Aug 1, 1976

Clonidine and related analogues. Quantitative correlations

Journal of Medicinal Chemistry
B RouotC G Wermuth

Abstract

Twenty-two structural derivatives of clonidine [2-(2,6-dichlorophenylimino)imidazolidine] have been synthesized and their main physicochemical parameters (log P, deltaRM, pKa) determined. Quantitative correlations between the peripheral alpha-mimetic action (pithed rats) and physicochemical parameters pointed out the critical role of the steric effect in the ortho positions. On the other hand, attempted quantitative correlations between physicochemical parameters and central hypotensive activity were unsuccessful. These results are discussed in the light of the postulated mechanism of action of clonidine.

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Mentioned in this Paper

Derivatives
Structure-Activity Relationship
Diastolic Blood Pressure
Mimetics
Adrenergic alpha-Agonists
Hypotensive
Imidazoles
Physicochemical Phenomena
Isoglaucon
Clonidine

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