Wydział Chemii

Giuseppina Sanna

Silvia Madeddu

Gabriele Giliberti

Sandra Piras

Marta Struga

Małgorzata Wrzosek

Grażyna Kubiak-Tomaszewska

Anna E. Kozioł

Oleksandra Savchenko

Tadeusz Lis

Joanna Stefanska

Piotr Tomaszewski

Michał Skrzycki

Daniel Szulczyk

2018

Molecules

23

2554/1-2554/17

10.3390/molecules23102554

Naukowa

Angielski

Artykuł

A series of 2-(1H-indol-3-yl)ethylthiourea derivatives were prepared by condensation of 2-(1H-indol-3-yl)ethanamine with appropriate aryl/alkylisothiocyanates in anhydrous media. The structures of the newly synthesized compounds were confirmed by spectroscopic analysis and the molecular structures of 8 and 28were confirmed by X-ray crystallography. All obtained compounds were tested for antimicrobial activity against Gram-positive cocci, Gram-negative rods and for antifungal activity. Microbiological evaluation was carried out over 20 standard strains and 30 hospital strains. Compound 6 showed significant inhibition against Gram-positive cocci and had inhibitory effect on the S. aureus topoisomerase IV decatenation activity and S. aureusDNA gyrase supercoiling activity. Compounds were tested for cytotoxicity and antiviral activity against a large panel of DNA and RNA viruses, including HIV-1 and other several important human pathogens. Interestingly, derivative 8 showed potent activity against HIV-1 wild type and variants bearing clinically relevant mutations. Newly synthesized tryptamine derivatives showed also a wide spectrum activity, proving to be active against positive- and negative-sense RNA viruses.

antibacterial activity, anti-HIV activity, antiviral activity, thiourea derivatives of indole, topoisomerase

CC-BY

http://dx.doi.org/10.3390/molecules23102554

http://www.mdpi.com/journal/metals