Literature DB >> 21489787

SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors.

Gang Zhou1, Pauline C Ting, Robert Aslanian, Jianhua Cao, David W Kim, Rongze Kuang, Joe F Lee, John Schwerdt, Heping Wu, R Jason Herr, Andrew J Zych, Jinhai Yang, Sang Lam, Samuel Wainhaus, Todd A Black, Paul M McNicholas, Yiming Xu, Scott S Walker.   

Abstract

A novel series of pyridazinone analogs has been developed as potent β-1,3-glucan synthase inhibitors through structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one (1). The effect of changes to the core structure is described in detail. Optimization of the sulfonamide moiety led to the identification of important compounds with much improved systematic exposure while retaining good antifungal activity against the fungal strains Candida glabrata and Candida albicans. Published by Elsevier Ltd.

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Year:  2011        PMID： 21489787     DOI： 10.1016/j.bmcl.2011.03.083

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


  7 in total

1.  Crystal structure and Hirshfeld surface analysis of ethyl 2-[5-(3-chloro-benz-yl)-6-oxo-3-phenyl-1,6-di-hydro-pyridazin-1-yl]acetate.

Authors:  Fouad El Kalai; Cemile Baydere; Said Daoui; Rafik Saddik; Necmi Dege; Khalid Karrouchi; Noureddine Benchat
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2019-05-24

2.  A complex game of hide and seek: the search for new antifungals.

Authors:  Huy X Ngo; Sylvie Garneau-Tsodikova; Keith D Green
Journal:  Medchemcomm       Date:  2016-05-17       Impact factor: 3.597

3.  Discovery of a novel class of orally active antifungal beta-1,3-D-glucan synthase inhibitors.

Authors:  Scott S Walker; Yiming Xu; Ilias Triantafyllou; Michelle F Waldman; Cara Mendrick; Nathaniel Brown; Paul Mann; Andrew Chau; Reena Patel; Nicholas Bauman; Christine Norris; Barry Antonacci; Maya Gurnani; Anthony Cacciapuoti; Paul M McNicholas; Samuel Wainhaus; R Jason Herr; Rongze Kuang; Robert G Aslanian; Pauline C Ting; Todd A Black
Journal:  Antimicrob Agents Chemother       Date:  2011-08-15       Impact factor: 5.191

4.  Antifungal resistance and new strategies to control fungal infections.

Authors:  Patrick Vandeputte; Selene Ferrari; Alix T Coste
Journal:  Int J Microbiol       Date:  2011-12-01

5.  Crystal structure, Hirshfeld surface analysis and DFT studies of 6-[(E)-2-(thio-phen-2-yl)ethenyl]-4,5-di-hydro-pyridazin-3(2H)-one.

Authors:  Said Daoui; Emine Berrin Çınar; Fouad El Kalai; Rafik Saddik; Necmi Dege; Khalid Karrouchi; Noureddine Benchat
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2019-11-15

6.  Crystal structure and Hirshfeld surface analysis of (E)-6-(4-hy-droxy-3-meth-oxy-styr-yl)-4,5-di-hydro-pyridazin-3(2H)-one.

Authors:  Said Daoui; Cemile Baydere; Fouad El Kalai; Rafik Saddik; Necmi Dege; Khalid Karrouchi; Noureddine Benchat
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2019-10-31

7.  In silico screening for identification of novel β-1,3-glucan synthase inhibitors using pharmacophore and 3D-QSAR methodologies.

Authors:  Potshangbam Angamba Meetei; R S Rathore; N Prakash Prabhu; Vaibhav Vindal
Journal:  Springerplus       Date:  2016-07-04
  7 in total

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