SYNTHESIS AND AMINOPEPTIDASE N INHIBITING ACTIVITY OF 3-(NITROPHENOXYMETHYL)-[1,3,2]DIOXABOROLAN-2-OLS AND THEIR OPEN ANALOGUES

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14160%2F17%3A00120955" target="_blank" >RIV/00216224:14160/17:00120955 - isvavai.cz</a>

Alternative codes found

RIV/62157124:16370/17:43876166

Result on the web

<a href="https://europepmc.org/article/med/29474769" target="_blank" >https://europepmc.org/article/med/29474769</a>

DOI - Digital Object Identifier

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Result language

angličtina

Original language name

SYNTHESIS AND AMINOPEPTIDASE N INHIBITING ACTIVITY OF 3-(NITROPHENOXYMETHYL)-[1,3,2]DIOXABOROLAN-2-OLS AND THEIR OPEN ANALOGUES

Original language description

Aminopeptidase N (APN) represents a class of zinc metallopeptidases with broad substrate specifity. This enzyme is involved in control of angioneogenesis in cancer and microvascular conditions. It also serves as a superficial cellular receptor that enables attachment of some viruses including coronaviruses to the host cell. APN takes part also in metabolism of some important neuropeptides. That is why APN can be a promising therapeutic target and compounds which influence its activity interesting potential drugs. Here, synthesis of compounds which in most contain 3-phenoxypropan-1,2 diol moiety and evaluation of their inhibition activity against APN is described. 4-[1-, 2- and 3-(Nitrophenoxymethyl)]-[1,3,2]dioxaborolan-2-ols are novel compounds which have never been previously reported in the literature. 3-(Aminophenoxy)propyl-1,2-diols revealed greater activity than both 3-(nitrophenoxy)propyl-1,2-diols and 3-(nitrophenoxymethyl)-[1,3,2]dioxaborolan-2-ols. A QSAR study revealed a linear correlation between lipophilicity and inhibition activity.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

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OECD FORD branch

30104 - Pharmacology and pharmacy

Project

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Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2017

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

ACTA POLONIAE PHARMACEUTICA

ISSN

0001-6837

e-ISSN

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Volume of the periodical

74

Issue of the periodical within the volume

1

Country of publishing house

PL - POLAND

Number of pages

9

Pages from-to

127-135

UT code for WoS article

000410257700014

EID of the result in the Scopus database

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