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Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.

McKittrick BA, Caldwell JP, Bara T, Boykow G, Chintala M, Clader J, Czarniecki M, Courneya B, Duffy R, Fleming L, Giessert R, Greenlee WJ, Heap C, Hong L, Huang Y, Iserloh U, Josien H, Khan T, Korfmacher W, Liang X, Mazzola R, Mitra S, Moore K, Orth P, Rajagopalan M, Roy S, Sakwa S, Strickland C, Vaccaro H, Voigt J, Wang H, Wong J, Zhang R, Zych A
Bioorg Med Chem Lett 25 1592-6 (2015)
Related entries: 4s1g, 4xx4

Cited: 4 times
EuropePMC logo PMID: 25728416

Abstract

The development of renin inhibitors with favorable oral pharmacokinetic profiles has been a longstanding challenge for the pharmaceutical industry. As part of our work to identify inhibitors of BACE1, we have previously developed iminopyrimidinones as a novel pharmacophore for aspartyl protease inhibition. In this letter we describe how we modified substitution around this pharmacophore to develop a potent, selective and orally active renin inhibitor.

Reviews citing this publication (2)

  1. Development and Structural Modification of BACE1 Inhibitors. Gu T, Wu WY, Dong ZX, Yu SP, Sun Y, Zhong Y, Lu YT, Li NG. Molecules 22 E4 (2016)
  2. Synthesis of amino heterocycle aspartyl protease inhibitors. Chambers RK, Khan TA, Olsen DB, Sleebs BE. Org Biomol Chem 14 4970-4985 (2016)

Articles citing this publication (2)

  1. Substrate Peptidomimetic Inhibitors of P. falciparum Plasmepsin X with Potent Antimalarial Activity. Richardson LW, Ashton TD, Dans MG, Nguyen N, Favuzza P, Triglia T, Hodder AN, Ngo A, Jarman KE, Cowman AF, Sleebs BE. ChemMedChem 17 e202200306 (2022)
  2. Renin inhibition by soyasaponin I: a potent native anti-hypertensive compound. Tavassoli Z, Taghdir M, Ranjbar B. J Biomol Struct Dyn 36 166-176 (2018)


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