Biological activities and receptor affinities of some natural and synthetic oestrogens and their D-homo analogues

1978 ◽  
Vol 34 (10) ◽  
pp. 1373-1374 ◽  
Author(s):  
W. Lotz
2018 ◽  
Vol 24 (10) ◽  
pp. 1100-1120 ◽  
Author(s):  
Sarah Line Skovbakke ◽  
Andre Holdfeldt ◽  
Huamei Forsman ◽  
Johan Bylund ◽  
Henrik Franzyk

In recent years, the therapeutic potential of antimicrobial peptides (AMPs) as immunomodulators has become generally accepted. Nevertheless, only very few AMP-based compounds have progressed into clinical trials. This paradox may be explained by the fact, that some of the intrinsic properties of natural peptides, such as proteolytic and oxidative instability, render them inconvenient as therapeutics. Therefore, substantial research efforts have been dedicated to mimic the physico-chemical properties as well as biological activities of AMPs by designing and identifying more stable peptidomimetics displaying analogous immunomodulatory activity profiles. Neutrophils play key roles in host defense as major effector cells in clearance of pathogens by phagocytosis and by regulating other processes of innate immunity as well as by promoting resolution of inflammation. Several aspects of these effects are correlated to their expression of formyl peptide receptors (FPRs) that have been shown to be targets of both natural and synthetic antimicrobial peptides. In the present review recent findings highlighting the role of FPRs in mediating immunomodulatory activities of natural and synthetic AMPs as well as of stabilized peptidomimetics are discussed, and prospects for future development of immunomodulatory therapeutics are presented.


2011 ◽  
Vol 63 (2) ◽  
pp. 305-336 ◽  
Author(s):  
Grzegorz Cholewiński ◽  
Krystyna Dzierzbicka ◽  
Aleksander M. Kołodziejczyk

Author(s):  
Guilherme Arraché Gonçalves ◽  
Hugo Cerecetto ◽  
Gilsane Lino von Poser ◽  
Rômulo Faria Santos Canto ◽  
Vera Lucia Eifler-Lima

The complexity of Chagas disease is still a challenge in endemic regions and an emergent public health problem in non-endemic countries. The causative agent of this neglected tropical disease, Trypanosoma cruzi, is mainly transmitted by triatomine vectors and possesses multiple epidemiologically important strains. Current chemotherapeutics are outdated and their limited efficacy is one of the major reasons for treatment discontinuation. In this context, it is urgent the development of novel, safe and economically accessible antichagasic drugs. Various classes of heterocycles and natural compounds have been described as potential antichagasic scaffolds, and coumarins are no exception. These versatile compounds have a wide spectrum of biological activities, and numerous natural and synthetic coumarins have been reported with antichagasic potential. The aim of this review is to discuss the available literature between 2001 and 2020 regarding natural and synthetic coumarins with anti-Trypanosoma cruzi activity. Moreover, some of the studies herein comprised are dedicated to the potential of coumarins to inhibit promising targets in Trypanosoma cruzi.


2020 ◽  
Vol 32 (5) ◽  
pp. 1255-1258
Author(s):  
Nakul Kumar ◽  
Chhagan Lal ◽  
Bijendra Singh ◽  
Angik K. Patel

The synthesis of spiropyrrolidines by the Knoevenagel condensation has been reported as highly bioactive natural and synthetic organic products. The synthesis was initiated by Knoevenagel condensation of indole-2-one with an appropriate benzaldehyde in presence of L-proline to afford spiropyrrolidines. Herein, a design and pathway of syntheses of a library of spiropyrrolidines bearing spiro heterocyclic indeno[1,2-b]quinoxaline-11-one motifs were reported, which also demonstrated an exceptional inhibitory activity against the anticancer cells. A novel series of dispiroindenoquinoxaline pyrrolizidines were synthesized by the condensation of indeno[1,2-b]quinoxalin-11-one and starting material (a product of ninhydrin and aldehyde derivatives). The structure of the synthesized compounds was established by spectral data.


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