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AbstractA polarographic method has been developed for the determination of an antidepressant, 10-(m-chlorophenyl)-2,3,4,10-tetrahydropyrimido [1, 2a] indol-10-ol hydrochloride. The method is not subject to interference from the immediate precursor in the synthetic route of drug preparation or the products of thermal degradation of the active drug substance. The method may be used to monitor storage stability studies.

01 Jul 1974·Journal of Medicinal ChemistryQ1 · MEDICINE

Benzamidopiperidines. 2. Heterocyclic compounds related to indoramin

Q1 · MEDICINE

Article

Author: Archibald, John L. ; Benke, Gerald A.

A series of 19 title compounds prepared from 4-benzamidopiperidine [33953-37-6] by alkylation, acylation, Mannich or Michael-type reactions, or ring closure reactions were evaluated for hypotensive activity in anesthetized normotensive rats and antihypertensive activity in conscious renal hypertensive rats.The most active hypotensive compounds were I, R = 2-hydroxy-2-pyrrol-2-ylethyl [36793-50-7] and I, R = 2-(2-quinolyl)ethyl [36793-54-1].The most active antihypertensive compounds were I, R = 2-(4-pyridyl)ethyl [36793-45-0], I, R = 2-(2-pyridyl)ethyl [36806-71-0], I, R = 2-(3-benzo[b]thienyl)ethyl [36793-52-9], and I, R = 2-(3-benz[g]indolyl)ethyl [36806-70-9].None of the compounds were as potent as indoramin [26844-12-2] in either test.I, R = 2-phenothiazin-10-ylethyl [52818-64-1] caused noncompetitive antagonism of histamine in an isolated guinea-pig ileum preparationStructure-activity relations were discussed.

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Pipeline

Pipeline Snapshot as of 23 Jan 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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