2101-86-2Relevant articles and documents
Cu(i)-catalyzed microwave-assisted synthesis of 1,2,3-triazole linked with 4-thiazolidinones: A one-pot sequential approach
Kumar, Yogesh,Matta, Akanksha,Kumar, Prashant,Parmar, Virinder S.,Van Der Eycken, Erik V.,Singh, Brajendra K.
, p. 1628 - 1639 (2015)
A novel copper(i) catalyzed, microwave-assisted one-pot, four-component sequential reaction between a propargyloxybenzaldehyde, a substituted phenyl azide, a substituted aniline and thioglycolic acid has been developed for the synthesis of 3-phenyl-2-[4-{
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Fischer,Anselme
, p. 5284 (1967)
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Spauschus,Scott
, p. 208 (1951)
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A mild TCEP-based para-azidobenzyl cleavage strategy to transform reversible cysteine thiol labelling reagents into irreversible conjugates
Maruani, Antoine,Alom, Shamim,Canavelli, Pierre,Lee, Maximillian T. W.,Morgan, Rachel E.,Chudasama, Vijay,Caddick, Stephen
, p. 5279 - 5282 (2015)
It has recently emerged that the succinimide linkage of a maleimide thiol addition product is fragile, which is a major issue in fields where thiol functionalisation needs to be robust. Herein we deliver a strategy that generates selective cysteine thiol
Triazole [5, 4-d] pyrimidone tricyclic compounds as well as preparation method and application thereof
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Paragraph 0064; 0067-0070; 0075, (2021/07/09)
The invention relates to triazole [5, 4-d] pyrimidone tricyclic compounds as well as a preparation method and application thereof.The triazole [5, 4-d] pyrimidone tricyclic compounds are prepared by following steps: taking different substituted anilines a
Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents
Chiarelli, Laurent R.,Fan, Dongguang,Han, Quanquan,Lu, Yu,Qiao, Chunhua,Shi, Rui,Stelitano, Giovanni,Wang, Bin,Huszár, Stanislav,Miku?ová, Katarína,Savková, Karin
supporting information, p. 14526 - 14539 (2021/10/26)
The benzothiazinone (BTZ) scaffold compound PBTZ169 kills Mycobacterium tuberculosis by inhibiting the essential flavoenzyme DprE1, consequently blocking the synthesis of the cell wall component arabinans. While extraordinarily potent against M. tuberculosis with a minimum inhibitory concentration (MIC) less than 0.2 ng/mL, its low aqueous solubility and bioavailability issues need to be addressed. Here, we designed and synthesized a series of 6-methanesulfonyl substituted BTZ analogues; further exploration introduced five-member aromatic heterocycles as linkers to attach an aryl group as the side chain. Our work led to the discovery of a number of BTZ derived compounds with potent antitubercular activity. The optimized compounds 6 and 38 exhibited MIC 47 and 30 nM, respectively. Compared to PBTZ169, both compounds displayed increased aqueous solubility and higher stability in human liver microsomes. This study suggested that an alternative side-chain modification strategy could be implemented to improve the druglike properties of the BTZ-based compounds.