287971-19-1Relevant academic research and scientific papers
The first total synthesis of gobichelin B: A mixed-ligand siderophore of: Streptomyces sp. NRRL F-4415
Sridhar, Perali Ramu,Venkatesh,Kalesha, Shaik,Sudharani, Chalapala
, p. 3732 - 3740 (2018/05/30)
The first total synthesis of a structurally diverse mixed ligand siderophore, gobichelin B produced by Streptomyces sp. NRRL F-4415, is reported. The systematic assembly of the building blocks to synthesize Gob-B 1st half and Gob-B 2nd half and subsequent coupling of these two fragments followed by global deprotection using Pearlman's catalyst led to the isolation of gobichelin B in excellent yield and purity.
Antibacterial Agents
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Page/Page column 33, (2009/01/20)
The invention provides compounds of formula (I) and salts thereof: R1-L-R2—B wherein R1, L, R2, and B have any of the values defined herein, as well as compositions comprising such compounds, and therapeutic methods comprising the administration of such compounds or salts. The compounds block siderophore production in bacteria and are useful as antibacterial agents.
Salicylanilides: Selective inhibitors of interleukin-12p40 production
Brown, Michael E.,Fitzner, Jeffrey N.,Stevens, Tracey,Chin, Wilson,Wright, Clifford D.,Boyce, Jim P.
experimental part, p. 8760 - 8764 (2009/04/05)
Interleukin (IL)-12p40, a subunit component of both IL-12 and IL-23, is being widely studied for its role in inflammatory disease. As part of an effort to profile cellular signaling pathways across different cell types, we report salicylanilide inhibitors of IL-12p40 production in stimulated dendritic cells. Based on a hypothesis that a desirable therapeutic profile is one that could block IL-12p40 but not IL-6 production, we engaged in directed analoging. This resulted in salicylanilides with similar IL-12p40 related potency but enhanced selectivity relative to IL-6 production.
Rationally-designed nucleoside antibiotics that inhibit siderophore biosynthesis of Mycobacterium tuberculosis
Somu, Ravindranadh V.,Boshoff, Helena,Qiao, Chunhua,Bennett, Eric M.,Barry III, Clifton E.,Aldrich, Courtney C.
, p. 31 - 34 (2007/10/03)
A rationally designed nucleoside inhibitor of Mycobacterium tuberculosis growth (MIC99 = 0.19 μM) that disrupts siderophore biosynthesis was identified. The activity is due to inhibition of the adenylate-forming enzyme MbtA which is involved in
Synthesis and physicochemical assessment of novel 2-substituted 3-hydroxypyridin-4-ones, novel iron chelators
Moridani, Majid Y.,Tilbrook, Gary S.,Khodr, Hicham H.,Hider, Robert C.
, p. 349 - 364 (2007/10/03)
Novel 3-hydroxypyridin-4-one containing tridentate ligands were synthesised and their physicochemical properties characterised, including ionisation constants and stoichiometric titration with Fe(III). There is an urgent demand for orally active iron chelators with potential for the treatment of thalassaemia. In principle, tridentate ligands are likely to be more kinetically stable than bidentate molecules, but to date no satisfactory molecules have been identified. Fe(III) stability constants were assessed by competition with the hexadentate ligand EDTA. In all cases no evidence was found for a tridentate mode of iron chelation; instead the ligands behaved as bidentate hydroxypyridinones. As a consequence they provide no advantage over the more simple alkyl hydroxypyridinones.
