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Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors.

Landi G, Linciano P, Borsari C, Bertolacini CP, Moraes CB, Cordeiro-da-Silva A, Gul S, Witt G, Kuzikov M, Costi MP, Pozzi C, Mangani S
ACS Infect Dis 5 1105-1114 (2019)
Related entries: 6hnc, 6hnr

Cited: 9 times
EuropePMC logo PMID: 31012301

Abstract

Cycloguanil is a known dihydrofolate-reductase (DHFR) inhibitor, but there is no evidence of its activity on pteridine reductase (PTR), the main metabolic bypass to DHFR inhibition in trypanosomatid parasites. Here, we provide experimental evidence of cycloguanil as an inhibitor of Trypanosoma brucei PTR1 (TbPTR1). A small library of cycloguanil derivatives was developed, resulting in

Articles - 6how mentioned but not cited (1)

  1. Evidence of Pyrimethamine and Cycloguanil Analogues as Dual Inhibitors of Trypanosoma brucei Pteridine Reductase and Dihydrofolate Reductase. Tassone G, Landi G, Linciano P, Francesconi V, Tonelli M, Tagliazucchi L, Costi MP, Mangani S, Pozzi C. Pharmaceuticals (Basel) 14 636 (2021)


Reviews citing this publication (3)

  1. Dihydrofolate reductase, thymidylate synthase, and serine hydroxy methyltransferase: successful targets against some infectious diseases. Shamshad H, Bakri R, Mirza AZ. Mol Biol Rep 49 6659-6691 (2022)
  2. Structure and dynamics of pteridine reductase 1: the key phenomena relevant to enzyme function and drug design. Panecka-Hofman J, Poehner I. Eur Biophys J 52 521-532 (2023)
  3. Tackling Sleeping Sickness: Current and Promising Therapeutics and Treatment Strategies. Jamabo M, Mahlalela M, Edkins AL, Boshoff A. Int J Mol Sci 24 12529 (2023)

Articles citing this publication (5)

  1. IM Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-6. Vanden Eynde JJ, Mangoni AA, Rautio J, Leprince J, Azuma YT, García-Sosa AT, Hulme C, Jampilek J, Karaman R, Li W, Gomes PAC, Hadjipavlou-Litina D, Capasso R, Geronikaki A, Cerchia L, Sabatier JM, Ragno R, Tuccinardi T, Trabocchi A, Winum JY, Luque FJ, Prokai-Tatrai K, Spetea M, Gütschow M, Kosalec I, Guillou C, Vasconcelos MH, Kokotos G, Rastelli G, de Sousa ME, Manera C, Gemma S, Mangani S, Siciliano C, Galdiero S, Liu H, Scott PJH, de Los Ríos C, Agrofoglio LA, Collina S, Guedes RC, Muñoz-Torrero D. Molecules 25 E119 (2019)
  2. Repurposing the Trypanosomatidic GSK Kinetobox for the Inhibition of Parasitic Pteridine and Dihydrofolate Reductases. Santucci M, Luciani R, Gianquinto E, Pozzi C, Pisa FD, Dello Iacono L, Landi G, Tagliazucchi L, Mangani S, Spyrakis F, Costi MP. Pharmaceuticals (Basel) 14 1246 (2021)
  3. High-Throughput Phenotypic Screening and Machine Learning Methods Enabled the Selection of Broad-Spectrum Low-Toxicity Antitrypanosomatidic Agents. Linciano P, Quotadamo A, Luciani R, Santucci M, Zorn KM, Foil DH, Lane TR, Cordeiro da Silva A, Santarem N, B Moraes C, Freitas-Junior L, Wittig U, Mueller W, Tonelli M, Ferrari S, Venturelli A, Gul S, Kuzikov M, Ellinger B, Reinshagen J, Ekins S, Costi MP. J Med Chem 66 15230-15255 (2023)
  4. Microwave-assisted efficient one-pot synthesis of N 2-(tetrazol-5-yl)-6-aryl/heteroaryl-5,6-dihydro-1,3,5-triazine-2,4-diamines. Moustafa MS, Mekheimer RA, Al-Mousawi SM, Abd-Elmonem M, El-Zorba H, Hameed AMA, Mohamed TM, Sadek KU. Beilstein J Org Chem 16 1706-1712 (2020)
  5. Synthesis and Antiprotozoal Activity of Azabicyclo-Nonane Pyrimidine Hybrids. Hinteregger C, Dolensky J, Seebacher W, Saf R, Mäser P, Kaiser M, Weis R. Molecules 28 307 (2022)


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