53219-37-7Relevant articles and documents
Neat reaction microwave technology for the synthesis of N-substituted-1,4-dihydropyridines Mazaahir Kidwai and Richa Mohan
Kidwai,Mohan
, p. 427 - 429 (2004)
Hantzsch synthesis of N-substituted-1,4-dihydropyridines (1,4-DHP) was carried out using an environmentally benign procedure. Neat reactants were subjected to microwave irradiation (MWI) to give the required products in excellent yield. Appreciable results were not obtained when conventional synthesis using neat reactants was carried out. The good yield and rate enhancement observed in the case of microwave irradiation is attributed to the uniform heating effect of microwaves.
Discovery of novel enhancers of isoniazid toxicity in mycobacterium tuberculosis
Lentz, Fabian,Reiling, Norbert,Martins, Ana,Molnár, Joseph,Hilgeroth, Andreas
, (2018/04/14)
Abstract: The number of effective first-line antibiotics for the treatment of Mycobacterium tuberculosis infection is strongly limited to a few drugs. Due to emerging resistance against those drugs, second- and third-line antibiotics have been established in therapy with certain problems and also increasing mycobacterial resistance. An alternative to such novel drugs or combined therapeutic regimes which may reduce resistance development is finding enhancers of mycobacterial drug effectiveness, especially enhancers that counteract causative resistance mechanisms. Such enhancers may reduce the extracellular drug efflux mediated by bacterial efflux pumps and thus enhance the intracellular drug toxicity. We developed novel 1,4-dihydropyridines (DHPs) as potential efflux pump inhibitors with some determined P-gp affinities. The influence on the antituberculotic drug toxicity has been investigated for three prominent antituberculotic drugs. Exclusive and selective toxicity enhancing effects have been detected for isoniazid (INH) which could be related to certain substituent effects of the 1,4-DHPs. So, structure-dependent activities have been found. Thus, promising enhancers could be identified and a suggested efflux pump inhibition is discussed.
Novel synthese of heterocycles with N-(1-haloalkyl)azinium halides. Part 5. Preparation of N-substituted 1,4-dihydropyridines
Vanden Eynde,Mayence,Maquestiau,Anders
, p. 3291 - 3304 (2007/10/02)
Thirty N-substituted Hantzsch 1,4-dihydropyridines were prepared under mild and neutral conditions from N-substituted enaminocarbonyl derivatives and aldehydes activated under the form of N-(1-chloroalkyl)pyridinium chlorides by means of thionyl chloride