Browsing by Author "Rivero-Jerez, Paula S."

Now showing 1 - 3 of 3
  • No Thumbnail Available
    Item
    Assessment of the Activity of Nitroisoxazole Derivatives against Trypanosoma cruzi
    (2024) Moncada-Basualto, Mauricio; Saavedra-Olavarria, Jorge; Rivero-Jerez, Paula S.; Rojas, Cristian; Maya, Juan D.; Liempi, Ana; Zuniga-Bustos, Matias; Olea-Azar, Claudio; Lapier, Michel; Perez, Edwin G.; Pozo-Martinez, Josue
    The development of new compounds to treat Chagas disease is imperative due to the adverse effects of current drugs and their low efficacy in the chronic phase. This study aims to investigate nitroisoxazole derivatives that produce oxidative stress while modifying the compounds' lipophilicity, affecting their ability to fight trypanosomes. The results indicate that these compounds are more effective against the epimastigote form of T. cruzi, with a 52 +/- 4% trypanocidal effect for compound 9. However, they are less effective against the trypomastigote form, with a 15 +/- 3% trypanocidal effect. Additionally, compound 11 interacts with a higher number of amino acid residues within the active site of the enzyme cruzipain. Furthermore, it was also found that the presence of a nitro group allows for the generation of free radicals; likewise, the large size of the compound enables increased interaction with aminoacidic residues in the active site of cruzipain, contributing to trypanocidal activity. This activity depends on the size and lipophilicity of the compounds. The study recommends exploring new compounds based on the nitroisoxazole skeleton, with larger substituents and lipophilicity to enhance their trypanocidal activity.
  • No Thumbnail Available
    Item
    Fast and efficient synthesis of 2-(benzyloxy)-N,N-disubtituted-2-phenylethan-1-amines
    (2023) Rivero-Jerez, Paula S.; Saavedra-Olavarria, Jorge; Perez, Edwin G.
    A concise, metal catalyst free synthesis of 6-benzyloxyphenethylamines using the regioisomeric mixture obtained in the dialkylamine styrene oxide-ring opening products which reacted with MsCl to produce an aziridinium intermediate. This intermediate reacts, separately, with different benzyl alcohols to produce the desired products but using modern techniques such as fast heating in both steps.& COPY; 2023 Elsevier Ltd. All rights reserved.
  • No Thumbnail Available
    Item
    Synthesis of N-arylsulfonamides via Chan-Lam Coupling Between Aryl Boronic Acids and N-[(sulfonyl)imino]phenyliodinanes
    (2021) Merchan-Arenas, Diego R.; Rivero-Jerez, Paula S.; Perez, Edwin G.
    We synthesized a library of 32 sulfonamides via CuBr2 catalyzed Chan-Lam C-N coupling, reaching excellent yields (until 81 %) under ligand-base-free, mild conditions, and short reaction times. A new non-toxic, versatile and easy to prepare starting materials, N-[(Sulfonyl)imino]phenyliodinanes were first time proposed as the nitrogen source in this synthetic tool. Finally, the sulfonamides were used as valuable building blocks in the synthesis of mono-alkyl anilines through their alkylation and Fukuyama deprotection steps.