MOHANE COUMAR S.
M. Pharm.
UNIVERSITY INSTITUTE OF PHARMACEUTICAL SCIENCES
PANJAB UNIVERSITY, CHANDIGARH, INDIA
THESIS
SUBMITTED FOR THE AWARD OF THE DEGREE OF
DOCTOR OF PHILOSOPHY
OF THE PANJAB UNIVERSITY, CHANDIGARH
(FACULTY OF PHARMACEUTICAL SCIENCES)
2001
Thou art everywhere, but I worship thee here;
Thou art without form, but I worship thee in these forms;
Thou needest no praise, yet I offer thee these prayers and salutations.
Lord, forgive three sins that are due to my human limitations.
- M.M Kaye
ACKNOWLEDGEMENTS
INTRODUCTION ------------------------------------------------------------1
ARYLETHANOLAMINE DERIVATIVES
ARYLOXYPROPANOLAMINE DERIVATIVES
STRUCTURE-ACTIVITY RELATIONSHIPS
THERAPEUTIC USES OF beta-ADRENERGIC BLOCKING AGENTS
ADVERSE EFFECTS OF beta-ADRENERGIC BLOCKING AGENTS AND PRECAUTIONS
RESEARCH ENVISAGED -----------------------------------------------87
RESUM� AND DISCUSSION ------------------------------------------88
EXPERIMENTAL WORK ----------------------------------------------127
SYNTHESIS
VANILLIN-DERIVED ARYLOXYPROPANOLAMINES ----------------------127
THYMOL-DERIVED ARYLOXYPROPANOLAMINES -----------------------147
4-AMINOPHENOL-DERIVED ARYLOXYPROPANOLAMINES ------------151
3,4-Dimethoxybenzamide series
3,4,5-Trimethoxybenzamide series
5-AMINO-1-NAPHTHOL-DERIVED ARYLOXYPROPANOLAMINES
Acetamide series
3,4-Dimethoxybenzamide series
MISCELLANEOUS COMPOUNDS
PHARMACOLOGICAL TESTING ---------------------------------------------179
beta-ADRENOCEPTOR BINDING ASSAY
beta-ADRENOCEPTOR BLOCKING ACTIVITY
LOCAL ANAESTHETIC ACTIVITY
DETERMINATION OF PARTITION COEFFICIENT ------------------------185
REFERENCES ------------------------------------------------------------187