Adrenergic Activators and Inhibitors: Part I - download pdf or read online

By D. K. Phillips (auth.), Professor Dr. Lászlo Szekeres (eds.)

ISBN-10: 3642675050

ISBN-13: 9783642675058

ISBN-10: 3642675077

ISBN-13: 9783642675072

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CX ~ I CH2CH=CH2 OCH 2CHCH 2NHCH(CH 3h I OH (90) (91 ) 2. , 1969) (see Sect. B. 1). -butyl (CROWTHER and SMITH, 1968). , isobutyl, led to a decrease in activity. Hydroxyl substituents caused no great loss of activity, but alkoxy and amino substituents did. Arylalkylamino groups, particularly those with an alkyl rx substituent, were very active, which suggested significant receptor interaction. , 1976). , 1977), and the acylaminoalkylamines (95) (SMITH, 1974, 1976a, b). The dimethoxyphenylethyl side chain ofCI-775 appeared to confer greater CH 3 ~1I'b:CII'NHCH,cII,o-O-CONII' (93) ~ OCH2CHCH2NHCH2CH2NHR oI OH (95) (94) R = -COR', -CONHR', -S02NHR' cardioselectivity to a number of antagonists when it was substituted for isopropyl.

On the basis of their pharmacological findings and the results of nuclear magnetic resonance spectroscopic studies, JEN and KAISER (1977) proposed that the side chains of the protonated species of aryloxypropanolamines in chloroform solution existed in a bicyclic "rigid" conformation (63) involving two intramolecular hydrogen bonds. , 1968); and the methylene (HOWE, 1970) isosteric analogs of propranolol. , 1975), which are capable of double intramolecular hydrogen bonding, have significant adrenergic activity.

The tert-butyl-amino analog (C-78) (39 a) of clorprenaline, was reported to be orally active and more potent. , 1975). K. , 1977). These metabolites may participate in the activity and duration of the action of C-78. R2 Cl rl CHCH2NHCH(CH h Lli OH RI 3 (38) Cl H CHCH 2NHC(CH h -«J-I OH 3 (39) a: RI = R2= H b: RI = OH; R2 = H c: RI = H; R2 = OH KECK and co-workers (1972) examined a large number of halogen-substituted aminophenylethanolamines for adrenergic properties and found compounds with exand p-stimulant and blocking properties, as well as analgesic substances.

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Adrenergic Activators and Inhibitors: Part I by D. K. Phillips (auth.), Professor Dr. Lászlo Szekeres (eds.)


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