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Molecules, Volume 22, Issue 3

March 2017 - 163 articles

Cover Story: In the New Medicines for Trypanosomatidic Infections (NMTRypI) project funded by the EU, we have discovered novel anti-leishmania and anti-trypanosoma hits that inhibit pteridine reductase 1 (PTR1). Here, we synthesized compounds with a flavanone scaffold and characterized their antiparasitic activity and ADME-tox properties. Crystal structure determination and computational docking explain differences in their inhibition of PTR1. Two crystal structures of one compound with different PTR1 enzymes provide a basis for further scaffold optimization to develop inhibitors targeting PTR1 enzymes from different parasites. View this paper.
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Articles (163)

  • Review
  • Open Access
65 Citations
11,543 Views
20 Pages

Potential Antivirals: Natural Products Targeting Replication Enzymes of Dengue and Chikungunya Viruses

  • Ana Flávia Costa da Silveira Oliveira,
  • Róbson Ricardo Teixeira,
  • André Silva de Oliveira,
  • Ana Paula Martins de Souza,
  • Milene Lopes da Silva and
  • Sérgio Oliveira de Paula

Dengue virus (DENV) and chikungunya virus (CHIKV) are reemergent arboviruses that are transmitted by mosquitoes of the Aedes genus. During the last several decades, these viruses have been responsible for millions of cases of infection and thousands...

  • Article
  • Open Access
14 Citations
5,195 Views
9 Pages

Carapanosins A–C from Seeds of Andiroba (Carapa guianensis, Meliaceae) and Their Effects on LPS-Activated NO Production

  • Keiichiro Higuchi,
  • Teppei Miyake,
  • Shoko Ohmori,
  • Yoshimi Tani,
  • Katsuhiko Minoura,
  • Takashi Kikuchi,
  • Takeshi Yamada and
  • Reiko Tanaka

Two new phragmalin-type limonoids, Carapanosins A and B (1 and 2), and a new gedunin-type limonoid, Carapansin C (3), together with five known limonoids (4–8) were isolated from the oil of Carapa guianensis AUBLET (Meliaceae) seeds, a traditional med...

  • Article
  • Open Access
53 Citations
9,458 Views
11 Pages

The Anti-Allergic Rhinitis Effect of Traditional Chinese Medicine of Shenqi by Regulating Mast Cell Degranulation and Th1/Th2 Cytokine Balance

  • Yang-Yang Shao,
  • Yi-Ming Zhou,
  • Min Hu,
  • Jin-Ze Li,
  • Cheng-Juan Chen,
  • Yong-Jiang Wang,
  • Xiao-Yun Shi,
  • Wen-Jie Wang and
  • Tian-Tai Zhang

Shenqi is a traditional Chinese polyherbal medicine has been widely used for the treatment of allergic rhinitis (AR). The aim of this study was to investigate the anti-allergic rhinitis activity of Shenqi and explore its underlying molecular mechanis...

  • Article
  • Open Access
10 Citations
5,862 Views
11 Pages

The effects of poly(lactic acid) (PLA)-based film with inorganic antimicrobial nano-TiO2 and nano-Ag on the physicochemical and microbial quality of Tremella aurantialba stored at 4 ± 1 °C for 16 days was investigated. Rosemary essential oil (REO, 9...

  • Article
  • Open Access
15 Citations
5,865 Views
20 Pages

Consecutive One-Pot versus Domino Multicomponent Approaches to 3-(Diarylmethylene)oxindoles

  • Sunhwa Park,
  • Jiyun Lee,
  • Kye Jung Shin,
  • Euichaul Oh and
  • Jae Hong Seo

Based on consecutive one-pot conditions combining three palladium-catalyzed reactions (Sonogashira, Heck and Suzuki-Miyaura reactions), a more efficient domino multicomponent method has been successfully developed to access a wide variety of 3-(diary...

  • Article
  • Open Access
42 Citations
6,693 Views
11 Pages

Synthesis, Characterization, and the Antioxidant Activity of Double Quaternized Chitosan Derivatives

  • Lijie Wei,
  • Qing Li,
  • Wenqiang Tan,
  • Fang Dong,
  • Fang Luan and
  • Zhanyong Guo

With the specialty of improving the water solubility of chitosan, quaternary ammonium salts have broadened the application of this polysaccharide in food, medicine and pesticides. To identify the effect of quaternary ammonium salts’ quantity, single...

  • Article
  • Open Access
7 Citations
4,926 Views
10 Pages

The Effects of Sweet Foods on the Pharmacokinetics of Glycyrrhizic Acid by icELISA

  • Bingqian Jiang,
  • Huihua Qu,
  • Hui Kong,
  • Yue Zhang,
  • Shuchen Liu,
  • Jinjun Cheng,
  • Xin Yan and
  • Yan Zhao

The effect of sweet foods, such as honey, was investigated from the perspective of pharmacokinetics on the absorption of glycyrrhizic acid (GA). Due to the unique properties of indirect competitive enzyme-linked immunosorbent assay (icELISA), namely,...

  • Article
  • Open Access
8 Citations
6,262 Views
13 Pages

Pyragrel, a new anticoagulant drug, is derived from the molecular combination of ligustrazine and ferulic acid. Pyragrel showed significant inhibitory activity against platelet aggregation induced by adenosine diphosphate (ADP), and had been approved...

  • Article
  • Open Access
10 Citations
5,353 Views
15 Pages

3-Substituted N-Benzylpyrazine-2-carboxamide Derivatives: Synthesis, Antimycobacterial and Antibacterial Evaluation

  • Lucia Semelková,
  • Ondřej Janďourek,
  • Klára Konečná,
  • Pavla Paterová,
  • Lucie Navrátilová,
  • František Trejtnar,
  • Vladimír Kubíček,
  • Jiří Kuneš,
  • Martin Doležal and
  • Jan Zitko

A series of substituted N-benzyl-3-chloropyrazine-2-carboxamides were prepared as positional isomers of 5-chloro and 6-chloro derivatives, prepared previously. During the aminolysis of the acyl chloride, the simultaneous substitution of chlorine with...

  • Article
  • Open Access
36 Citations
8,191 Views
14 Pages

Ginsenosides, the major compounds present in ginseng, are known to have numerous physiological and pharmacological effects. The physiological processes, enzymes and genes involved in ginsenoside synthesis in P. ginseng have been well characterized. H...

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Molecules - ISSN 1420-3049