Design and synthesis of pyrano[3,2-b]indolones showing antimycobacterial activity was written by Monakhova, Natalia;Kordulakova, Jana;Vocat, Anthony;Egorova, Anna;Lepioshkin, Alexander;Salina, Elena G.;Nosek, Jozef;Repkova, Eva;Zemanova, Julia;Jurdakova, Helena;Gorova, Renata;Roh, Jaroslav;Degiacomi, Giulia;Sammartino, Jose Camilla;Pasca, Maria Rosalia;Cole, Stewart T.;Mikusova, Katarina;Makarov, Vadim. And the article was included in ACS Infectious Diseases in 2021.Product Details of 827-01-0 This article mentions the following:
Latent Mycobacterium tuberculosis infection presents one of the largest challenges for tuberculosis control and novel antimycobacterial drug development. A series of pyrano[3,2-b]indolone-based compounds was designed and synthesized via an original eight-step scheme. The synthesized compounds were evaluated for their in vitro activity against M. tuberculosis strains H37Rv and streptomycin-starved 18b (SS18b), representing models for replicating and nonreplicating mycobacteria, resp. Some of compound exhibited good activity with MIC99 values of 0.3 and 0.4濠电偞鎸鹃幐?mL against H37Rv and SS18b, resp., as well as low toxicity, acceptable intracellular activity, and satisfactory metabolic stability and was selected as the lead compound for further studies. An anal. of 10a-resistant M. bovis mutants disclosed a cross-resistance with pretomanid and altered relative amounts of different forms of cofactor F420 in these strains. Complementation experiments showed that F420-dependent glucose-6-phosphate dehydrogenase and the synthesis of mature F420 were important for 10a activity. Overall these studies revealed 10a to be a prodrug that is activated by an unknown F420-dependent enzyme in mycobacteria. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Product Details of 827-01-0).
5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Product Details of 827-01-0
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Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles