Literature DB >> 12657279

Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.

Ping Chen1, Derek Norris, Kristin D Haslow, T G Murali Dhar, William J Pitts, Scott H Watterson, Daniel L Cheney, Donna A Bassolino, Catherine A Fleener, Katherine A Rouleau, Diane L Hollenbaugh, Robert M Townsend, Joel C Barrish, Edwin J Iwanowicz.   

Abstract

Screening of our in-house compound collection led to the discovery of 5-bromo-6-amino-2-isoquinoline 1 as a weak inhibitor of IMPDH. Subsequent optimization of 1 afforded a series of novel 2-isoquinolinoaminooxazole-based inhibitors, represented by 17, with single-digit nanomolar potency against the enzyme.

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Year:  2003        PMID: 12657279     DOI: 10.1016/s0960-894x(03)00107-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  IMP dehydrogenase: structure, mechanism, and inhibition.

Authors:  Lizbeth Hedstrom
Journal:  Chem Rev       Date:  2009-07       Impact factor: 60.622

2.  Identification of novel Mt-Guab2 inhibitor series active against M. tuberculosis.

Authors:  Veeraraghavan Usha; Judith V Hobrath; Sudagar S Gurcha; Robert C Reynolds; Gurdyal S Besra
Journal:  PLoS One       Date:  2012-03-29       Impact factor: 3.240

3.  Diverse Isoquinoline Scaffolds by Ugi/Pomeranz-Fritsch and Ugi/Schlittler-Müller Reactions.

Authors:  Yuanze Wang; Pravin Patil; Katarzyna Kurpiewska; Justyna Kalinowska-Tluscik; Alexander Dömling
Journal:  Org Lett       Date:  2019-04-29       Impact factor: 6.005

4.  A Chemo- and Regioselective Tandem [3 + 2]Heteroannulation Strategy for Carbazole Synthesis: Combining Two Mechanistically Distinct Bond-Forming Processes.

Authors:  Emma Campbell; Andrea Taladriz-Sender; Olivia I Paisley; Alan R Kennedy; Jacob T Bush; Glenn A Burley
Journal:  J Org Chem       Date:  2022-03-18       Impact factor: 4.354

  4 in total

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