摘要:

AbstractA series of fused 5,5‐diphenyl and 5‐arylidene‐2‐thiohydantoin derivatives were examined for their oxygen free radical inhibitory and radical scavenging properties (RSC) using both an enzymic and non‐enzymic biological generators of free radicals. Non‐enzymic lipid peroxidation (OH radicals) was assayed as the amount of malondialdehyde (MDA) that had been formed during incubation of boiled rat liver microsomes in the presence of ascorbic acid and ferric ions. Superoxide anions (02−anion radicals) were generated enzymatically in the xanthine‐xanthine oxidase system. Among the 20 investigated compounds only four fused arylidene 2‐thiohydantoin derivatives showed weak antioxidant activity scavenging OH radicals. There is a relationship between the electrophilic OH radical scavenging properties (RSC) of the tested molecules and the value of their HOMO energy derived from semiempirica

ISSN:0365-6233    

DOI:10.1002/ardp.19973300402

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractIn a search for new anticonvulsants, two series of compounds, viz. derivatives ofN‐benzylamides of α‐(4‐phenylpiperazine)‐γ‐hydroxybutyric acid (Aand derivatives ofN‐benzylamides of α‐(4‐benzylpiperazine)‐γ‐hydroxybutyric acid (B), were investigated. These amides were obtained by aminolysis of 3‐(4‐phenyl‐, or 4‐benzylpiperazine)‐tetrahydrofuran‐2‐one with primary arylalkylamines (i.e. 2‐phenylethylamine and 2,3,4‐substituted derivatives of benzylamine). Preliminary pharmacological tests, a maximal electroshock (MES) and a subcutaneous metrazole (scMet), and a rotorod toxicity assay were employed. All compounds displayed anticonvulsant activity at range of doses 100–300 mg/kg in the MES screens. In order to point to some structural features correlating with the MES anticonvulsant activity crystal structure analysis followed by conformational analysis was carried out on

ISSN:0365-6233    

DOI:10.1002/ardp.19973300403

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

Abstract6‐[(4‐Quinolinyl)oxy]hexanoic acids and the corresponding esters were designed and synthesized as inhibitors of the production of arachidonic acid metabolites. The inhibitory activities were assayedin vitroby evaluation of serum leukotriene B4and thromboxane B2production. While all 6‐[(4‐quinolinyl)oxy]hexanoic acids and their esters proved to be inactive, theN‐alkyl‐4‐quinolones, obtained as by‐products in their synthesis, were found to be a new class of leukotriene biosynth

ISSN:0365-6233    

DOI:10.1002/ardp.19973300404

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractBenzothiophene compounds3aand3b, structurally similar to propafenone (1), are described.

ISSN:0365-6233    

DOI:10.1002/ardp.19973300405

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractPeptides from small combinatorial libraries, covalently attached to polymeric TentaGel beads, can be directly sequenced using amino acid analysis. For libraries with restricted diversity, generated by the split‐mix synthesis method, the amino acids on a selected single bead identified by pre‐column derivatization witho‐phthaldialdehyde (OPA) correlate directly with the sequence of a given peptide. This is shown on a tripeptide (343 different compounds) and a tetrapeptide (4096 different compounds) library. This method allows for rapid peptide sequence determination without relying on complex encoding strat

ISSN:0365-6233    

DOI:10.1002/ardp.19973300406

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractThe synthesis and odour properties of the new santalol analogue, methyl‐β‐santalol, are described. The additional methyl group adjacent to the hydroxyl function of the standard molecule, β‐santalol, deprives the new compound of the sandalwood note. The synthesis and the odour evaluation of this compound supports the proposed model for sandalwood fragrance as it shows that the methyl group located at the osmophoric center prevents association of the molecule with the hypothetical r

ISSN:0365-6233    

DOI:10.1002/ardp.19973300407

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

ISSN:0365-6233    

DOI:10.1002/ardp.19973300408

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

ISSN:0365-6233    

DOI:10.1002/ardp.19973300401

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY