Bioorganic & Medicinal Chemistry
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- Sciencedirect from 1993, Proquest, Rcgp, Ingenta, Gale, and CSA
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB in...
Studies towards the synthesis of indolizin-5(3H)-one derivatives and related 6,5-azabicyclic scaffolds by ring-closing metathesis
Effect of arginine methylation on the RNA recognition and cellular uptake of Tat-derived peptides
Design, synthesis and decoration of molecular scaffolds for exploitation in the production of alkaloid-like libraries
Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: Design, synthesis and 3D-QSAR studies.
We designed and synthesized 33 biphenyl amides based on our previously reported lead compound. The biological results indicated that four compounds (18b, 20e, 20h and 20j) are potent VEGFR-2 inhibitors which are comparable to positive control. Compound 18b displayed the most potent VEGFR-2 inhibitio...
Synthesis of new ligands for targeting the S1P1 receptor.
We developed new agonists for the S1P1 receptor. The biological activity was tested in vivo and promising ligands were fluorinated at different positions to identify candidates for positron emission tomography (PET) imaging after [(18)F]-labelling. The radioligands shall enable the imaging of S1P1 r...
Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity.
A series of phenoxybutanoic acid derivatives were synthesized and tested for their antagonistic activity on the contraction of the rat thoracic aortic ring induced by endothelin-1. Preliminary screening results showed that 6e and 6g with benzoheterocycles demonstrated significant antagonistic activi...
Transformation of naltrexone into mesembrane and investigation of the binding properties of its intermediate derivatives to opioid receptors...
We transformed naltrexone (5) with the morphinan skeleton into mesembrane (4) belonging to the Sceletium alkaloids via key intermediate 6, characterized by a cis-fused hydroindole skeleton with a suspended phenyl ring fixed by an epoxy bridge. We then investigated the binding affinities of 4 and the...
Clofazimine analogs with antileishmanial and antiplasmodial activity
Oseltamivir hydroxamate and acyl sulfonamide derivatives as influenza neuraminidase inhibitors