Hydrophobic constants and quantitative structure activity relationships (QSAR) in sets of phenothiazine drugs was written by Barbato, Francesco;Recanatini, Maurizio;Silippo, Carlo;Vittoria, Antonio. And the article was included in European Journal of Medicinal Chemistry in 1982.Category: piperazines This article mentions the following:
Octanol/water partition coefficients of a large set of phenothiazine drugs I [R = Me2N(CH2)3, CH2CHMeNMe2, CH2CHMeCH2NMe2, etc.; R1 = H, Cl, CN, Me, CF3, etc.] were determined and related to the corresponding high-performance liquid chromatog. capacity factors. The bovine serum albumin binding affinity and antihemolytic activity of sets of congeners are discussed from the quant. structure-activity point of view. Results show that both activities are largely affected by the degree of hydrophobicity of the mols. as measured by the log P apparent values, while other factors play only a minor role. Moreover, in vivo data are considered to uncover quant. correlations between structural features and neuroleptic biol. activities. Correlation equations show that the major factor influencing the considered activities is a particular electronic demand of the phenothiazine side chain, while 2-R1-substituents may enhance the activity either affecting the side chain conformation or directly interacting at receptor site. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Category: piperazines).
N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics