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Cyclic peptides can bind to protein targets with high affinities and selectivities, which makes them an attractive modality for the development of research reagents and therapeutics. Additional properties, including low inherent toxicity, efficient chemica ...
An antimicrobial activity screen of Burkholderia gladioli BCC0238, a clinical isolate from a cystic fibrosis patient, led to the discovery of gladiolin, a novel macrolide antibiotic with potent activity against Mycobacterium tuberculosis H37Rv. Gladiolin i ...
Due to the spongistatins' fascinating and complex molecular architectures, and their important biological activities, these marine macrolides have been the subject of intensive efforts directed towards their total synthesis. As an attractive alternative to ...
The first Ni-catalyzed Suzuki-Miyaura coupling of alkyl halides with alkenyl-(9-BBN) reagents is reported. Both primary and secondary alkyl halides including alkyl chlorides can be coupled. The coupling method can be combined with hydroboration of terminal ...
Polyketides show interesting biological activities and therefore represent an important class of natural products. The necessity of their diastereo- and enantioselective synthesis led to the development of numerous methodologies. A brief overview of this t ...
Using readily available chiral auxiliaries such as (+)- and (-)-camphanic acid, (R,R)- and (S,S)-tartaric acid derivatives (e.g. RADO(R)-COCl, SADO(R)-COCl) efficient diastereoselective syntheses of rare sugars and glycomimetics have been developed. They e ...
Polypropionates are common products of metabolism in bacteria, insects, fungi and marine organisms. They constitute an important class of products with a wide range of interesting biological activities. Our group has shown previously that 1-alkoxy-3-acylox ...
New pathways toward the synthesis of polyketide-like macrolides have been developed through the functionalization of long chain polyolic fragments readily obtained from 3,3'-methylenebis{[6-(benzyloxy)methoxy]cyclohept-3-en-1-ol} derivatives 6. This synthe ...
The ionotropic GABA(A) receptors represent the main target for different groups of widely used drugs having hypnotic and anxiolytic effects. So far, most approaches used to assess GABA activity involve invasive low -throughput electrophysiological techniqu ...
During the last two decades, marine organisms such as sponges, tunicates, softcoral and starfish proved to be productive sources of structurally complex metabolites presenting unprecedented architectures.[1] These marine natural products often display unex ...
