bioisoster​e

Discovery of [1,2,4]Triazolo[1,5-a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists


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  • R. Nakajima, H. Oono, S. Sugiyama, Y. Matsueda, T. Ida, S. Kakuda, J. Hirata, A. Baba, A. Makino, R. Matsuyama, R.D. White, R.. Wurz, Y. Shin, X. Min, A. Guzman-Perez, Z. Wang, A. Symons, S.K. Singh, S.R. Mothe, S. Belyakov, A. Chakrabarti, and S. Shuto, "Discovery of [1,2,4]Triazolo[1,5-a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists", ACS Medicinal Chemistry Letters, vol. 11, pp. 528-534, 2020. http://dx.doi.org/10.1021/acsmedchemlett.9b00649
  • Dual Photoredox/Nickel-Catalyzed Conversion of Aryl Halides to Aryl Aminooxetanes: Computational Evidence for a Substrate-Dependent Switch in Mechanism

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  • K. Kolahdouzan, R. Khalaf, J.M. Grandner, Y. Chen, J.A. Terrett, and M.P. Huestis, "Dual Photoredox/Nickel-Catalyzed Conversion of Aryl Halides to Aryl Aminooxetanes: Computational Evidence for a Substrate-Dependent Switch in Mechanism", ACS Catalysis, vol. 10, pp. 405-411, 2019. http://dx.doi.org/10.1021/acscatal.9b03596
  • Heterocycle amide isosteres: An approach to overcoming resistance for HIV-1 integrase strand transfer inhibitors

    BMS research
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  • K.M. Peese, B.N. Naidu, M. Patel, C. Li, D.R. Langley, B. Terry, T. Protack, V. Gali, Z. Lin, H.K. Samanta, M. Zheng, S. Jenkins, I.B. Dicker, M.R. Krystal, N.A. Meanwell, and M.A. Walker, "Heterocycle amide isosteres: An approach to overcoming resistance for HIV-1 integrase strand transfer inhibitors", Bioorganic & Medicinal Chemistry Letters, vol. 30, pp. 126784, 2020. http://dx.doi.org/10.1016/j.bmcl.2019.126784
  • CF2H, a Functional Group-Dependent Hydrogen-Bond Donor: Is It a More or Less Lipophilic Bioisostere of OH, SH, and CH3?


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  • Y. Zafrani, G. Sod-Moriah, D. Yeffet, A. Berliner, D. Amir, D. Marciano, S. Elias, S. Katalan, N. Ashkenazi, M. Madmon, E. Gershonov, and S. Saphier, "CF2H, a Functional Group-Dependent Hydrogen-Bond Donor: Is It a More or Less Lipophilic Bioisostere of OH, SH, and CH3?", Journal of Medicinal Chemistry, vol. 62, pp. 5628-5637, 2019. http://dx.doi.org/10.1021/acs.jmedchem.9b00604
  • CF2H, a Functional Group-Dependent Hydrogen-Bond Donor: bioisosteric comparison to OH, SH, and CH3


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  • Y. Zafrani, G. Sod-Moriah, D. Yeffet, A. Berliner, D. Amir, D. Marciano, S. Elias, S. Katalan, N. Ashkenazi, M. Madmon, E. Gershonov, and S. Saphier, "CF2H, a Functional Group-Dependent Hydrogen-Bond Donor: Is It a More or Less Lipophilic Bioisostere of OH, SH, and CH3?", Journal of Medicinal Chemistry, vol. 62, pp. 5628-5637, 2019. http://dx.doi.org/10.1021/acs.jmedchem.9b00604
  • Sulfonimidamides and Imidosulfuric Diamides: Compounds from an Underexplored Part of Biologically Relevant Chemical Space

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  • S.V. Zasukha, V.M. Timoshenko, A.A. Tolmachev, V.O. Pivnytska, O. Gavrylenko, S. Zhersh, Y. Shermolovich, and O.O. Grygorenko, "Sulfonimidamides and Imidosulfuric Diamides: Compounds from an Underexplored Part of Biologically Relevant Chemical Space", Chemistry – A European Journal, vol. 25, pp. 6928-6940, 2019. http://dx.doi.org/10.1002/chem.201900440
  • 3-((Hetera)cyclobutyl)azetidines, “Stretched” Analogues of Piperidine, Piperazine, and Morpholine: Advanced Building Blocks for Drug Discovery


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  • I.O. Feskov, A.V. Chernykh, Y.O. Kuchkovska, C.G. Daniliuc, I.S. Kondratov, and O.O. Grygorenko, "3-((Hetera)cyclobutyl)azetidines, “Stretched” Analogues of Piperidine, Piperazine, and Morpholine: Advanced Building Blocks for Drug Discovery", The Journal of Organic Chemistry, vol. 84, pp. 1363-1371, 2018. http://dx.doi.org/10.1021/acs.joc.8b02822
  • Synthesis of 3,3-Diarylazetidines by Calcium(II)-Catalyzed Friedel–Crafts Reaction of Azetidinols with Unexpected Cbz Enhanced Reactivity

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  • C. Denis, M.A.J. Dubois, A.S. Voisin-Chiret, R. Bureau, C. Choi, J.J. Mousseau, and J.A. Bull, "Synthesis of 3,3-Diarylazetidines by Calcium(II)-Catalyzed Friedel–Crafts Reaction of Azetidinols with Unexpected Cbz Enhanced Reactivity", Organic Letters, vol. 21, pp. 300-304, 2018. http://dx.doi.org/10.1021/acs.orglett.8b03745
  • 3-((Hetera)cyclobutyl)azetidines, “Stretched” Analogues of Piperidine, Piperazine, and Morpholine: Advanced Building Blocks for Drug Discovery


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  • I.O. Feskov, A.V. Chernykh, Y.O. Kuchkovska, C.G. Daniliuc, I.S. Kondratov, and O.O. Grygorenko, "3-((Hetera)cyclobutyl)azetidines, “Stretched” Analogues of Piperidine, Piperazine, and Morpholine: Advanced Building Blocks for Drug Discovery", The Journal of Organic Chemistry, vol. 84, pp. 1363-1371, 2018. http://dx.doi.org/10.1021/acs.joc.8b02822
  • De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors

    An unusual bioisostere phenyl

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  • Y. Wang, H. Zhao, J.T. Brewer, H. Li, Y. Lao, W. Amberg, B. Behl, I. Akritopoulou-Zanze, J. Dietrich, U.E.W. Lange, F. Pohlki, C. Hoft, W. Hornberger, S.W. Djuric, J. Sydor, M. Mezler, A.L. Relo, and A. Vasudevan, "De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors", Journal of Medicinal Chemistry, vol. 61, pp. 7486-7502, 2018. http://dx.doi.org/10.1021/acs.jmedchem.8b00295
  • Validating Eaton’s Hypothesis: Cubane as a Benzene Bioisostere


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  • B.A. Chalmers, H. Xing, S. Houston, C. Clark, S. Ghassabian, A. Kuo, B. Cao, A. Reitsma, C.P. Murray, J.E. Stok, G.M. Boyle, C.J. Pierce, S.W. Littler, D.A. Winkler, P.V. Bernhardt, C. Pasay, J.J. De Voss, J. McCarthy, P.G. Parsons, G.H. Walter, M.T. Smith, H.M. Cooper, S.K. Nilsson, J. Tsanaktsidis, G.P. Savage, and C.M. Williams, "Validating Eaton's Hypothesis: Cubane as a Benzene Bioisostere", Angewandte Chemie International Edition, vol. 55, pp. 3580-3585, 2016. http://dx.doi.org/10.1002/anie.201510675