当前位置： SCI文献检索 > BIOORGANIC CHEMISTRY期刊下所有文献 > Synthesis and biological evaluation of some N-(3-(1H-tetrazol-5-yl) phenyl)acetamide derivatives as novel non-carboxylic PTP1B inhibitors designed through bioisosteric modulation.

Synthesis and biological evaluation of some N-(3-(1H-tetrazol-5-yl) phenyl)acetamide derivatives as novel non-carboxylic PTP1B inhibitors designed through bioisosteric modulation.

Abstract：

:Described herein is the synthesis and biological evaluation of a series of non-carboxylic inhibitors of Protein Tyrosine Phosphatase 1B designed using bioisosteric replacement strategy. Six N-(3-(1H-tetrazol-5-yl)phenyl)acetamide derivatives designed employing the aforementioned strategy were synthesized and screened for PTP1B inhibitory activity. Among the synthesized compounds, compound NM-03 exhibited the most potent inhibitory activity with IC50 value of 4.48 µM. Docking studies with NM-03 revealed the key interactions with desired amino acids in the binding site of PTP1B. Furthermore, compound NM-03 also elicited good in vivo activity. Taken together, the results of this study establish N-(3-(1H-tetrazole-5-yl)phenyl)-2-(benzo[d]oxazol-2-ylthio)acetamide (NM-03) as a valuable lead molecule with great potential for PTP1B inhibitor development targeting diabetes.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Maheshwari N,Karthikeyan C,Bhadada SV,Sahi C,Verma AK,Hari Narayana Moorthy NS,Trivedi P

doi

10.1016/j.bioorg.2018.06.016

subject

Has Abstract

pub_date

2018-10-01 00:00:00

pages

145-150

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)30313-4

journal_volume

80

pub_type

杂志文章

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