122368-54-1Relevant articles and documents
Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials
Anusha, Sebastian,Sinha, Ameya,Babu Rajeev,Chu, Trang T. T.,Mathai, Jessin,Ximei, Huang,Fuchs, Julian E.,Shivananju, Nanjundaswamy,Bender, Andreas,Preiser, Peter Rainer,Rangappa, Kanchugarakoppal S.,Basappa,Chandramohanadas, Rajesh
, p. 10681 - 10690 (2015)
Malaria parasites are currently gaining drug-resistance rapidly, across countries and continents. Hence, the discovery and development of novel chemical scaffolds, with superior antimalarial activity remain an important priority, for the developing world. Our report describes the development, characterization and evaluation of novel bepotastine-based sulphonamide antimalarials inhibiting asexual stage development of Plasmodium falciparum parasites in vitro. The screening results showed potent inhibitory activity of a number of novel sulphonamides against P. falciparum at low micromolar concentrations, in particular in late-stage parasite development. Based on computational studies we hypothesize N-myristoyltransferase as the target of the compounds developed here. Our results demonstrate the value of novel bepotastine-based sulphonamide compounds for targeting the asexual developmental stages of P. falciparum.
Light-induced metal-free transformations of unactivated pyridotriazoles
Zhang, Ziyan,Yadagiri, Dongari,Gevorgyan, Vladimir
, p. 8399 - 8404 (2019/09/30)
A highly efficient and practical method for incorporation of the arylmethylpyridyl moiety into diverse molecules has been developed. This method features the transition metal-free light-induced room temperature transformation of pyridotriazoles into pyridyl carbenes, which are capable of smooth arylation, X-H insertion, and cyclopropanation reactions. The synthetic usefulness of the developed method was illustrated in a facile synthesis of biologically active molecules.
METHOD OF SYNTHESIZING BEPOTASTINE OR BENZENESULFONIC ACID SALT THEREOF AND INTERMEDIATES USED THEREIN
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, (2014/03/21)
The present invention relates to a novel method of synthesizing bepotastine or its benzenesulfonic acid salt and novel intermediates used therein. The present invention uses L-α-hydroxy acid for chiral resolution to form an L-α-hydroxy acid salt of a compound represented by the following formula (VII-1), so as to synthesize bepotastine or its benzenesulfonic acid salt in high optical purity.