title: Synthesis and Biological Activities of Ethyl 2-(2-pyridylacetate) Derivatives Containing Thiourea, 1,2,4-triazole, Thiadiazole and Oxadiazole Moieties.
abstract: Thirty six novel heterocyclic derivatives of ethyl 2-(2-pyridylacetate) were efficiently synthesized. The new compounds involve the linkage of a 2-pyridyl ring with thiosemicarbazide (compounds1-7), 1,2,4-triazole (compounds1a-7a), 1,3,4-thiadiazole (compounds1b-7b), and 1,3,4-oxadiazole (compounds1f-7f) moieties. The last group of compounds1e-7einvolves the connection of a 2-pyridyl ring with 1,2,4-triazole and thiourea. ¹H-NMR,13C-NMR and MS methods were used to confirm the structures of the obtained derivatives. The molecular structures of3,3b,7aand7fwere further confirmed by X-ray crystallography. All obtained compounds were tested in vitro against a number of microorganisms, including Gram-positive cocci, Gram-negative rods andCandida albicans. In addition, the obtained compounds were tested for cytotoxicity and antiviral activity against HIV-1.
authors.affiliation: Department of Biochemistry and Pharmacogenomics, Faculty of Pharmacy, Medical University of Warsaw, 02-097 Warsaw, Poland. daniel.szulczyk@wum.edu.pl.|Laboratory of Centre for Preclinical Research, Medical University of Warsaw, Banacha 1B, 02-097 Warsaw, Poland. daniel.szulczyk@wum.edu.pl.
authors.forename: Daniel
authors.initials: D
authors.lastname: Szulczyk
authors.affiliation: Department of Biochemistry, Second Faculty of Medicine, Medical University of Warsaw, 02-097 Warsaw, Poland. piotr.tomaszewski@wum.edu.pl.
authors.forename: Piotr
authors.initials: P
authors.lastname: Tomaszewski
authors.affiliation: Department of Biochemistry and Pharmacogenomics, Faculty of Pharmacy, Medical University of Warsaw, 02-097 Warsaw, Poland. michal.jozwiak@wum.edu.pl.|Laboratory of Centre for Preclinical Research, Medical University of Warsaw, Banacha 1B, 02-097 Warsaw, Poland. michal.jozwiak@wum.edu.pl.|Department of Biochemistry, Second Faculty of Medicine, Medical University of Warsaw, 02-097 Warsaw, Poland. michal.jozwiak@wum.edu.pl.
authors.forename: Michał
authors.initials: M
authors.lastname: Jóźwiak
authors.affiliation: Faculty of Chemistry, Maria Curie-Sklodowska University, 20-031 Lublin, Poland. anna.koziol@poczta.umcs.lublin.pl.
authors.forename: Anna E
authors.initials: AE
authors.lastname: Kozioł
authors.affiliation: Faculty of Chemistry, University of Wroclaw, 50-383 Wroclaw, Poland. tadeusz.lis@chem.uni.wroc.pl.
authors.forename: Tadeusz
authors.initials: T
authors.lastname: Lis
authors.affiliation: Department of Life and Environmental Sciences, Section of Microbiology and Virology, University of Cagliari, 09042 Cittadella Universitaria Monserrato, Italy. david.collu@unica.it.
authors.forename: David
authors.initials: D
authors.lastname: Collu
authors.affiliation: Department of Molecular Medicine, Institute of Virology, Slovak Academy of Sciences, Dubravska cesta 9, 845 05 Bratislava, Slovak. filippo.iuliano@unica.it.
authors.forename: Filippo
authors.initials: F
authors.lastname: Iuliano
authors.affiliation: Department of Biochemistry and Pharmacogenomics, Faculty of Pharmacy, Medical University of Warsaw, 02-097 Warsaw, Poland. marta.struga@wum.edu.pl.|Laboratory of Centre for Preclinical Research, Medical University of Warsaw, Banacha 1B, 02-097 Warsaw, Poland. marta.struga@wum.edu.pl.
authors.forename: Marta
authors.initials: M
authors.lastname: Struga
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002460:Cell Line; D002478:Cells, Cultured; D018360:Crystallography, X-Ray; D005658:Fungi / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D010069:Oxadiazoles / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000737:chemistry*; D013890:Thiourea / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000890:Anti-Infective Agents; D010069:Oxadiazoles; D013830:Thiadiazoles; D014230:Triazoles; C045575:1,2,4-triazole; D013890:Thiourea
keywords: 1,2,4-triazole; 1,3,4-oxadiazole; 1,3,4-thiadiazole; X-ray crystal structure analysis; biological activity; thiourea