[EN] HYDRAZIDE DERIVATIVES AND THEIR SPECIFIC USE AS ANTIBACTERIAL AGENTS BY CONTROLLING ACINETOBACTER BAUMANNII BACTERIUM<br/>[FR] DÉRIVÉS D'HYDRAZIDE ET LEUR UTILISATION SPÉCIFIQUE EN TANT QU'AGENTS ANTIBACTÉRIENS POUR LUTTER CONTRE UNE BACTÉRIE ACINETOBACTER BAUMANNII
申请人:YNCREA HAUTS DE FRANCE
公开号:WO2020169682A1
公开(公告)日:2020-08-27
The present invention relates to compounds of the following general formula (I): or a pharmaceutically acceptable salt and/or solvate thereof, their use as a drug, in particular as antibacterial agent, notablyforpreventingand/or treating disorders associated to Acinetobacter baumannii. The present invention also relates to pharmaceutical compositions containing said compoundsand the process for preparing said compounds.
An iodine-promoted, metal-, base-, and solvent-free cross-couplingreaction was developed for the synthesis of various useful secondary amides via an aryl N-addition reaction of aryl groups to cyano groups. This aryl transfer reaction proceeds with arylhydrazine hydrochlorides serving as the aryl donors. A labelling experiment shows that the N atom in the product comes from the cyano group of the nitriles
A compound of the following formula or a pharmacologically acceptable salt thereof:
1
wherein A represents a phenyl group or the like, B represents an aryl group or the like, X represents an oxygen atom or the like, and n represents 0 or 1. The compound is a PPAR &ggr; modulator which is a therapeutic agent for retrograde osteoporosis in which excessive differentiation of adipocytes is inhibited and formation and differentiation of osteoblasts from stem cells is facilitated, and for diabetes mellitus without characteristics such as excessive adipogenesis, liver dysfunction, vascular disorders, heart diseases and the like.
An Efficient Synthesis of Sulfonylhydrazides and Sulfonylsemicarbazides by Utilizing Alumina as a Catalyst
作者:Javad Safaei-Ghomi
DOI:10.1002/jccs.200700220
日期:2007.12
Sulfonyl hydrazides and sulfonyl semicarbazides are readily prepared by the reacting of hydrazine derivatives with sulfonyl chlorides in the presence of basic alumina under solvent-free conditions. Reaction of a sulfonyl chloride with t-butylcarbazate, followed by hydrolysis provides the corresponding sulfonyl hydrazides in higher yield and shorter time than previously reported.
Reactivities of mono and difunctional thiosulfonates toward several nucleophilic compounds, such as thiols, amines and the related compounds, were examined. In the result, some chemical behaviors unexpected were found in addition to the reactivity anticipated. Namely, in the reaction with piperazine, aralkyl thiosulfonate afforded aralkyltrisulfide in about 20% yield, without any formation of sulfenamide. Moreover, aromatic thiosulfonate gave a comparable good yield of 1-phenyl-2-arylsulfonylhydrazine in the reaction with phenylhydrazine, in addition to the formation of phenylhydrazinium salt of aromatic sulfinic acid.