Histamine Antagonists. II.¹ Unsymmetrical 1,4-Disubstituted Piperazines

Thiophene Compounds of Biological Interest

“…When equal doses of the drugs were administered, chlorothenylpyramine protected against histamine shock twice as long as tripelennamine (01). Thiophene isosteres of other well established antihistamine drugs have also been prepared (50,58,(62)(63)(64)(65)(66). However, the thiophene compounds have not shown marked superiority as antihistamines to compounds of…”

Relative Rates of Migration of Aryl Groups in the Schmidt Reaction of Benzhydrols1

“…'s are 60°,12 59-60°,22 66-68°23 and 68°. 23 Schmidt Reaction of « -Chlorobenzhydrol. (a) Normal Procedure.-A 500-ml., 3-necked flask rvas equipped with a dropping funnel, a mercury sealed stirrer and a reflux condenser, to the top of which was attached in series a safety bottle and a bubbler filled with sodium hydroxide solution.…”

Efficient synthesis of antihistamines clocinizine and chlorcyclizine

“…Antihistamine drugs are commonly used for relief of allergies caused by intolerances of proteins. The clocinizine (1) (Wright and Martins, 1968) and chlorcyclizine (2) (Hamlin et al, 1949, Albro et al, 1949, Sengmany et al, 2007 are the first generation antihistamine agents belong to diaryl piperazine group (Fig. 1).…”