Synthesis and biological activities of novel β-carbolines as PDE5 inhibitors

被引：16

作者：

Sui, ZH ^{[1
]}

Guan, JH ^{[1
]}

Macielag, MJ ^{[1
]}

Jiang, WQ ^{[1
]}

Qiu, YH ^{[1
]}

Kraft, P ^{[1
]}

Bhattacharjee, S ^{[1
]}

John, TM ^{[1
]}

Craig, E ^{[1
]}

Haynes-Johnson, D ^{[1
]}

Clancy, J ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(02)01036-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-2-furoyl and N(2)pyrimidinyl beta-carbolines was discovered to possess potent inhibitors activity against PDE5. During the synthesis we developed a tandem resin quenching protocol. which allowed us to synthesize large number of target compounds in a rapid fashion. Representative Compounds exhibit superior selectivity to sildenafil versus other isozymes of PDEs. and demonstrated in vivo efficacy in increasing introcavernosal pressure in dogs. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：761 / 765

页数：5

共 50 条

[21] Comparison of phosphodiesterase type 5 (PDE5) inhibitors
Wright, P. J.
INTERNATIONAL JOURNAL OF CLINICAL PRACTICE, 2006, 60 (08) : 967 - 975
[22] Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors
Wang, YG
Chackalamannil, S
Hu, ZY
Boyle, CD
Lankin, CM
Xia, Y
Xu, R
Asberom, T
Pissarnitski, D
Stamford, AW
Greenlee, WJ
Skell, J
Kurowski, S
Vemulapalli, S
Palamanda, J
Chintala, M
Wu, P
Myers, J
Wang, P
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (21) : 3149 - 3152
[23] A molecular dynamics study comparing the interactions of four major PDE5 inhibitors with PDE5/PDE6
Song, Seunghun
Park, Soon Woo
Lee, Byung Ho
Kim, Moon K.
BIOPHYSICAL JOURNAL, 2024, 123 (03) : 470A - 470A
[24] Further reassurance regarding PDE5 inhibitors
Hackett, G. I.
INTERNATIONAL JOURNAL OF CLINICAL PRACTICE, 2007, 61 (09) : 1426 - 1427
[25] PDE5 inhibitors beyond erectile dysfunction
P Sandner
J Hütter
H Tinel
K Ziegelbauer
E Bischoff
International Journal of Impotence Research, 2007, 19 : 533 - 543
[26] PDE5 inhibitors and permanent visual loss
Tomsak, R
INTERNATIONAL JOURNAL OF IMPOTENCE RESEARCH, 2005, 17 (06) : 547 - 549
[27] PDE5 inhibitors: looking beyond ED
Jackson, G
INTERNATIONAL JOURNAL OF CLINICAL PRACTICE, 2003, 57 (03) : 159 - 160
[28] PDE5 inhibitors in diabetic peripheral neuropathy
Hackett, G.
INTERNATIONAL JOURNAL OF CLINICAL PRACTICE, 2006, 60 (09) : 1123 - 1126
[29] The efficacy of PDE5 inhibitors in diabetic patients
Swiecicka, Agnieszka
ANDROLOGY, 2023, 11 (02) : 245 - 256
[30] Effect of PDE5 inhibitors in diabetic neuropathy
Kulkarni, Shrinivas K.
Patil, Chandrashekhar S.
Singh, Vijay P.
INFLAMMATION RESEARCH, 2005, 54 : S192 - S192

← 1 2 3 4 5 →