Aziridine-2-carboxylic acid derivatives and its open-ring isomers as a novel PDIA1 inhibitors

被引：3

作者：

Leite, Irena ^{[1
]}

Andrianov, Victor ^{[1
]}

Zelencova-Gopejenko, Diana ^{[1
]}

Loza, Einars ^{[1
]}

Kazhoka-Lapsa, Iveta ^{[1
]}

Domracheva, Ilona ^{[1
]}

Stoyak, Marta ^{[2
]}

Chlopicki, Stefan ^{[2
]}

Kalvins, Ivars ^{[1
]}

机构：

[1] Latvian Inst Organ Synth, 21 Aizkraukles St, LV-1006 Riga, Latvia

[2] Jagiellonian Univ, Jagiellonian Ctr Expt Therapeut, 14 Bobrzynskiego St, PL-30348 Krakow, Poland

来源：

CHEMISTRY OF HETEROCYCLIC COMPOUNDS | 2021年 / 57卷 / 11期

关键词：

aziridine-2-carboxylic acid; DFT calculation; isomerisation; PDIA1 inhibitors P; PROTEIN DISULFIDE-ISOMERASE; CHARGES; ESTERS;

D O I：

10.1007/s10593-021-03034-x

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Acyl derivatives of aziridine-2-carboxylic acid have been synthesized and tested as PDIA1 inhibitors. Calculations of charge value and distribution in aziridine ring system and some alkylating agents were performed. For the first time was found that acyl derivatives of aziridine-2-carboxylic acid are weak to moderately active PDIA1 inhibitors.

引用

页码：1086 / 1106

页数：21

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