1093281-33-4Relevant academic research and scientific papers
Identification of C5-NH2 Modified Oseltamivir Derivatives as Novel Influenza Neuraminidase Inhibitors with Highly Improved Antiviral Activities and Favorable Druggability
Bertagnin, Chiara,Du, Ruikun,Guizzo, Laura,Hou, Lingxin,Huang, Bing,Jia, Ruifang,Ju, Han,Kang, Dongwei,Kong, Xiujie,Li, Ping,Liu, Xinyong,Loregian, Arianna,Ma, Xiuli,Murugan, N. Arul,Poongavanam, Vasanthanathan,Zhan, Peng,Zhang, Ying
, p. 17992 - 18009 (2021/11/18)
Our previous efforts have proved that modifications targeting the 150-cavity of influenza neuraminidase can achieve more potent and more selective inhibitors. In this work, four subseries of C5-NH2 modified oseltamivir derivatives were designed
AZABENZIMIDAZOLES AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 53, (2011/06/23)
This invention relates to the use of azabenzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of azabenzimidazoles in the treatment of cancer.
BENZIMIDAZOLES AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 54, (2011/06/11)
This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.
CYP17 inhibitors. Annulations of additional rings in methylene imidazole substituted biphenyls: Synthesis, biological evaluation and molecular modelling
Pinto-Bazurco Mendieta, Mariano A. E.,Negri, Matthias,Hu, Qingzhong,Hille, Ulrike E.,Jagusch, Carsten,Jahn-Hoffmann, Kerstin,Mueller-Vieira, Ursula,Schmidt, Dirk,Lauterbach, Thomas,Hartmann, Rolf W.
experimental part, p. 547 - 609 (2009/04/04)
Twenty-one novel compounds originating from two classes of annulated biphenyls were synthesized as mimetics of the steroidal A- and C-rings and examined for their potency as inhibitors of human CYP17. Selected compounds were tested for inhibition of the hepatic CYP enzyme 3A4. Potent CYP17 inhibitors were found for each class, compound 9 (17 and 71% at 0.2 and 2 μM, respectively) and 21 (591 nM). Compound 21 showed only weak inhibition of CYP3A4 (32 and 64% at 2 and 10 μM, respectively). Both compounds, however, exhibited moderate to strong inhibition of the glucocorticoid-forming enzyme CYP11B1. The most interesting compounds were docked into our protein model. They bound into one of the modes which we have previously published. New interaction regions were identified.
