학술저널
3β-치환 5-Androstene-17-Carboxamides 합성과 5α-Reductase 저해 활성
Synthesis and 5α-Reductase Inhibitory Activity of 3β-Substituted 5-Androstene-17-Carboxamides
- 대한약학회
- 약학회지
- 제54권 제6호 (2010년)
-
2010.12466 - 473 (8 pages)
- 7
A series of 3β-substituted 5-androstene-17β-carboxamides were synthesized from analogs of 3β-hydroxy-5-androstene-17β-carboxylic acid (1) with tert-butylamine, N,N-diethylamine and 3-aminopyridine and some compounds were epoxidized with mCPBA. A rat prostate testosterone 5α-reductase inhibitory activity of synthesized compounds was assessed by radioimmunoassay using [1,2,6,7-3H]-testosterone as substrate. All synthesized compounds showed lower activity than finasteride and the N-(3-pyridino)-3β-carboxycarbonyloxy-5-androstene-17β-carboxamide (12) showed weak inhibitory activity (IC50: 2.4×10-7 M).
(0)
(0)