4-(5,6-Dimethoxy-1-oxo-isoindoline) and 4-Acetamido-Substituted Phenoxy-3-amino-propane Derivatives andTheir β 1 -, β 2 -Adrenergic Receptor Binding Studies. -The β-adrenoceptor binding affinity and selectivity of the synthesized compounds (V) are tested. All the tested compounds (V) exhibit better cardioselectivity than the standard cardioselective β-blocker atenolol. -(JINDAL, D. P.; SINGH, B.; SHARMA, N.; COUMAR*, M. S.; BRUNI, G.; MASSARELLI, P.; Indian J.
The synthesis of 2-substituted-N-(2-diethylaminoethyl)acetamide oxalates (6a, 6b) and the evaluation of their in vivo local anaesthetic activities are described. The compounds 6a and 6b were obtained starting from 4-acetamidophenol and 1-naphthol, respectively. The in vivo local anesthetic activity was evaluated by infiltration anaesthesia, sciatic nerve block and corneal anaesthesia models. N-(2-Diethylaminoethyl)-2-(naphthalen-1-yloxy)acetamide oxalate (6b) was found to have potency, onset and duration of action comparable to that of lidocaine (2) (lidocaine hydrochloride, CAS 6108-05-0). Procaine (1) (procaine hydrochloride, CAS 51-05-8) was also used for comparison. Dissociation constants (pKa) of compounds 5a and 5b (2-substituted-N-(2-diethylaminoethyl)acetamide) have been determined to be 8.9 and 8.6, respectively.
2‐Mercapto‐3‐phenylchinazolin‐4(3H)‐on (I) läßt sich mit den Phenacylbromiden (II) in Gegenwart von Alkali in guten Ausbeuten zu den Chinazolinon‐Derivaten (III) umsetzen, deren NaBH4‐Reduktion die Dihydrochinazolinone (IV) ergibt, die sich mit Essigsäureanhydrid/p‐Toluolsulfonsäure zu den Thiazolido(3,2‐a)chinazolinonen (V) cyclodehydratisieren lassen.
111 uas Brommethylchinazolinon (I) glDI mit (ICH l′! atnumsaizen VO? ACCIYIEICCIOII, Diäthylmalonat und Acetessigester die Kondensationsprodukte (II), (III) und (IV).
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