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New 4‐Amino‐7,8‐dimethoxy‐5 h ‐pyrimido[5,4‐ b ]indole Derivatives: Synthesis and Studies as Inhibitors of Phosphodiesterases
Author(s) -
Monge Antonio,
MartínezCrespo Francisco J.,
Villanueva M. Aránzazu,
Font María,
Santiago Esteban,
Mart Juan J.,
de Irujo Ínez,
Alberdi Elena,
LópezUnzu M. José,
Cenarruzabeitia Edurne,
Castiella Elena,
Frechillac Diana
Publication year - 1993
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19933261108
Subject(s) - indole test , chemistry , stereochemistry , phosphodiesterase , chemical synthesis , combinatorial chemistry , enzyme , organic chemistry , biochemistry , in vitro
A series of 4‐amino‐7,8‐dimethoxy‐5 h ‐pyrimido[5,4‐ b ]indole derivatives has been synthesized. These compounds resemble carbazeram and other pyridazino compounds with activity in the cardiovascular system. Some of these new compounds possess inotropic activity (Table 2), with a complementary effect on the inhibition of different CGI‐PDE (Table 3). The most active compounds 5, 6d , and 7 also possess activity as vasodilators (Table 4). Some of these new compounds inhibit blood platelet aggregation induced by ADP and AA and are active as inhibitors of human platelet PDEs (Tables 5 and 6).