Bioorganic and Medicinal Chemistry Letters p. 1935 - 1940 (1998)
Update date:2022-09-26
Topics:
Jacobs, Robert T.
Shenvi, Ashok B.
Mauger, Russell C.
Ulatowski, Terrance G.
Aharony, David
Buckner, Carl K.
A series of 4-alkylpiperidine derivatives related to the potent neurokinin-2 (NK2) receptor antagonist SR-48968 (1) is described. Simple aliphatic derivatives were found to be poorly active, but appropriate placement of an alcohol functional group afforded compounds that were of similar activity to 1. Several representatives in this series, such as the 4- (1-hydroxy-1-ethylpropyl)piperidine (14), were found to exhibit oral activity in a model of labored abdominal breathing in guinea pigs. These results expand the latitude of substituents available in this region of this series of NK2 receptor antagonists.
View MoreContact:+86-(0)21-3770 9035
Address:Room 301, Building 2, Meijiabang Road 1508, Shanghai China
lianyungang jinkang pharmaceutical technology co., ltd.
Contact:008651885445517
Address:Jinshan industrial park, Ganyu county, Lianyungang, Jiangsu Province, 222115, China
Shandong Jiulong Hisince Pharmaceutical Co.,Ltd.
Contact:+86-15853188990
Address:Huadian Pioneer Park, Huadian Township, Qihe County, Dezhou City, Shandong, P.R.China
Zhejiang Golden-Shell Pharmaceutical Co.,Ltd.
Contact:+86-576-87501888 / 87501988
Address:No.89 Zhongxing Road. Li'ao, Yuhuan, Zhejiang, China
website:https://www.synose.com/
Contact:86-579-82275537
Address:No.1958 Liyu Road , jinhua,zhejiang,China
Doi:10.1039/c39940002081
(1994)Doi:10.1021/ja502238a
(2014)Doi:10.1002/anie.201311245
(2014)Doi:10.1002/recl.19941130603
(1994)Doi:10.1055/s-0033-1340220
(2014)Doi:10.1021/np500260z
(2014)
