Relationships between octanol-​water partition data, chromatographic indexes and their dependence on pH in a set of beta-​adrenoceptor blocking agents

A thorough investigation on the dependence of octanol​/water distribution coeffs. (log D) of basic and amphiprotic β-​blocker drugs on pH and pKa values was carried out. An attempt was made to clarify the factors which govern the chromatog. parameters (log k') in reversed-​phase HPLC in terms of chem. structure and of distribution coeffs. The correlations between log D and log k' of different compds. show that the bulkiness and the branching of nitrogen substituent are controlling factors in HPLC measurements. Finally, an ion pair chromatog. system is considered for the prediction of octanol​/water partition coeffs

Synthesis and trazodone-like pharmacological profile of 1- and 2-[3-[4(X)-1-piperazinyl]-propyl]-benzotriazoles

A series of 1- and 2-[3-[4-(X)-1-piperazinyl]-propyl]benzotriazoles were prepared and evaluated for their trazodone-like pharmacological profile; as preliminary pharmacological screening, the compounds were tested for their antiserotonergic, antiadrenergic and antihistamine in vitro activity as well as for their analgesic in vivo action. Structure-activity relationships showed that among the synthesized compounds, the analogues bearing on the 4-piperazine nitrogen either an unsubstituted phenyl ring or a 2- or 3-chloro phenyl moiety show a pharmacological profile similar to that of the antidepressant trazodone