3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation
摘要:
3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural test these compounds were effective in reducing exudate volume and accumulation of white blood cells. This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin. The structural requirements for inhibiting the Arthus reactions were studied by systematic chemical modification of 1. These structure-activity relationship studies revealed that nitrogen 1' of the hydrazino group is essential for activity and must be electron rich, whereas chemical modifications of other sites of 1 had only a modest effect on activity.
[1-(2-Oxazolyl) or -(2-thiazolyl) hydrazino]alkyl nitriles
申请人:Abbott Laboratories
公开号:US04489084A1
公开(公告)日:1984-12-18
Described are oxazolyl (or thiazolyl) hydrazinoalkyl nitrile compounds of the formula ##STR1## wherein R is hydrogen or loweralkyl, R.sub.1 and R.sub.2 independently of one another denote hydrogen, loweralkyl, or phenyl or naphthyl substituted with halo, loweralkyl or loweralkoxy, X is oxygen or sulfur, n and m are each an integer from 0 to 3 inclusive, or pharmaceutically acceptable salts thereof. The compounds are useful as anti-inflammatory agents.
HAVIV, FORTUNA;RATAJCZYK, JAMES D.;DENET, ROBERT W.;KERDESKY, FRANCIS A.;+, J. MED. CHEM., 31,(1988) N 9, C. 1719-1728
作者:HAVIV, FORTUNA、RATAJCZYK, JAMES D.、DENET, ROBERT W.、KERDESKY, FRANCIS A.、+
DOI:——
日期:——
US4489084A
申请人:——
公开号:US4489084A
公开(公告)日:1984-12-18
3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation
作者:Fortuna Haviv、James D. Ratajczyk、Robert W. DeNet、Francis A. Kerdesky、Roland L. Walters、Steven P. Schmidt、James H. Holms、Patrick R. Young、George W. Carter
DOI:10.1021/jm00117a010
日期:1988.9
3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural test these compounds were effective in reducing exudate volume and accumulation of white blood cells. This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin. The structural requirements for inhibiting the Arthus reactions were studied by systematic chemical modification of 1. These structure-activity relationship studies revealed that nitrogen 1' of the hydrazino group is essential for activity and must be electron rich, whereas chemical modifications of other sites of 1 had only a modest effect on activity.