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Literature DB >> 16260134

Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5].

Frank Bennett¹, Anil K Saksena, Raymond G Lovey, Yi-Tsung Liu, Naginbhai M Patel, Patrick Pinto, Russel Pike, Edwin Jao, Viyyoor M Girijavallabhan, Ashit K Ganguly, David Loebenberg, Haiyan Wang, Anthony Cacciapuoti, Eugene Moss, Fred Menzel, Roberta S Hare, Amin Nomeir.

Abstract

As part of a detailed study, the syntheses, biological activities, and pharmacokinetic properties of hydroxylated analogues of the previously described broad spectrum antifungal agents, Sch 51048 (1), Sch 50001 (3), and Sch 50002 (4), are described. Based on an overall superior profile, one of the alcohols, Sch 56592 (2), was selected for clinical studies.

Entities: Chemical

Mesh：

Substances：

Year: 2005 PMID： 16260134 DOI： 10.1016/j.bmcl.2005.09.031

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

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Cited

6 in total

1. Efficacy, safety and feasibility of antifungal prophylaxis with posaconazole tablet in paediatric patients after haematopoietic stem cell transplantation.

Authors: Michaela Döring; Karin Melanie Cabanillas Stanchi; Manon Queudeville; Judith Feucht; Franziska Blaeschke; Patrick Schlegel; Tobias Feuchtinger; Peter Lang; Ingo Müller; Rupert Handgretinger; Werner J Heinz
Journal: J Cancer Res Clin Oncol Date: 2017-03-03 Impact factor: 4.553

2. Rational modification of a candidate cancer drug for use against Chagas disease.

Authors: James M Kraus; Christophe L M J Verlinde; Mandana Karimi; Galina I Lepesheva; Michael H Gelb; Frederick S Buckner
Journal: J Med Chem Date: 2009-03-26 Impact factor: 7.446

3. Enantioselective synthesis of 2,2-disubstituted tetrahydrofurans: palladium-catalyzed [3+2] cycloadditions of trimethylenemethane with ketones.

Authors: Barry M Trost; Dustin A Bringley
Journal: Angew Chem Int Ed Engl Date: 2013-03-12 Impact factor: 15.336

Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5].

1. Efficacy, safety and feasibility of antifungal prophylaxis with posaconazole tablet in paediatric patients after haematopoietic stem cell transplantation.

2. Rational modification of a candidate cancer drug for use against Chagas disease.

3. Enantioselective synthesis of 2,2-disubstituted tetrahydrofurans: palladium-catalyzed [3+2] cycloadditions of trimethylenemethane with ketones.

Review 4. Posaconazole : a review of its use in the prophylaxis of invasive fungal infections.

5. Ultrafast ¹H MAS NMR Crystallography for Natural Abundance Pharmaceutical Compounds.

Review 6. Drug strategies targeting CYP51 in neglected tropical diseases.

Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5].

1. Efficacy, safety and feasibility of antifungal prophylaxis with posaconazole tablet in paediatric patients after haematopoietic stem cell transplantation.

2. Rational modification of a candidate cancer drug for use against Chagas disease.

3. Enantioselective synthesis of 2,2-disubstituted tetrahydrofurans: palladium-catalyzed [3+2] cycloadditions of trimethylenemethane with ketones.

Review 4. Posaconazole : a review of its use in the prophylaxis of invasive fungal infections.

5. Ultrafast 1H MAS NMR Crystallography for Natural Abundance Pharmaceutical Compounds.

Review 6. Drug strategies targeting CYP51 in neglected tropical diseases.

5. Ultrafast ¹H MAS NMR Crystallography for Natural Abundance Pharmaceutical Compounds.