Artificial Intelligence Applied to the Rapid Identification of New Antimalarial Candidates with Dual-Stage Activity

Authors: Marilia N. N. Lima, Joyce V. B. Borba, Gustavo C. Cassiano, Melina Mottin, Sabrina S. Mendonça, Arthur C. Silva, Kaira C. P. Tomaz, Juliana Calit, Daniel Y. Bargieri, Fabio T. M. Costa, Carolina H. Andrade
Publication Year: 2021
Journal: Chemmedchem, 16(7), pp 1093-1103
Link: https://doi.org/10.1002/cmdc.202000685

ABSTRACT Increasing reports of multidrug-resistant malaria parasites urge the discovery of new effective drugs with different chemical scaffolds. Protein kinases play a key role in many cellular processes such as signal transduction and cell division, making them interesting targets in many diseases. Protein kinase 7 (PK7) is an orphan kinase from the Plasmodium genus, essential […]
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N-cinnamoylation of antimalarial classics: quinacrine analogues with decreased toxicity and dual-stage activity

Authors: Albuquerque I, Gomes A, Gomes P, Machado M, Nogueira F, Perez B, Prudencio M, Teixeira C
Publication Year: 2014
Journal: Chemmedchem
Link: https://www.ncbi.nlm.nih.gov/pubmed/24474655

Plasmodium falciparum, the causative agent of the most lethal form of malaria, is becoming increasingly resistant to most available drugs. A convenient approach to combat parasite resistance is the development of analogues of classical antimalarial agents, appropriately modified in order to restore their relevance in antimalarial chemotherapy. Following this line of thought, the design, synthesis […]
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N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials

Authors: Gomes A, Gomes P, Lobo L, Machado M, Nogueira F, Prudencio M, Teixeira C
Publication Year: 2015
Journal: Chemmedchem
Link: http://www.ncbi.nlm.nih.gov/pubmed/26038181

In a follow-up study to our reports of N-cinnamoylated chloroquine and quinacrine analogues as promising dual-stage antimalarial leads with high in vitro potency against both blood-stage Plasmodium falciparum and liver-stage Plasmodium berghei, we decided to investigate the effect of replacing the cinnamoyl moiety with other acyl groups. Thus, a series of N-acylated analogues were synthesized, and their activities against blood- and liver-stage Plasmodium spp. were assessed along with their in vitro cytotoxicities.
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Artificial Intelligence Applied to the Rapid Identification of New Antimalarial Candidates with Dual-Stage Activity

N-cinnamoylation of antimalarial classics: quinacrine analogues with decreased toxicity and dual-stage activity

N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials

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