|Keywords||Antidepression / 11, 13, 15-Triazasteroid / Benzocycloheptapyrimidine / Antireserpine / B-Homoazasteroid / B, D-Dihomoazasteroid / 17-Oxide / 11, 13, 15, 17-Tetraazasteroid / 抗うつ / 11,13,15ートリアザステロイド / ベンゾシクロヘプタビリミジン / 抗レセルピン / Bーホモアザステロイド / B,Dージホモアザステロイド / 17ーオキシド / 11,13,15,17ーテトラアザステロイド / アザステロイド / ベンゾシクロヘプタピリミジン / アルキルアミン / B-ホモアザステロイド / B,D-ジホモアザステロイド / 11、13、15-トリアザステロイド|
As one of the researches of synthesis of the compounds related to azasteroid and their evaluation of antidepressive activity using 11, 13, 15-triazasteroid (1) as a lead compound, B-homo-11, 13, 15-triazasteroids (2) bearing a alkyl group on D ring, B,D-dihomo-11, 13, 15-triaza-steroids (3) bearing a alkyl group on D ring, 6, 7-dihydro-5H-benzo [6, 7] cyclohepta [1, 2-d] pyrimidines (4) corresponding to D-secoazasteroid and bearing a alkylamino group on its 4-position, 11, 13, 15, 17-tetraazasteroids (5, n = 1) whose D ring was expanded to pyrimidine from imidazole, their B-homologue (5, n=2), and 17-oxides (6) of compound 5 were synthesized. Next, the evaluation of the antireserpine acivity of the above synthesized compounds and their precursors was performed as one of the first screening of the antidepressive activity. In compounds 2, only some tricyclic benzo [6, 7] cyclohepta [1, 2-d] pyrimidines which were precursors of corresponding tetracyclic azasteroid exhibited effective activity. In compounds 3, neither compounds 3 nor their precursors exhibited antireserpine activity. In compounds 4, only compounds, which have two carbon atoms between nitrogen atom attached to 4-position and oxygen atom at the terminal position of the side chain and also have branched side chain, exhibited effective one. In compounds, both 11, 13, 15, 17-tetraazasteroid without any substituent on its skeleton and ist B-homolgue exhibited effective activity. Their precursor, 4-amino-6, 7-dihydro -5H-benzo [6, 7] cyclohepta [1, 2-d] pyrimidine, also exhibited the similar one. In N-oxides (6), positive compounds could not be recognized.