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Raymond J Bergeron

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Articles 28
Citations 155
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Recent Articles
1.
Ghayee H, Hatch H, Bergeron R, Hadrava Vanova K, Pacak K, Tevosian S
Eur J Clin Invest . 2024 Feb; 54(5):e14162. PMID: 38381501
No abstract available.
2.
Bergeron R, Bharti N, McManis J, Wiegand J
Bioorg Med Chem . 2015 Aug; 23(17):5954-71. PMID: 26231739
Extensive structure activity relationship (SAR) studies focused on the desferrithiocin [DFT, (S)-4,5-dihydro-2-(3-hydroxy-2-pyridinyl)-4-methyl-4-thiazolecarboxylic acid] pharmacophore have led to three different DFT analogs being evaluated clinically for the treatment of iron overload...
3.
Bergeron R, Wiegand J, McManis J, Bharti N
J Med Chem . 2014 Sep; 57(22):9259-91. PMID: 25207964
The successful search for orally active iron chelators to treat transfusional iron-overload diseases, e.g., thalassemia, is overviewed. The critical role of iron in nature as a redox engine is first...
4.
Bergeron R, Wiegand J, Bharti N, McManis J
J Med Chem . 2012 Aug; 55(16):7090-103. PMID: 22889170
Desferrithiocin (DFT, 1) is a very efficient iron chelator when given orally. However, it is severely nephrotoxic. Structure-activity studies with 1 demonstrated that removal of the aromatic nitrogen to provide...
5.
Bergeron R, Singh S, Bharti N
Tetrahedron . 2012 Apr; 67(18):3163-3169. PMID: 22539866
The synthesis of the Rhodococcus erythropolis siderophores heterobactins A and B, and the structurally related Nocardia heterobactin, is described. Two approaches for the assembly of these asymmetric ligand donor chelators...
6.
Bergeron R, Singh S, Bharti N, Jiang Y
Synthesis (Stuttg) . 2011 Oct; 2010(21):3631-3636. PMID: 22013282
Iron chelators have been shown to control the growth of cancer cells in culture by sequestering exogenous iron in the media. Thus, the ligands prevent cellular access to the metal....
7.
Bergeron R, Wiegand J, Bharti N, McManis J, Singh S
Biometals . 2010 Nov; 24(2):239-58. PMID: 21103911
The current solution to iron-mediated damage in transfusional iron overload disorders is decorporation of excess unmanaged metal, chelation therapy. The clinical development of the tridentate chelator deferitrin (1, Table 1)...
8.
Bergeron R, Bharti N, Wiegand J, McManis J, Singh S, Abboud K
J Med Chem . 2010 Mar; 53(7):2843-53. PMID: 20232803
(S)-2-(2,4-Dihydroxyphenyl)-4,5-dihydro-4-methyl-4-thiazolecarboxylic acid (2) was abandoned in clinical trials as an iron chelator for the treatment of iron overload disease because of its nephrotoxicity. However, subsequent investigations revealed that replacing the...
9.
Bergeron R, Bharti N, Singh S, McManis J, Wiegand J, Green L
J Med Chem . 2009 Jun; 52(12):3801-13. PMID: 19492834
A new target strategy in the development of bacterial vaccines, the induction of antibodies to microbial outer membrane ferrisiderophore complexes, is explored. A vibriobactin (VIB) analogue, with a thiol tether,...
10.
Bergeron R, Wiegand J, Singh S
Int J Radiat Biol . 2009 Apr; 85(4):348-61. PMID: 19399680
Purpose: Previous systematic structure-activity studies of the desferrithiocin (DFT) platform have allowed the design and synthesis of analogues and derivatives of DFT that retain the exceptional iron-clearing activity of the...