Synthesis and antiviral activity of new acrylamide derivatives containing 1,2,3-thiadiazole as inhibitors of hepatitis B virus replication.

Eur J Med Chem

State Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center (Tianjin), Nankai University, Tianjin 300071, China.

Published: May 2010

A series of new acrylamide derivatives containing 1,2,3-thiadiazole were synthesized, characterized, and evaluated for their anti-hepatitis B virus (HBV) activities in vitro. The IC50 of compounds 9b (10.4 microg/mL), 9c (3.59 microg/mL) and 17a (9.00 microg/mL) of the inhibition on the replication of HBV DNA were higher than that of the positive control lamivudine (14.8 microg/mL). Compound 9d exhibited significant activity against secretion of HBeAg (IC50=12.26 microg/mL).

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2010.01.032DOI Listing

Publication Analysis

Top Keywords

acrylamide derivatives
8
derivatives 123-thiadiazole
8
microg/ml
5
synthesis antiviral
4
antiviral activity
4
activity acrylamide
4
123-thiadiazole inhibitors
4
inhibitors hepatitis
4
hepatitis virus
4
virus replication
4

Similar Publications

Succinyldiamide derivatives are important structural motifs in various natural products, pharmaceuticals, and functional materials. Herein, a novel, mild, and environmentally friendly method was developed for synthesizing functionalized succinyldiamides each containing a quaternary carbon center. This strategy was designed to involve photocatalytic decarboxylation of readily available oxalic monoamide using a non-precious metal photocatalyst, 4CzIPN, followed by a free-radical addition/Smiles rearrangement cascade reaction of -aryl--(arylsulfonyl)acrylamides.

View Article and Find Full Text PDF

Under the increasing severity of drought issues and the urgent need for the resourceful utilization of agricultural waste, this study aimed to compare the soil water retention properties of hydrogels prepared from Chinese cabbage waste (CW) and banana peel (BP) using grafting techniques with acrylic acid (AA) and acrylamide (AAm). Free radical polymerization was initiated with ammonium persulfate (APS), and N, N'-methylene bisacrylamide (MBA) served as the crosslinking agent to fabricate the grafted polymer hydrogels. The hydrogels were subjected to detailed evaluations of their water absorption, reusability, and water retention capabilities through indoor experiments.

View Article and Find Full Text PDF

Discovery and biological evaluation of potent 2-trifluoromethyl acrylamide warhead-containing inhibitors of protein disulfide isomerase.

Eur J Med Chem

February 2025

Ph.D. Program in Drug Discovery and Development Industry, College of Pharmacy, Taipei Medical University, Taipei, Taiwan; School of Pharmacy, Taipei Medical University, Taipei, Taiwan. Electronic address:

Protein disulfide isomerase (PDI) regulates multiple protein functions by catalyzing the oxidation, reduction, and isomerization of disulfide bonds. The enzyme is considered a potential target for treating thrombosis. We previously developed a potent PDI inhibitor, CPD, which contains the propiolamide as a warhead targeting cysteine residue in PDI.

View Article and Find Full Text PDF

This study investigated the neuromodulatory potential of zinc against acrylamide-induced cognitive impairment. Acrylamide (AA), a toxic substance commonly found in certain foods such as potato, grains and coffee, is known to cause neurological damage and severe cognitive decline. Twenty (20) male Wistar rats were divided into four groups (n = 5) by random selection.

View Article and Find Full Text PDF

This study aims to develop a series of cation exchange hydrogel resins via gamma irradiation technique through copolymerizing styrene sodium sulfonate with three acrylamide derivatives (designated as poly(X-co-styrene sodium sulfonate), where X refers to acrylamide (PAASS), methacrylamide (PMASS), and isopropyl acrylamide (PIASS)). The prepared hydrogel resins were characterized and tested for the adsorption removal of hard/scale metal cations (e.g.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!