Novel fluorinated antiinflammatory steroid with reduced side effects: methyl 9 alpha-fluoroprednisolone-16-carboxylate.
Novel fluorinated antiinflammatory steroid with reduced side effects: methyl 9 alpha-fluoroprednisolone-16-carboxylate.
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副作用减少的新型氟化抗炎类固醇：9 α-氟泼尼松龙-16-甲酸甲酯。
DOI：
10.1002/jps.2600830406
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发表时间：
1994
影响因子：
3.8
通讯作者：
Lee,HJ
中科院分区：
文献类型：
--
作者：
McLean,HM;Khalil,MA;Heiman,AS;Lee,HJ
In an effort to test the hypothesis that 9α-fluorination of a steroidal antedrug would enhance receptor binding affinity and local antiinflammatory activity, without concomitantly increasing adverse systemic effects, a fluorinated analog,10, of methyl 11β,21-dihydroxy-3,20-dioxo-1,4-pregnadiene-16α-carboxylate (DP16CM,1) was synthesized and evaluated. In the acute rat croton oil-induced ear edema bioassay,10was found to be twice as potent as1. This increase in topical potency was consistent with enhanced binding affinity of10, relative to1. The IC50values for displacement of [3H] dexamethasone from glucocorticoid receptors of rat hepatoma tissue culture cells were 0.16, 1.2, and 0.03μM for10, 1, and prednisolone, respectively. Following multiple topical ID50applications of prednisolone,1, and its new fluorinated analog,10, in the rat subacute croton oil-induced ear edema bioassay, only prednisolone exhibited significant untoward effects, such as reduction in relative thymus and adrenal weights, plasma corticosterone levels, and normal body weight gain. Thus, while fluorination of1enhanced its topical potency, there was not a concomitant increase in untoward systemic effects. This lack of adverse systemic effects is ostensibly due to the presence of the metabolically labile 16-carboxylate ester moiety.
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通讯：16-亚甲基和 Δ15-16-甲基皮质类固醇
影响因子：
3.6
作者：
D. Taub;R. D. Hoffsommer;N. Wendler
通讯作者：
N. Wendler
影响因子：
3.8
作者：
PONEC, M;KEMPENAAR, J;CARON, JC
通讯作者：
CARON, JC
合成新型抗炎类固醇 20-甲酰胺：(20R)- 和 (20S)-21-(N-取代氨基)-11 beta,17,20-三羟基-3,21-二氧代-1,4-孕二烯。
影响因子：
7.3
作者：
Kim,HP;Bird,J;Heiman,AS;Hudson,GF;Taraporewala,IB;Lee,HJ
通讯作者：
Lee,HJ
抗炎吡唑类固醇：强效糖皮质激素，含有大量 A 环取代基且不含 C3-羰基。
DOI：
--
发表时间：
1979
期刊：
Biochemical and Biophysical Research Communications - BBRC
影响因子：
--
作者：
S. Simons;E. Thompson;D. F. Johnson
通讯作者：
D. F. Johnson
氢化可的松类似物的生物活性与其被大鼠肝酶系统灭活的速率之间的关系。
影响因子：
4.8
作者：
E. M. Glenn;R. O. Stafford;S. C. Lyster;B. Bowman
通讯作者：
B. Bowman