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Synthesis and biological testing of 3‐phenyloctahydro‐pyrimido[1,2‐ a ]‐ s ‐triazine derivatives
Author(s) -
Lucry Line,
Enoma Ferdinand,
Estour François,
MÉnager Sabine,
Lafont Olivier,
Oulyadi Hassan
Publication year - 2002
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570390410
Subject(s) - chemistry , synthon , microsporum canis , triazine , in vitro , stereochemistry , antifungal , 1,3,5 triazine , biological activity , combinatorial chemistry , organic chemistry , biochemistry , microbiology and biotechnology , biology
A series of 46 3‐phenyloctahydropyrimido[1,2‐ a ]‐ s –triazine derivatives were synthesized. This synthesis was performed via iminodimethylation of dialkylated 2‐aminopyrimidinedione synthons by substituted primary arylamines. In vitro pharmacological evaluation of these compounds is reported. One of them exhibited antifungal activity against Microsporum canis (10 −6 50 10 −5 mol/L), and another showed affinity for serotoninergic 5‐HT 1A and 5‐HT 2b receptors (10 −8 50 10 −7 mol/L).