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Prooligonucleotides with alternating S-Acyl-ThioEthyl (SATE) phosphotriester and phosphodiester linkages or a gap were synthesized by elimination of cyanoethyl group with non-nucleophilic base DBU. Their half-lives in the presence of Pig Liver Esterases (PLE) and in total cell extract were...
Steroidal derivatives as IL-1β release inhibitors are discussed.
A short and efficient synthesis of novel benzo(c)quinolizin-3-one derivatives is described. The synthesis is based on the tandem Mannich-Michael cyclization between 2-silyloxy-1,3-butadienes and a N - t -Boc iminium ion. The prepared derivatives are selective inhibitors of human steroid...
In the photoprotein of an Okinawan squid bioluminescence of Symplectoteuthis oualaniensis L a dehydrocoelenterazine has been assigned as a chromophoric precursor to its apoprotein. To prove this mechanism, we have established new synthetic route to ca. 100 %- 13 C incorporated...
Starting from a series of 2-aminotetralins 1 , a novel series of N-(4-(4-phenylbenzoylamino)butyl)-octahydrobenzoquinolines and hexahydrobenzoindoles with high potency and selectivity for the dopamine D 3 receptor has been designed. The effect of ligand chirality on binding affinity has been...
Electroenzymatic reduction of NAD + to NADH for subsequent use in enzymatic synthesis has been carried out at carbon electrodes bearing lipoamide dehydrogenase (LiDH) immobilized under a Nafion R film. The self-mediated electron transfer was made possible by an excess of flavin adenine...
Starting from ( S )- and ( R )-aspartic acid enantiomerically pure β-proline derivatives were synthesized. These chiral building blocks were transformed into β-analogs of the dopamine receptor modulating peptide PLG. According to dopamine receptor binding studies, significant enhancement of ( 3...
Several kinds of naturally occurring fernane-type triterpenoids isolated from a Euphorbia genus were tested on the inhibitory effects of DNA Topoisomerases I (Topo I) and II (Topo II) activities. A-ring cleaved 3,4- sero -8 βH -ferna-4(23),9(11)-dien-3-oic acid and its 3-hydroxyl derivative were...
During development of nitroheterocycles with potential antimycobacterial activities we have tested against Mycobacterium tuberculosis a number of pyrroles strictly related to pyrrolnitrin, an antifungal antibiotic isolated from Streptomyces pyrrocinia . Some of the tested arylpyrrole derivatives...
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