Synthesis of prolyl endopeptidase inhibitors and evaluation of their structure-activity relationships: In vitro inhibition of prolyl endopeptidase from canine brain

DOI: 10.1248/cpb.41.1583

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1583 - 1588 (1993)

Update date:2022-09-26

Topics: Synthesis Inhibitors In vitro Structure-activity relationships Prolyl endopeptidase

Authors:

Arai Arai

Nishioka

Niwa Niwa

Yamanaka

Tanaka Tanaka

Yoshinaga

Kobayashi

Miura Miura

Ikeda Ikeda

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

Article abstract of DOI:10.1248/cpb.41.1583

By chemical modification of a known prolyl endopeptidase (PEP) inhibitor (N-[N-(4-phenylbutanoyl)-L-prolyl]pyrrolidine; SUAM-1221), several arylalkanoyl derivatives (V-1-27) were synthesized and tested for in vitro inhibitory activity towards PEP from canine brain. Among them, 4-(2- thienyl)butanoyl derivatives (V-24-27) showed more potent PEP-inhibitory activity than SUAM-1221. The structure-activity relationships of these compounds are discussed.

Full text of DOI:10.1248/cpb.41.1583

NII-Electronic Library Service

Products guided by the article

Product name:(S)-1-(4-Phenyl-butyryl)-piperidine-2-carboxylic acid

Cas No:130791-47-8

R&D Labs maybe for 130791-47-8

KINHENG CHEMICAL(SHANGHAI)CO., LTD.

Contact:+8621-60490170

Address:Room401, No.28,Lane 189, Yangshupu Rd. Shanghai, China.
MS( MAOSHENG )Chemical CO.,LTD

Contact:+86-519-82726678.82726378

Address:TAOXI INDUSTRY ZONE JINTAN
jiangsu senxuan pharmaceutical and chemical co.,ltd

Contact:86-523-87982810

Address:hongqiao industrial zone,taixing,jiangsu china
Chemsigma International Co.,Ltd.

website:http://www.chemsigma.com

Contact:86-025-58748998

Address:Rm.705, 15th Building,Rd.Xinke II
LIAONING DMSO CHEMICALS CO.,LTD.

website:http://www.chinadmso.com

Contact:+86-427-6503033

Address:FLOOR 16, BLOCK A, FINANCIAL SQUARE, XINGLONGTAI DISTRICT, PANJIN CITY, LIAONING P.R. CHINA

Relevant to this article

Resolution of pentafluorophenyl 2-phenylpropanoate using combinations of quasi-enantiomeric oxazolidin-2-ones

Doi:10.1016/j.tetasy.2011.02.022
(2011)
Donor-Acceptor Distance Sampling Enhances the Performance of "better than Nature" Nicotinamide Coenzyme Biomimetics

Doi:10.1021/jacs.6b05625
(2016)
Azaindolo[3,2,1-jk]carbazoles: New Building Blocks for Functional Organic Materials

Doi:10.1002/chem.201805578
(2019)
The first total synthesis of (±)-cyclophostin and (±)-cyclipostin P: Inhibitors of the serine hydrolases acetyl cholinesterase and hormone sensitive lipase

Doi:10.1021/ol200991x
(2011)
Concise substrate-controlled asymmetric total synthesis of (+)-3-(Z)-dihydrorhodophytin

Doi:10.3987/COM-10-S(E)76
(2011)
Enantioselective cycloetherification in a micellar catalysis system

Doi:10.1016/S1872-2067(10)60169-6
(2011)

Article Doi