Studies on agents with vasodilator and β-blocking activities. V. Synthesis and pharmacological activity of the optical isomers of TZC-5665

DOI: 10.1248/cpb.46.84

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 84 - 96 (1998)

Update date:2022-08-05

Topics:

Authors:

Seki, Toshimi

Kanada, Arihiro

Nakao, Tomio

Shiraiwa, Masahumi

Asano, Hajime

Miyazawa, Katuhiko

Ishimori, Tsutomu

Minami, Nobuyoshi

Shibata, Kenyu

Yasuda, Kikuo

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

Article abstract of DOI:10.1248/cpb.46.84

Synthesis of the four optical isomers of TZC-5665 (1), a candidate for the treatment of congestive heart failure, was achieved by the reaction of chiral diaminopyridazinone (2) with chiral glycidyl ether (3). The hypotensive and β-blocking activities of 1 and its optical isomers were examined when given intravenously into anesthetized rats. Furthermore these compounds were evaluated for inhibitory activity on cAMP phosphodiesterase III. Among the four optical isomers, R(A),S(B)-one (1c) possessed the essential activities of TZC-5665 (1).

Full text of DOI:10.1248/cpb.46.84

NII-Electronic Library Service

Products guided by the article

Product name:4-(4-Acetylamino-phenyl)-2-hydroxy-3-methyl-4-oxo-butyric acid

Cas No:203259-42-1

R&D Labs maybe for 203259-42-1

Shanghai doly chemical Co.,Ltd

Contact:+86-21-34716221

Address:No.328,WuHe Roard,MinHang,ShangHai China
Huangshi Shennong Chemical Technology Co., Ltd

Contact:+86-714-3072290

Address:Eastern industrial park , Tieshan district , Huangshi city ,Hubei province , China
Taiwan Surfactant Corp.

Contact:886 2 2541 0022

Address:8 Fl., No. 11, Sec. 1, Chung Shan North Rd., Taipei, Taiwan R.O.C.
YingYing Pharmaceutical Co.,Ltd

Contact:86-18854126208

Address:55#, yingxiongshan road
Jinan Kaypharm Chemical Co.,Ltd

Contact:86-0531-86986780

Address:Room101,No189-2,Huayuan Road,Jinan City,Shandong Province

Relevant to this article

Doi:10.1021/ja01083a022
(1965)
Concerning the alkaloid eripine from Hunteria umbellata

Doi:10.1002/hlca.19680510627
(1968)
Symmetry-Assisted Synthesis of C₂-Symmetric trans-α,α'-Bis(hydroxymethyl)pyrrolidine and -piperidine Derivatives via Double Sharpless Asymmetric Dihydroxylation of αω-Terminal Dienes

Doi:10.1021/jo971995f
(1998)
Total synthesis and structural revision of viridicatumtoxin B

Doi:10.1002/anie.201304691
(2013)
Design, synthesis and metal binding properties of a mixed-donor macrobicycle

Doi:10.1039/a707354b
(1998)
Synthetic studies toward astins A, B and C. Efficient syntheses of cis- 3,4-dihydroxyprolines and (-)-(3S,4R)-dichloroproline esters

Doi:10.1016/S0957-4166(97)00617-4
(1998)

Article Doi