Amidoxime Derivatives with Local Anesthetic, Antitubercular, and Antidiabetic Activity

Abstract

Оur task in the field of new derivatives of amidoximes was the elaboration for new medication with increased activity and lower toxicity than medications used in practice. Here are the results of the search for new painkillers and antitubercular and antidiabetic drugs in the class of amidoxime derivatives. Nitrous derivatives of α-chloro-α-isonitrosoacetone, O-aroyl-β-aminopropioamidoximes, and 3-[β-(piperidine-1-yl)]ethyl-5-aryl-1,2,4-oxadiazoles were tested for conduction, infiltration, and terminal anesthesia. Among them hit compounds were discovered. The search for new anti-TB drugs is executed in the world. Salts and bases of O-aroylation products of β-(thiomorpholin-1-yl) and β-(4-methylpiperazin-1-yl) propioamidoximes during in vitro antitubercular screening for DS, DR, and MDR strains of M. tuberculosis manifest themselves as highly active competitive compounds. In the series of the derivatives of β-aminopropioamidoximes, a search for new antidiabetic drugs was done. The compounds with pronounced antidiabetic properties were revealed. The obtained data of the most promising samples with a preliminary assessment of their average toxic dose in animals can be used in further in vivo testing of infiltration anesthesia conditions, of antidiabetic properties, and at the development of doses and new treatment regimens for TB.

Boulton-Katritzky Rearrangement of 5-Substituted Phenyl-3-[2-(morpholin-1-yl)ethyl]-1,2,4-oxadiazoles as a Synthetic Path to Spiropyrazoline Benzoates and Chloride with Antitubercular Properties

“…The practical interest in the class of β-aminopropioamidoxime derivatives is supported by their pronounced local anesthetic, antitubercular, and antidiabetic activities [ 13 , 14 , 15 , 16 ].…”

“…In addition, spiropyrazolinium structures-2-amino-8-oxa-1,5-diazaspiro[4.5]dec-1-ene-5-ammonium arylsulfonates are formed at arylsulfochlorination of β-aminopropioamidoximes (Scheme 4) [12]. The practical interest in the class of β-aminopropioamidoxime derivatives is supported by their pronounced local anesthetic, antitubercular, and antidiabetic activities [13][14][15][16].…”