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- Title
Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas.
- Authors
Sanna, Giuseppina; Madeddu, Silvia; Giliberti, Gabriele; Piras, Sandra; Struga, Marta; Wrzosek, Małgorzata; Kubiak-Tomaszewska, Grażyna; Koziol, Anna E.; Savchenko, Oleksandra; Lis, Tadeusz; Stefanska, Joanna; Tomaszewski, Piotr; Skrzycki, Michał; Szulczyk, Daniel
- Abstract
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.
- Subjects
CONDENSATION; MOLECULAR structure; INDOLE derivatives; MICROBIOLOGY; TRYPTAMINE; RNA viruses; X-ray crystallography
- Publication
Molecules, 2018, Vol 23, Issue 10, p2554
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules23102554