Biomedical subjects

J Büchi

Publications and source records attributed to J Büchi.

4 recordsLinked to original sources

PubMed1979

[Synthesis of several phenoxymethylphenyl derivatives with local-anesthetic activity (author's transl)].

1. Several 4-phenoxymethyl-procaine derivatives (IV) were synthetised in order to investigate the influence of the intermediate chain on the activity. 2. By replacing the CH2-CH2-group in fomocain by a COO-group we succeeded in doubling the efficacy of this local anesthetic. 3. The type and position of the hetero atoms, N,S and O in the intermediate chain of the procaine (I), xylocaine (II), cinchocaine (III) and phenoxymethyl-procaine (IV) series have in each of these series quite a different effect due to the structural specificity of the remaining part of the molecule. 4. Other examples confirm the significance of the ester group in the intermediate chain for the liposolubility and reactivity. In ketones these properties are altered unfavourably.

Anesthetics, Local↗

PubMed1979

[Synthesis of several benzyloxphenyl derivatives with local anesthetic activity (author's transl)].

Several 2- and 4-benzyloxy- and 4-(2'- and 4'-substituted) benzyloxy-beta-substituted amino-propiophenones, some of the corresponding alcohols, some 4-benzyloxy-alpha-substituted amino-acetophenones were synthetised and tested for their pharmacological activity.

Acetophenones↗

PubMed1977

[Investigation of some basic propyl(alkyl)-phenyl ketones with local-anesthetic activity (author's transl)].

We synthetised several ketone analogues of procain (II) with different lipophilic substituents (XVI). In order to investigate structure-activity relationship, the Rm values (measure for the partition coefficient), the -CO- wave frequency (expression of electron density) and the local anesthetic activity (rabbit cornea) were determined. The studied lipophilic substituents do not influence the inductive or mesomeric effect on the carbonyl oxygen and so do not increase its electron density. On the other hand, they do increase the partition coefficient, therefore the hydrophobic binding effect of the substituents is improved. The lower efficacy of the carbonyl group in ketones against the acrboxyl group can be compenstaed for by introduction of groups with higher liposolubility, so that even in ketones it is possible to prepare substances with high local-anesthetic activity.

Anesthetics, Local↗

PubMed1975

[Relationship between the physico-chemical properties, the chemical reactivity and the local anesthetic effect. 32. 2: The binding capacity of structural protein (wool) for local anesthetics].

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Adsorption↗