40219-06-5Relevant articles and documents
4-Arylthieno[2,3-b]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents
Alder, Arne,Gilberger, Tim,Kunick, Conrad,Schwed, Sandra I.
, (2020/08/24)
Malaria causes hundreds of thousands of deaths every year, making it one of the most dangerous infectious diseases worldwide. Because the pathogens have developed resistance against most of the established anti-malarial drugs, new antiplasmodial agents are urgently needed. In analogy to similar antiplasmodial ketones, 4-arylthieno[2,3-b]pyridine-2-carboxamides were synthesized by Thorpe-Ziegler reactions. In contrast to the related ketones, these carboxamides are only weak inhibitors of the plasmodial enzyme PfGSK-3 but the compounds nevertheless show strong antiparasitic activity. The most potent representatives inhibit the pathogens with IC50values in the two-digit nanomolar range and exhibit high selectivity indices (>100).
Novel multicomponent synthesis of 6,7-dihydro-5H-cyclopenta[b]pyridine derivatives
Dorovatovskii, Pavel V.,Dyachenko, Ivan V.,Dyachenko, Vladimir D.,Khrustalev, Victor N.,Nenajdenko, Valentine G.
, p. 1592 - 1598 (2021/01/11)
[Figure not available: see fulltext.] The multicomponent condensation of malononitrile, hydrogen sulfide, aldehydes, 1-(cyclopent-1-en-1-yl)pyrrolidine, and alkylating agents leads to the formation of 6,7-dihydro-5H-cyclopenta[b]pyridine derivatives. The structure of a number of heterocycles obtained on their basis was studied by X-ray structural analysis.
Organophosphorus chemistry, 291. The action of 2,4-bis-(4-methoxyphenyl)-1,3,2,4-dithiaphosphetane-2,4-disulfide (Lawesson's reagent) on α, ss-unsaturated nitriles
Khidre, Maha D.,Yakout, El-Sayed M.A.,Refat, Mohamed,Mahran
, p. 119 - 125 (2007/10/03)
The reaction of 2,4-bis-(4-methoxyphenyl)-1,3,2,4-dithiaphosphetane-2,4-disulfide (Lawesson's reagent. LR, 1) with ylidenemalononitriles (5a-f) was studied. Partial hydrolysis of 5a-f followed by thiation with LR yields the respective thioamides 7a-f. Nuc
