Influence of imidazole replacement in different structural classes of histamine H3-receptor antagonists

The mechanism of inactivation of penicillin by cysteine and other mercaptoamines.

The invention provides compounds, compositions, methods, and kits for the treatment of neurogenic inflammation.

Permanently charged sodium and calcium channel blockers as anti-inflammatory agents

2-Mercaptoethylamine and 2-amino-3-mercaptobutane have been condensed with various carbonyl compounds. The structure of 14 of these condensation products has been studied by physical methods (molecular refraction, infrared spectrum, ultraviolet spectrum). In all cases, the products formed were thiazolidines and not Schiff bases; in this respect, the 2-mercaptoamines behave differently from their oxygen isologs.



For comparison, the condensations of N-substituted 2-mercaptoethylamines with various carbonyl compounds have also been studied (22 examples). The thiazolidine ring causes a depression of the molecular refraction and is characterized by a series of infrared bands in the 1000–1380 cm−1 region. Contrary to the experience with N-phenylethanolamine, N-phenyl-2-mercaptoethylamine is capable of condensing not only with aldehydes, but also with ketones.

Reaction products of primary β-hydroxyamines with carbonyl compounds. XIII. Condensation of Primary β-Mercaptoamines with Carbonyl Compounds†

Glucose esters of 4‐ and 5‐aminosalicylic acid were obtainable by reaction of the benzyloxynitrobenzoic acid chlorides with diacetone glucose, followed by catalytic hydrogenation of the nitro groups. Conversion of the amines to hydrochlorides removed one or both of the acetone groups from the glucose. Complete removal of the acetone groups gave a glucose ester that was unstable on standing, but the protected glucose esters were found to be stable. The free‐amino ester of 4‐amino‐salicylic acid was obtained in excellent yield for tuberculostatic and toxicity determinations.

U. J. Salvador

Papers

Derivatives of 4-Amino-2-hydroxybenzoic Acid. II

Sulfur-containing amines; local anesthetics.

Derivatives of 4-Amino-2-hydroxybenzoic Acid. IV. Amides

Dialkylaminoalkyl 4-Alkylaminobenzoates

Derivatives of 4-Amino-2-hydroxybenzoic Acid. III. Thiol Esters