Bioorganic and Medicinal Chemistry p. 1895 - 1899 (2001)
Update date:2022-07-30
Topics: Characterization Chemical Synthesis Structure-Activity Relationship (SAR) Studies Safety and Toxicity Assessment Design and Synthesis Publication and Reporting
Kim, Dae-Kee
Ryu, Do Hyun
Lee, Namkyu
Lee, Ju Young
Kim, Jae-Sun
Lee, Sukho
Choi, Jin-Young
Ryu, Je-Ho
Kim, Nam-Ho
Im, Guang-Jin
Choi, Won-Son
Kim, Tae-Kon
New sildenafil analogues with an N-acylamido group at the 5′-position of the phenyl ring, 6a-e, were prepared from the readily available starting compound 2 in four straightforward steps. Enzyme assays demonstrated that all the target compounds 6a-e showed higher PDE5 inhibitory activities than sildenafil. It was observed that the PDE5 inhibitory activity was enhanced as the chain length of R group increased, but introduction of the branched alkyl groups such as isopropyl (6d) and cyclohexyl (6e) resulted in the drop of potency compared with 6c. In particular the N-butyrylamido derivative 6c exhibited the highest PDE5 inhibitory activity, and was about 6-fold more potent than sildenafil. However, all the compounds exhibited somewhat weak selectivity (1-3-fold) over PDE6, indicating that the compounds 6a-e have intrinsically lower selectivity than sildenafil. Copyright
View MoreJining tiansheng chemical co.,ltd.
Contact:+86-537-5158722
Address:ROOM 1011, BLOCK B, CUIDU INTERNATIOAL BUSINESS CENTER, JINING CITY, CHINA
XI'AN CHUKANG BIOTECHNOLOGY CO.,LTD
Contact:29-63685658 63685359
Address:Room 3-1202,Building 1,Oriental oasis,East of Xianning Road,Xi'an,Shaanxi 710043 P.R.China
Changzhou Litong Chemical Co., Ltd.
website:http://www.litonchem.com/
Contact:+86-519-86301238
Address:Laoba Rd, Hutang town Changzhou Jiangsu
SPRING CHEMICAL INDUSTRY CO.,LTD
Contact:86-187-66672125
Address:linchi industry park.zouping
Shanghai Kangxin Chemical Co., Ltd
Contact:+86 21 60717227
Address:118,Ganbai Village,Waigang Town,Jiading District,Shanghai
Doi:10.1007/s13738-021-02192-1
(2021)Doi:10.1055/s-2001-16089
(2001)Doi:10.1002/chem.200900608
(2009)Doi:10.1016/0040-4020(72)80085-1
(1972)Doi:10.1021/ja00820a041
(1974)Doi:10.1007/BF00477432
()