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Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1.

Venier O, Pascal C, Braun A, Namane C, Mougenot P, Crespin O, Pacquet F, Mougenot C, Monseau C, Onofri B, Dadji-Faïhun R, Leger C, Ben-Hassine M, Van-Pham T, Ragot JL, Philippo C, Güssregen S, Engel C, Farjot G, Noah L, Maniani K, Nicolaï E
Bioorg Med Chem Lett 21 2244-51 (2011)
Cited: 9 times
EuropePMC logo PMID: 21439819

Abstract

A High Throughput Screening campaign allowed the identification of a novel class of ureas as 11β-HSD1 inhibitors. Rational chemical optimization provided potent and selective inhibitors of both human and murine 11β-HSD1 with an appropriate ADME profile and ex vivo activity in target tissues.

Articles - 3qqp mentioned but not cited (3)

  1. Novel 2-(Adamantan-1-ylamino)Thiazol-4(5H)-One Derivatives and Their Inhibitory Activity towards 11β-HSD1-Synthesis, Molecular Docking and In Vitro Studies. Studzińska R, Kupczyk D, Płaziński W, Baumgart S, Bilski R, Paprocka R, Kołodziejska R. Int J Mol Sci 22 8609 (2021)
  2. Search for Compounds with Hypoglycemic Activity in the Series of 1-[2-(1H-Tetrazol-5-yl)-R(1)-phenyl]-3-R(2)-phenyl(ethyl)ureas and R(1)-Tetrazolo[1,5-c]quinazolin-5(6H)-ones. Antypenko OM, Kovalenko SI, Zhernova GO. Sci Pharm 84 233-254 (2016)
  3. Synthesis of Novel 2-(Cyclopentylamino)thiazol-4(5H)-one Derivatives with Potential Anticancer, Antioxidant, and 11β-HSD Inhibitory Activities. Baumgart S, Kupczyk D, Archała A, Koszła O, Sołek P, Płaziński W, Płazińska A, Studzińska R. Int J Mol Sci 24 7252 (2023)


Articles citing this publication (6)

  1. Discovery of SAR184841, a potent and long-lasting inhibitor of 11β-hydroxysteroid dehydrogenase type 1, active in a physiopathological animal model of T2D. Venier O, Pascal C, Braun A, Namane C, Mougenot P, Crespin O, Pacquet F, Mougenot C, Monseau C, Onofri B, Dadji-Faïhun R, Leger C, Ben-Hassine M, Van-Pham T, Ragot JL, Philippo C, Farjot G, Noah L, Maniani K, Boutarfa A, Nicolaï E, Guillot E, Pruniaux MP, Güssregen S, Engel C, Coutant AL, de Miguel B, Castro A. Bioorg. Med. Chem. Lett. 23 2414-2421 (2013)
  2. 1,1-Dioxo-5,6-dihydro-[4,1,2]oxathiazines, a novel class of 11ß-HSD1 inhibitors for the treatment of diabetes. Böhme T, Engel CK, Farjot G, Güssregen S, Haack T, Tschank G, Ritter K. Bioorg. Med. Chem. Lett. 23 4685-4691 (2013)
  3. Identification of novel 11β-HSD1 inhibitors by combined ligand- and structure-based virtual screening. Lagos CF, Vecchiola A, Allende F, Fuentes CA, Tichauer JE, Valdivia C, Solari S, Campino C, Tapia-Castillo A, Baudrand R, Villarroel P, Cifuentes M, Owen GI, Carvajal CA, Fardella CE. Mol. Cell. Endocrinol. 384 71-82 (2014)
  4. Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes. Wan ZK, Chenail E, Li HQ, Ipek M, Xiang J, Suri V, Hahm S, Bard J, Svenson K, Xu X, Tian X, Wang M, Li X, Johnson CE, Qadri A, Panza D, Perreault M, Mansour TS, Tobin JF, Saiah E. ACS Med Chem Lett 4 118-123 (2013)
  5. Synthesis and biological evaluation of novel urea- and guanidine-based derivatives for the treatment of obesity-related hepatic steatosis. Liang X, Pei H, Ma L, Ran Y, Chen J, Wang G, Chen L. Molecules 19 6163-6183 (2014)
  6. Avirulins, a Novel Class of HIV-1 Reverse Transcriptase Inhibitors Effective in the Female Reproductive Tract Mucosa. Cherne MD, Hall J, Kellner A, Chong CF, Cole AL, Cole AM. Viruses 11 (2019)


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