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IN SILICO and IN VITRO Estimation of MAO-B Inhibitory Activity of Newly Synthesized Hydrazones Bearing a Pyrrole Heterocyclic System

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Pharmaceutical Chemistry Journal Aims and scope

This paper is focused on the in silico and in vitro determination of MAO-B inhibitory activity on recombinant MAO-B enzyme (hMAOB) of newly synthesized substituted N-pyrrolyl hydrazide hydrazones. From the tested substances, only compound DI 5a has shown statistically significant inhibitory activity on human recombinant MAO-B enzyme, comparable with that of selegiline and better than that of melatonin, applied as standards. The molecular docking studies indicated formation of a stable complex in the aromatic “cage” of the enzyme and the 2-hydroxyphenyl moiety of DI 5a. An additional stable water-mediated hydrogen bond is formed with the carbonyl group located at third position in the pyrrole ring.

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Authors and Affiliations

  1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University Sofia, 2 Dunav str., 1000, Sofia, Bulgaria

    Diana Tzankova, Emilio Mateev, Lily Peikova & Maya Georgieva

  2. Department of Organic Synthesis and Fuels, University of Chemical Technology and Metallurgy, 8 Kl. Ohridski, 1756, Sofia, Bulgaria

    Stanislava Vladimirova

  3. Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University Sofia, 2 Dunav str., 1000, Sofia, Bulgaria

    Denitsa Stefanova & Magdalena Kondeva-Burdina

Authors
  1. Diana Tzankova
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  2. Emilio Mateev
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  3. Stanislava Vladimirova
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  4. Lily Peikova
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  5. Denitsa Stefanova
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  6. Magdalena Kondeva-Burdina
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  7. Maya Georgieva
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Correspondence to Diana Tzankova.

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Tzankova, D., Mateev, E., Vladimirova, S. et al. IN SILICO and IN VITRO Estimation of MAO-B Inhibitory Activity of Newly Synthesized Hydrazones Bearing a Pyrrole Heterocyclic System. Pharm Chem J 57, 1444–1448 (2023). https://doi.org/10.1007/s11094-023-03008-7

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  • DOI: https://doi.org/10.1007/s11094-023-03008-7

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