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New PNA monomers containing aminoprolines or pyrrolidines as backbones have been synthesized. Oligomerisation was carried out on a solid support. Resistance to enzymatic degradation was tested.
A trisulfide-containing analogue of (arginine 8 )-vasopressin has been synthesized from the corresponding dithiol derivative. Affinities for V1 and V2 receptors were determined. Characterization of the structural differences with the parent hormone was achieved by NMR analysis and a model was...
The synthesis and activities of a series of spiroindane growth hormone secretagogues is reported. Modification of the benzylic position of the spiroindane has resulted in a dramatic increase in potency resulting in subnanomolar peptidomimetic growth hormone secretagogues. In vivo data...
Derivatives of 3- and 1-(4′-hydroxy-3′-(hydroxymethyl)butyl)-imidazo(4,5- b )pyridine were prepared in several steps from 2-amino-5-chloropyridine. Selected compounds were evaluated against human cytomeglovirus (HCMV), herpes simplex virusus (HSV1/HSV2) and varicella zoster virus (VZV)....
The title synthesis was achieved by employing oxidative cyclization of the enaminodiester prepared by Michael addition of the 5-aminoindoline with dimethyl acetylenedicarboxylate, as a key step. Some of these novel bis(methoxycarbonyl)cyclopropapyrroloindole (MC 2 CPI) derivatives 9c , d and...
A Streptomyces galilaeus mutant carrying genes transfered from S. purpurascens is reported to produce two hybrid anthracyclines. This study demonstrates the possibility of producing hybrid anthracyclines in a combinatorial way by genetic engineering of anthracycline producing strains.
The biotransformation of aryltetralin lignans to arylnaphthalene lignans in presence of yeast is described. Podophyllotoxone, an oxidation product of podophyllotoxin on incubation with yeast from different sources produced dehydropodophyllotoxin, an important representative of arylnaphthalene...
The highly efficient preparation of two optically pure phenylalanine analogues containing p -N-aryl thiobenzamide moieties are described. These amino acids are readily incorporated into peptides via standard solid-phase strategies.
An enzymatic synthesis of peptidyl amino alcohols is described. The reactions were performed in organic solvents using as a catalyst subtilisin distributed on the surface of macroporous silica. Subsequent mild oxidation of peptidyl amino alcohols results in peptide aldehydes — the potent...
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