6-Bromoindole- and 6-Bromoindazole-Based Inhibitors of Bacterial Cystathionine γ-Lyase Containing 3-Aminothiophene-2-Carboxylate Moiety

6-Bromoindole- and 6-Bromoindazole-Based Inhibitors of Bacterial Cystathionine γ-Lyase Containing 3-Aminothiophene-2-Carboxylate Moiety Full article

Journal

Molecules
ISSN: 1420-3049

Output data

Year: 2025, Volume: 30, Number: 2, Article number : 388, Pages count : DOI: 10.3390/molecules30020388

Authors

Novikov Roman A. ^1,2 , Platonov Dmitry N. ² , Belyy Alexander Yu. ² , Potapov Konstantin V. ^1,2 , Novikov Maxim A. ^1,2 , Tomilov Yury V. ² , Kechko Olga I. ¹ , Seregina Tatiana A. ¹ , Zemskaya Anastasia S. ¹ , Solyev Pavel N. ¹ , Mitkevich Vladimir A. ¹

Affiliations

1	Engelhardt Institute of Molecular Biology of the Russian Academy of Sciences, 32 Vavilov St., Moscow 119991, Russia
2	Zelinsky Institute of Organic Chemistry of the Russian Academy of Sciences, 47 Leninsky Avenue, Moscow 119991, Russia

n recent years, a number of synthetic potentiators of antibiotics have been discovered. Their action can significantly enhance the antibacterial effect and limit the spread of antibiotic resistance through inhibition of bacterial cystathionine-γ-lyase. To expand the known set of potentiators, we developed methods for the synthesis of five new representatives of 6-bromoindole derivatives—potential inhibitors of bacterial cystathionine-γ-lyase—namely potassium 3-amino-5-((6-bromoindolyl)methyl)thiophene-2-carboxylate (MNS2) and its 6-bromoindazole analogs (MNS3 and MNS4), along with two 6-broindazole analogs of the parent compound NL2. Their syntheses are based on 6-bromoindole, 6-bromoindazole and methyl 5-(bromomethyl)-3-((ethoxycarbonyl)amino)thiophene-2-carboxylate as the main building blocks, assembling the rest of the heterocyclic system on their basis at the nitrogen atom. We assessed the ability of the new inhibitors to potentiate the antimicrobial activity of gentamicin.

Novikov R.A. , Platonov D.N. , Belyy A.Y. , Potapov K.V. , Novikov M.A. , Tomilov Y.V. , Kechko O.I. , Seregina T.A. , Zemskaya A.S. , Solyev P.N. , Mitkevich V.A.
6-Bromoindole- and 6-Bromoindazole-Based Inhibitors of Bacterial Cystathionine γ-Lyase Containing 3-Aminothiophene-2-Carboxylate Moiety
Molecules. 2025. V.30. N2. 388 . DOI: 10.3390/molecules30020388 WOS Scopus OpenAlex

≡ Web of science:	WOS:001404438700001
≡ Scopus:	2-s2.0-85216186247
≡ OpenAlex:	W4406586151