159675-87-3Relevant academic research and scientific papers
Amidinophenol derivatives
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, (2008/06/13)
Amidinophenol derivatives of the formula (I): STR1 wherein R1 and R2 are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO2, (vii) benzoyl, (viii) COOR4 (in which R4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R5)=C(R6)-- (in which R5 and R6 are H or C1-4 alkyl; R3 is (i) CON(R7)(R8), (ii) CON(R9)--CH(R7)(R8) or (iii) STR2 in which STR3 is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R10 is H, C7-10 phenylalkyl or COOR13 (in which R13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R7 and R8 do not represent hydrogen at the same time, and (ii) when at least one group in R7, R8 and R9 represents the group containing t-butyl ester, the other groups do not represent tile group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.
New Orally Active Serine Protease Inhibitors: Structural Requirements for Their Good Oral Activity
Senokuchi, Kazuhiko,Nakai, Hisao,Nakayama, Yoshisuke,Odagaki, Yoshihiko,Sakaki, Katsuhito,et al.
, p. 4508 - 4517 (2007/10/03)
Synthesis and structural requirements for good oral activity of a series of para-substituted benzoyl esters of 4-hydroxybenzamidine serine protease inhibitors are described.The structure required for good oral activity was found to be general formula II w
