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Molecules, Volume 25, Issue 9

May-1 2020 - 263 articles

Cover Story: The discovery of novel GSK-3β inhibitors to hinder central disorders is highly needed. 1H-Indazole-3-carboxamide (INDZ) derivatives were previously reported as potent GSK-3β inhibitors. However, they suffer from poor brain penetration. Here, a computer-aided scaffold-hopping strategy was conceived leading to novel imidazo[1,5-a]pyridine-1-carboxamide (IMID 1) and imidazo[1,5-a]pyridine-3-carboxamide (IMID 2) compounds with ameliorated permeability, but slightly reduced GSK-3β potency with respect to the INDZ analogs. In order to rationalize the observed structure–activity relationship, retrospective in silico studies and NMR investigation were carried out, highlighting the key role of the acidic hydrogen of the central core for GSK-3β affinity. View this paper.
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Articles (263)

  • Article
  • Open Access
48 Citations
5,372 Views
15 Pages

Three new tetradentate NNNS Schiff bases (L1–L3) derived from 2-(piperidin-4-yl)ethanamine were prepared in high yields. UV–Visible and FTIR spectroscopy were used to monitor the dehydration reaction between 2-(piperidin-4-yl)ethanamine a...

  • Article
  • Open Access
14 Citations
4,479 Views
16 Pages

Wide-Antimicrobial Spectrum of Picolinium Salts

  • Sarka Salajkova,
  • Marketa Benkova,
  • Jan Marek,
  • Radek Sleha,
  • Lukas Prchal,
  • David Malinak,
  • Rafael Dolezal,
  • Kristina Sepčić,
  • Nina Gunde-Cimerman and
  • Kamil Kuca
  • + 1 author

Nosocomial infections, which greatly increase morbidity among hospitalized patients, together with growing antibiotic resistance still encourage many researchers to search for novel antimicrobial compounds. Picolinium salts with different lengths of...

  • Article
  • Open Access
25 Citations
5,681 Views
17 Pages

A Herbal Mixture from Propolis, Pomegranate, and Grape Pomace Endowed with Anti-Inflammatory Activity in an In Vivo Rheumatoid Arthritis Model

  • Valentina Parisi,
  • Antonio Vassallo,
  • Claudio Pisano,
  • Giacomo Signorino,
  • Francesco Cardile,
  • Milena Sorrentino,
  • Fabiana Colelli,
  • Alessandra Fucci,
  • Egildo Luca D’Andrea and
  • Nunziatina De Tommasi
  • + 2 authors

Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease characterized by the production of inflammatory factors. In order to overcome the side effects of currently used anti-inflammatory drugs, several attempts have been made to identi...

  • Article
  • Open Access
14 Citations
4,992 Views
29 Pages

The Antiproliferative Effects of Flavonoid MAO Inhibitors on Prostate Cancer Cells

  • Najla O. Zarmouh,
  • Samia S. Messeha,
  • Nelly Mateeva,
  • Madhavi Gangapuram,
  • Kacy Flowers,
  • Suresh V. K. Eyunni,
  • Wang Zhang,
  • Kinfe K. Redda and
  • Karam F. A. Soliman

Prostate cancer (PCa) patients commonly experience clinical depression. Recent reports indicated that monoamine oxidase-A (MAO-A) levels elevate in PCa, and antidepressant MAO-Is show anti-PCa properties. In this work, we aimed to find potential drug...

  • Feature Paper
  • Article
  • Open Access
18 Citations
4,319 Views
24 Pages

Search for ABCB1 Modulators Among 2-Amine-5-Arylideneimidazolones as a New Perspective to Overcome Cancer Multidrug Resistance

  • Aneta Kaczor,
  • Márta Nové,
  • Annamária Kincses,
  • Gabriella Spengler,
  • Ewa Szymańska,
  • Gniewomir Latacz and
  • Jadwiga Handzlik

Multidrug resistance (MDR) is a severe problem in the treatment of cancer with overexpression of glycoprotein P (Pgp, ABCB1) as a reason for chemotherapy failure. A series of 14 novel 5-arylideneimidazolone derivatives containing the morpholine moiet...

  • Article
  • Open Access
9 Citations
3,798 Views
11 Pages

Bamboo-plastic composites (BPCs) as new biomass-plastic composites have recently attracted much attention. However, weak mechanical performance and high moisture absorption as well as low thermal stability greatly limit their industrial applications....

  • Article
  • Open Access
13 Citations
4,634 Views
14 Pages

Exploring Structure-Property Relationships in a Bio-Inspired Family of Bipodal and Electronically-Coupled Bistriphenylamine Dyes for Dye-Sensitized Solar Cell Applications

  • Tamara Al-Faouri,
  • Francis L. Buguis,
  • Saba Azizi Soldouz,
  • Olga V. Sarycheva,
  • Burhan A. Hussein,
  • Reeda Mahmood and
  • Bryan D. Koivisto

A bio-inspired family of organic dyes with bichromic-bipodal architectures were synthesized and tested in dye-sensitized solar cells (DSSC). These dyes are comprised of a D-π-D-A motif with two triphenylamine (TPA) units acting as donors (D) and t...

  • Article
  • Open Access
10 Citations
3,882 Views
9 Pages

Differences in the aroma profiles of extruded maize puffs made from refined grain and whole grain flour were investigated. Gas chromatography/mass spectrometry/olfactometry (GC/MS/O) analysis reported 13 aroma compounds with a flavor dilution (FD) va...

  • Article
  • Open Access
17 Citations
4,921 Views
22 Pages

American ginseng, Panax quinquefolium (L.), is traditionally used in folk medicine. It exhibits a range of anti-inflammatory, hepatoprotective, anti-diabetic, anti-obesity, anti-hyperlipidemic and anti-carcinogenic effects. Its main components are gi...

  • Article
  • Open Access
32 Citations
5,064 Views
23 Pages

Surface Modification of Magnetic Nanoparticles by Carbon-Coating Can Increase Its Biosafety: Evidences from Biochemical and Neurobehavioral Tests in Zebrafish

  • Nemi Malhotra,
  • Gilbert Audira,
  • Jung-Ren Chen,
  • Petrus Siregar,
  • Hua-Shu Hsu,
  • Jiann-Shing Lee,
  • Tzong-Rong Ger and
  • Chung-Der Hsiao

Recently, magnetic nanoparticles (MNPs) have gained much attention in the field of biomedical engineering for therapeutic as well as diagnostic purposes. Carbon magnetic nanoparticles (C-MNPs) are a class of MNPs categorized as organic nanoparticles....

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Molecules - ISSN 1420-3049