English Journal

Eastwood P, Gonzalez J, Gomez E, Caturla F, Aguilar N, Mir M, Aiguade J, Matassa V, Balague C, Orellana A, Dominguez M.SourceAlmirall Research Center, Almirall Laboratories, Ctra. Laurea Miro 408, E-08980 St. Feliu de Llobregat, Barcelona, Spain.
Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2011 Nov 1;21(21):6253-7. Epub 2011 Sep 10.
Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38α inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have mode
PMID 21958544

Synthesis and SAR optimization of diketo acid pharmacophore for HCV NS5B polymerase inhibition.

Bhatt A, Gurukumar KR, Basu A, Patel MR, Kaushik-Basu N, Talele TT.SourceDepartment of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John's University, Queens, NY 11439, USA.
European journal of medicinal chemistry.Eur J Med Chem.2011 Oct;46(10):5138-45. Epub 2011 Aug 26.
Hepatitis C virus (HCV) NS5B polymerase is a key target for anti-HCV therapeutics development. Here we report the synthesis and biological evaluation of a new series of α,γ-diketo acids (DKAs) as NS5B polymerase inhibitors. We initiated structure-activity relationship (SAR) optimization around the
PMID 21893371

Japanese Journal

田村理,村上啓寿
有機合成化学協会誌 69(4), 393-402, 2011
… With respect to Rev-export inhibitor valtrate (3), the synthesis of 5,6-dihydroanalog (24), rationally designed with the aid of MO calculation, presented the alternative bioisosteric seed principle. …
NAID 130000927706

Sander Kerstin,Kottke Tim,Weizel Lilia,Stark Holger
CHEMICAL & PHARMACEUTICAL BULLETIN 58(10), 1353-1361, 2010
… In this work, kojic acid-derived structural elements were inserted into a well established H3R antagonist/inverse agonist scaffold to investigate the bioisosteric potential of γ-pyranones with respect to the different moieties of the H3R pharmacophore. …
NAID 130000405640