Molecules (2018)
Update date:2022-07-30
Topics:
Sanna, Giuseppina
Madeddu, Silvia
Giliberti, Gabriele
Piras, Sandra
Struga, Marta
Wrzosek, Ma?gorzata
Kubiak-Tomaszewska, Grazyna
Koziol, Anna E.
Savchenko, Oleksandra
Lis, Tadeusz
Stefanska, Joanna
Tomaszewski, Piotr
Skrzycki, Michal
Szulczyk, Daniel
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 28 were 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. aureus DNA 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.
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