Isocytosine-based inhibitors of xanthine oxidase: Design, synthesis, SAR, PK and in vivo efficacy in rat model of hyperuricemia

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 24, 2012, Pages 7543-7546

  Khanna, Smriti ^a   Burudkar, Sandeep ^a   Bajaj, Komal ^a   Shah, Pranay ^a   Keche, Ashish ^a   Ghosh, Usha ^a   Desai, Avani ^a   Srivastava, Ankita ^a   Kulkarni Almeida, Asha ^a   Deshmukh, Nitin J ^a   Dixit, Amol ^a   Brahma, Manoja K ^a   Bahirat, Umakant ^a   Doshi, Lalit ^a   Nemmani, Kumar V S ^a   Tannu, Prashant ^a   Damre, Anagha ^a   B Rao, Chandrika ^a   Sharma, Rajiv ^a   Sivaramakrishnan, H ^a  

^a Piramal Enterprises Limited   (India)

Author keywords

Docking; Isocytosine; Lead optimization; Structure activity relationship; Xanthine oxidase inhibitors

Indexed keywords

ALLOPURINOL; FEBUXOSTAT; ISOCYTOSINE DERIVATIVE; UNCLASSIFIED DRUG; XANTHINE OXIDASE; XANTHINE OXIDASE INHIBITOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; DRUG DESIGN; DRUG EFFICACY; DRUG HALF LIFE; DRUG SYNTHESIS; ENZYME INHIBITION; HYPERURICEMIA; IC 50; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; CYTOSINE; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; ENZYME INHIBITORS; HYPERURICEMIA; MODELS, MOLECULAR; MOLECULAR STRUCTURE; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; STRUCTURE-ACTIVITY RELATIONSHIP; TIME FACTORS; XANTHINE OXIDASE;

RATTUS;

EID: 84870235210     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.10.029     Document Type: Article

References (12)

1. D.B. Crittenden, and M.H. Pillinger Bull. NYU Hosp. Jt. Dis. 69 2011 257
2. K.Y. Kim, R.H. Schumacher, E. Hunsche, A.I. Wertheimer, and S.X. Kong Clin. Ther. 25 2003 1593
3. J.B. Mapa, and M.H. Pillinger Curr. Opin. Invest. Drugs. 11 2010 499
4. F. Borges, E. Fernandes, and F. Roleira Curr. Med. Chem. 9 2002 195
5. P. Pacher, A. Nivorozhkin, and C. Szabó Pharmacol. Rev. 58 2006 87
6. J.U. Adams Nat. Biotechnol. 27 2009 309
7. P.I. Hair, P.L. McCormack, and G.M. Keating Drugs 2008 1865 68
8. C. B-Rao, A. Kulkarni-Almeida, K.V. Katkar, S. Khanna, U. Ghosh, A. Keche, P. Shah, A. Srivastava, V. Korde, K.V.S. Nemmani, N.J. Deshmukh, A. Dixit, M. Brahma, U. Bahirat, L. Doshi, R. Sharma, and H. Sivaramakrishnan Bioorg. Med. Chem. 20 2012 2930
9. A. Fukunari, K. Okamoto, T. Nishino, B.T. Eger, E.F. Pai, M. Kamezawa, I. Yamada, and N. Kato J. Pharmacol. Exp. Ther. 311 2004 519
10. R.A. Friesner, R.B. Murphy, M.P. Repasky, L.L. Frye, J.R. Greenwood, T.A. Halgren, P.C. Sanschagrin, and D.T. Mainz J. Med. Chem. 49 2006 6177
11. Glide, version 5.7, Schrödinger, LLC, New York, NY, 2011.
12. The PyMOL Molecular Graphics System, Version 1.2r2, Schrödinger, LLC.