A New Type of 1,4-Benzothiazepine Derivatives

Kinetics and Mechanisms of Hydrolysis of 1,4‐Benzodiazepines I: Chlordiazepoxide and Demoxepam

“…Both bonds undergo heterolysis under appropriate solvolytic conditions, forming a substituted benzophenone product and a glycine derivative (1)(2)(3). This class of nitrogen heterocycles is susceptible to acid-base-catalyzed hydrolysis at two potential sites of scission: the 1,2-amide linkage and the 4,5-azomethine bond.…”

“…where k is the apparent first-order rate constant, ko is the rate constant a t zero ionic strength, Q is the constant equal to 0.55 a t 80' (8), 2, and ZB are the charges of reaction molecules, and p is the ionic strength. The positive slope values close to unity for the plots of log k -4 / ( 1 + 4) (Fig.…”

Structure and Photobiological Activity of 7‐chloro‐1,4‐benzodiazepines. Studies on the Phototoxic Effects of Chlordiazepoxide, Desmethylchlordiazepoxide and Demoxepam Using a Bacterial Indicator System

“…The following compounds were synthesized : demoxepam and diazepam-4-oxide (Sternbach et al, 1960;Bell et al, 1962), desmethylchlordiazepoxide (Sternbach et a/., 1960;1961a). the reduced form of chlordiazepoxide (Sternbach et al, 1961a), of demoxepam (Sternbach et al, 1960;Bell et al, 1962) and of desmethylchlordiazepoxide (Sternbach et al, 1961 b). The oxaziridines were prepared by irradiation of their corresponding nitrones.…”

New synthesis of substituted pyrrolo[1,2-α][1,3]diazepine and its pharmacological activity

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0 A facile route for the synthesis of the substituted pyrrolo[ 1,2-a] [1,3]diazepine nucleus from readily available starting material is reported. The compound was tested for antimalarial activity in mice, antineoplastic activity in mice, acute hypotensive activity in rats and dogs, effect on cholesterol-lipoprotein levels in rats, anti-inflammatory activity in rats, antiviral activity in mice, CNS depressant or stimulant activity in mice, diuretic activity in fasted rats, and antidiabetic activity in rats.

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“…Since the first synthesis of chlordiazepoxide was reported (1,2) and it was shown to possess antianxiety activity (3,4), there has been a tremendous interest in the 1,4-benzodiazepines as potential medicinal agents. In addition to chlordiazepoxide, diazepam (I), oxazepam, and flurazepam have been marketed in the United States for their psychopharmacological properties.…”