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Synthesis of the Indole-Based Inhibitors of Bacterial Cystathionine γ-Lyase NL1-NL3 by Konstantin V. Potapov; Roman A. Novikov; Maxim A. Novikov; Pavel N. Solyev; Yury V. Tomilov; Sergey N. Kochetkov; Alexander A. Makarov; Vladimir A. Mitkevich is a Chemistry article available to read on EtoBox.

What is Synthesis of the Indole-Based Inhibitors of Bacterial Cystathionine γ-Lyase NL1-NL3 about?

Bacterial cystathionine γ-lyase (bCSE) is the main producer of H~2~S in pathogenic bacteria such as __Staphylococcus aureus__, __Pseudomonas aeruginosa__, etc. The suppression of bCSE activity considerably enhances the sensitivity of bacteria to antibiotics. Convenient methods for the efficient synthesis of gram quantities of two selective indole-based bCSE inhibitors, namely (2-(6-bromo-1__H__-indol-1-yl)acetyl)glycine (NL1), 5-((6-bromo-1__H__-indol-1-yl)methyl)- 2-methylfuran-3-carboxylic acid (NL2), as well as a synthetic method for preparation 3-((6-(7-chlorobenzo[__b__]thiophen-2-yl)-1__H__-indol-1-yl)methyl)- 1__H__-pyrazole-5-carboxylic acid (NL3), have been developed. The syntheses are based on the use of 6-bromoindole as the main building block for all three inhibitors (NL1, NL2, and NL3), and the designed residues are assembled at the nitrogen atom of the 6-bromoindole core or by the substitution of the bromine atom in the case of NL3 using Pd-catalyzed cross-coupling. The developed and refined synthetic methods would be significant for the further biological screening of NL-series bCSE inhibitors and their derivatives.

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Author

Konstantin V. Potapov; Roman A. Novikov; Maxim A. Novikov; Pavel N. Solyev; Yury V. Tomilov; Sergey N. Kochetkov; Alexander A. Makarov; Vladimir A. Mitkevich

Publisher

MDPI AG

Published

2023

Language

EN

Field

Chemistry (Life Sciences)