Literature DB >> 24900660

Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.

Rémi Guillon1, Fabrice Pagniez2, Carine Picot2, Damien Hédou3, Alain Tonnerre1, Elizabeth Chosson3, Muriel Duflos1, Thierry Besson3, Cédric Logé1, Patrice Le Pape2.   

Abstract

Synthesis of a strict structural analogue of albaconazole in which the quinazolinone ring is fused by a thiazole moiety led to the discovery of a new triazole with broad-spectrum antifungal activity. Compound I exhibited high in vitro activity against pathogenic Candida species and filamentous fungi and showed preliminary in vivo antifungal efficacy in a mice model of systemic candidiasis.

Entities:  

Keywords:  Aspergillus; Candida; antifungal agents; azoles; thiazolo[4,5-g]quinazolin-8(7H)-one; zygomycetes

Year:  2013        PMID： 24900660      PMCID： PMC4027234          DOI： 10.1021/ml300429p

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  17 in total

1.  New developments in invasive fungal disease.

Authors:  Andreas H Groll; Joanna Lumb
Journal:  Future Microbiol       Date:  2012-02       Impact factor: 3.165

2.  Synthesis and evaluation of the antiproliferative activity of novel thiazoloquinazolinone kinases inhibitors.

Authors:  Alexandra Testard; Laurent Picot; Olivier Lozach; Melina Blairvacq; Laurent Meijer; Laurence Murillo; Jean-Marie Piot; Valérie Thiéry; Thierry Besson
Journal:  J Enzyme Inhib Med Chem       Date:  2005-12       Impact factor: 5.051

3.  Treatment of aspergillosis: clinical practice guidelines of the Infectious Diseases Society of America.

Authors:  Thomas J Walsh; Elias J Anaissie; David W Denning; Raoul Herbrecht; Dimitrios P Kontoyiannis; Kieren A Marr; Vicki A Morrison; Brahm H Segal; William J Steinbach; David A Stevens; Jo-Anne van Burik; John R Wingard; Thomas F Patterson
Journal:  Clin Infect Dis       Date:  2008-02-01       Impact factor: 9.079

4.  Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3.

Authors:  Alexandra Testard; Cédric Logé; Benoît Léger; Jean-Michel Robert; Olivier Lozach; Mélina Blairvacq; Laurent Meijer; Valérie Thiéry; Thierry Besson
Journal:  Bioorg Med Chem Lett       Date:  2006-04-27       Impact factor: 2.823

5.  New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.

Authors:  J Bartroli; E Turmo; M Algueró; E Boncompte; M L Vericat; L Conte; J Ramis; M Merlos; J García-Rafanell; J Forn
Journal:  J Med Chem       Date:  1998-05-21       Impact factor: 7.446

Review 6.  Molecular genetic analysis of azole antifungal mode of action.

Authors:  S L Kelly; A Arnoldi; D E Kelly
Journal:  Biochem Soc Trans       Date:  1993-11       Impact factor: 5.407

Review 7.  Newer antifungal agents.

Authors:  Ozden Türel
Journal:  Expert Rev Anti Infect Ther       Date:  2011-03       Impact factor: 5.091

8.  Design, synthesis, and in vitro antifungal activity of 1-[(4-substituted-benzyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols.

Authors:  Rémi Guillon; Fabrice Pagniez; Francis Giraud; Damien Crépin; Carine Picot; Marc Le Borgne; Florent Morio; Muriel Duflos; Cédric Logé; Patrice Le Pape
Journal:  ChemMedChem       Date:  2011-03-02       Impact factor: 3.466

9.  Optically active antifungal azoles. I. Synthesis and antifungal activity of (2R,3R)-2-(2,4-difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2-b utanol and its stereoisomers.

Authors:  A Tasaka; N Tamura; Y Matsushita; K Teranishi; R Hayashi; K Okonogi; K Itoh
Journal:  Chem Pharm Bull (Tokyo)       Date:  1993-06       Impact factor: 1.645

10.  Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.

Authors:  G W Rewcastle; B D Palmer; A J Bridges; H D Showalter; L Sun; J Nelson; A McMichael; A J Kraker; D W Fry; W A Denny
Journal:  J Med Chem       Date:  1996-02-16       Impact factor: 7.446
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  4 in total

1.  Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II.

Authors:  Alicia Foucourt; Damien Hédou; Carole Dubouilh-Benard; Angélique Girard; Thierry Taverne; Anne-Sophie Casagrande; Laurent Désiré; Bertrand Leblond; Thierry Besson
Journal:  Molecules       Date:  2014-09-26       Impact factor: 4.411

2.  Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part I.

Authors:  Alicia Foucourt; Damien Hédou; Carole Dubouilh-Benard; Laurent Désiré; Anne-Sophie Casagrande; Bertrand Leblond; Nadège Loäec; Laurent Meijer; Thierry Besson
Journal:  Molecules       Date:  2014-09-29       Impact factor: 4.411

3.  Antitubercular, Cytotoxicity, and Computational Target Validation of Dihydroquinazolinone Derivatives.

Authors:  Katharigatta N Venugopala; Nizar A Al-Shar'i; Lina A Dahabiyeh; Wafa Hourani; Pran Kishore Deb; Melendhran Pillay; Bashaer Abu-Irmaileh; Yasser Bustanji; Sandeep Chandrashekharappa; Christophe Tratrat; Mahesh Attimarad; Anroop B Nair; Nagaraja Sreeharsha; Pottathil Shinu; Michelyne Haroun; Mahmoud Kandeel; Abdulmalek Ahmed Balgoname; Rashmi Venugopala; Mohamed A Morsy
Journal:  Antibiotics (Basel)       Date:  2022-06-21

4.  Larvicidal Activities of 2-Aryl-2,3-Dihydroquinazolin -4-ones against Malaria Vector Anopheles arabiensis, In Silico ADMET Prediction and Molecular Target Investigation.

Authors:  Katharigatta N Venugopala; Pushpalatha Ramachandra; Christophe Tratrat; Raquel M Gleiser; Subhrajyoti Bhandary; Deepak Chopra; Mohamed A Morsy; Bandar E Aldhubiab; Mahesh Attimarad; Anroop B Nair; Nagaraja Sreeharsha; Rashmi Venugopala; Pran Kishore Deb; Sandeep Chandrashekharappa; Hany Ezzat Khalil; Osama I Alwassil; Sara Nidal Abed; Yazan A Bataineh; Ramachandra Palenge; Michelyne Haroun; Shinu Pottathil; Meravanige B Girish; Sabah H Akrawi; Viresh Mohanlall
Journal:  Molecules       Date:  2020-03-13       Impact factor: 4.411
  4 in total

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