14667-47-1Relevant articles and documents
Rational multistep synthesis of a novel polyfunctionalized benzo[d]thiazole and its thiazolo[5,4-b]pyridine analogue
Hédou, Damien,Deau, Emmanuel,Harari, Marine,Sanselme, Morgane,Fruit, Corinne,Besson, Thierry
, p. 5541 - 5549 (2014)
Reliable synthetic routes were studied for an access to a novel polyfunctionalized 6-amino-2-cyanobenzo[d]thiazole-5-carboxylate ester (1) and its analogue 5-amino-2-cyanothiazolo[5,4-b]pyridine-6-carboxylate ester (2). Both compounds 1 and 2 are functionalized as molecular bricks for the synthesis of innovative molecular systems. Part of the chemistry performed in this study was achieved under microwave irradiation.
Preparation and chemical behavior of 2-(tert-butoxycarbonyl)amino-3- bromomethyl pyridine, a novel alkylating agent
Krasavin, Mikhail,Shkavrov, Sergey,Kravchenko, Dmitry
, p. 181 - 186 (2006)
Synthesis of a novel heterocyclic alkylating agent has been developed. Its instability toward elevated temperatures and/or polar media can be used to prepare 8-aza-1,4-dihydrobenzo[1,3-d]oxazin-2-one. Copyright Taylor & Francis LLC.
Ruthenium-Catalyzed Reductive Arylation of N-(2-Pyridinyl)amides with Isopropanol and Arylboronate Esters
Ronson, Thomas O.,Renders, Evelien,Van Steijvoort, Ben F.,Wang, Xubin,Wybon, Clarence C. D.,Prokopcová, Hana,Meerpoel, Lieven,Maes, Bert U. W.
supporting information, p. 482 - 487 (2019/01/04)
A new three-component reductive arylation of amides with stable reactants (iPrOH and arylboronate esters), making use of a 2-pyridinyl (Py) directing group, is described. The N-Py-amide substrates are readily prepared from carboxylic acids and PyNH2, and the resulting N-Py-1-arylalkanamine reaction products are easily transformed into the corresponding chlorides by substitution of the HN-Py group with HCl. The 1-aryl-1-chloroalkane products allow substitution and cross-coupling reactions. Therefore, a general protocol for the transformation of carboxylic acids into a variety of functionalities is obtained. The Py-NH2 by-product can be recycled.
Discovering a new class of antifungal agents that selectively inhibits microbial carbonic anhydrases
Annunziato, Giannamaria,Giovati, Laura,Angeli, Andrea,Pavone, Marialaura,Del Prete, Sonia,Pieroni, Marco,Capasso, Clemente,Bruno, Agostino,Conti, Stefania,Magliani, Walter,Supuran, Claudiu T.,Costantino, Gabriele
, p. 1537 - 1544 (2018/10/15)
Infections caused by pathogens resistant to the available antimicrobial treatments represent nowadays a threat to global public health. Recently, it has been demonstrated that carbonic anhydrases (CAs) are essential for the growth of many pathogens and their inhibition leads to growth defects. Principal drawbacks in using CA inhibitors (CAIs) as antimicrobial agents are the side effects due to the lack of selectivity toward human CA isoforms. Herein we report a new class of CAIs, which preferentially interacts with microbial CA active sites over the human ones. The mechanism of action of these inhibitors was investigated against an important fungal pathogen, Cryptococcus neoformans, revealing that they are also able to inhibit CA in microbial cells growing in vitro. At our best knowledge, this is the first report on newly designed synthetic compounds selectively targeting β-CAs and provides a proof of concept of microbial CAs suitability as an antimicrobial drug target.