Novel phenoxyalkylamine derivatives. VII. Synthesis and pharmacological activities of 2-alkoxy-5-[(phenoxyalkylamino)alkyl]benzenesulfonamide derivatives

DOI: 10.1248/cpb.40.1443

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1443 - 1451 (1992)

Update date:2022-07-30

Topics:

Authors:

Sakurai Sakurai

Mitani Mitani

Hashimoto

Morikawa

Yasuda Yasuda

Koshinaka

Kato Kato

Ito Ito

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1248/cpb.40.1443

To find a novel α-blocker with high α-blocking selectivity against dopamine D₂-receptor affinity, we performed structural modification of the alkylene chains and the substituents on two benzene rings of 2-alkoxy-5-[(phenoxyalkylamino)alkyl]benzenesulfonamide derivatives. The modification of the alkylene chain between the amino moiety in the center of the molecule and the benzene ring (ring A) was found to be the most significant. 5-[2-[[2-(5-Fluoro-2-methoxyphenoxy)ethyl]amino]propyl]-2-methoxybenze nesulfonamide (II-4), which possesses 1-methylethyl as the alkylene chain, exhibited high α-blocking selectivity as well as potent α-blocking activity.

Full text of DOI:10.1248/cpb.40.1443

NII-Electronic Library Service

Products guided by the article

Product name:N-Hexyl-2-methoxy-5-(2-oxo-propyl)-benzenesulfonamide

Cas No:144818-73-5

R&D Labs maybe for 144818-73-5

qingdao goldenchem imp and exp co.,ltd.

Contact:532-55579246

Address:no.62 ,haier road laoshan distirct
Shanghai Puda Chemical Co.,Ltd

Contact:+86+571+56565965

Address:10F Haiyue Building,Danfeng Road,Binjiang District,Hangzhou,China
SHANDONG AONA CHEMICAL CO.,LTD.

Contact:86-532-85762926

Address:LIUYUAN TOWN, ZAOZHUANG CITY, SHANGDONG PROVINCE.
ANGCHEN BRIGHTCHEM CO., LTD

website:http://www.angchenchem.com

Contact:+86-510-88302099 82327577

Address:Rm. 404/405, Floor 4th, No. 983 FengXiang Road, Wuxi, China
shanghai Tauto Biotech Co., Ltd

website:http://www.tautobiotech.com/en/index.htm

Contact:+86-21-51320588 ext. 8025

Address:No. 326, Aidisheng Rd , Zhangjiang Hi-tech Park, Shanghai , P.R.CHINA

Relevant to this article

2,4,6-triarylphosphinines versus 2,4,6-triarylpyridines: An investigation of the differences in reactivity between structurally related aromatic phosphorus and nitrogen heterocycles

Doi:10.1002/chem.201302441
(2013)
Preparation of a nylon-11 precursor from renewable canola oil

Doi:10.1055/s-0033-1338478
(2013)
Synthesis of esters from acyl chlorides and halide under solid-liquid phase transfer catalysis

Doi:10.1080/00397919208021541
(1992)
Synthesis of functionalized cyclotriveratrylene analogues with C ₁-symmetry and the application for 1,4-Michael addition of alcohols to unsaturated aryl ketone

Doi:10.1016/j.tet.2013.06.077
(2013)
Oligo(2′-O-methylribonucleotides) and their derivatives: IV. Conjugates of oligo(2′-O-methylribonucleotides) with minor groove binders and intercalators: Synthesis, properties, and application

Doi:10.1134/S1068162013010081
(2013)
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses

Doi:10.1021/acs.jmedchem.7b01536
(2018)

Article Doi