Design, synthesis and evaluation of racemic 1-(4-hydroxyphenyl)-2-[3- (substituted phenoxy)-2-hydroxy-1-propyl]amino-1-propanol hydrochlorides as novel uterine relaxants

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 15, 2005, Pages 3532-3535

  Viswanathan, C L ^a   Kodgule, M M ^a   Chaudhari, A S ^a  

^a BOMBAY COLLEGE OF PHARMACY   (India)

Author keywords

2 Adrenoceptor stimulants; cAMP 3H assay; Uterine relaxants

Indexed keywords

BUPHENINE; CYCLIC AMP; ISOXSUPRINE; MUSCLE RELAXANT AGENT; PROPANOL DERIVATIVE; RITODRINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; LABOR; NONHUMAN; PHARMACOPHORE; RAT; SMOOTH MUSCLE RELAXATION; STRUCTURE ANALYSIS; TISSUE HOMOGENATE; UTERUS CAVITY; UTERUS RELAXATION;

1-PROPANOL; ANIMALS; CARDIOTONIC AGENTS; CYCLIC AMP; DRUG DESIGN; FEMALE; ISOXSUPRINE; MUSCLE RELAXATION; PREGNANCY; RATS; UTERUS;

CAVIA PORCELLUS;

EID: 21744445060     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.05.047     Document Type: Article

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10. Black J. W.; Duncan W. A. M.; Shanks R. G. Br. J. Pharmacol. 1965, 25, 577. The atrium was mounted in a jacketed organ bath filled with Ringer-Locke solution under a resting tension of 1 g. Carbogen gas was bubbled and the temperature was maintained at 37°C and the tissue was allowed to equilibrate for 45 min. Ten micromole of isoproterenol sulfate (ISP, Ref. Std) was added to the organ bath and the heart rate was recorded using a force transducer on a polygraph. Compounds 9a-d at doses of 10, 25, 50 and 100 μmol were added to the bath and incubated for 3 min, then 1 μmol ISP was added and the heart rate was recorded (Table 3). In a similar manner isoxsuprine hydrochloride was evaluated at 0.5, 0.75, 1.0 and 1.25 μmol doses