanto à in
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