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Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165.
A rational series of compounds based on UB-165 presents a systematic approach to defining subtype specific pharmacophores and it is clear that further refinements of this model are necessary in order to describe adequately the structural and electronic demands associated with this nAChR subtype. Expand
C-H activation and palladium migration within Biaryls under Heck reaction conditions.
Under the conditions used, crossover is increasingly favored when electron-deficient arenes are involved and products derived from transfer onto the pyridine ring have also been observed. Expand
Discovery of Molidustat (BAY 85‐3934): A Small‐Molecule Oral HIF‐Prolyl Hydroxylase (HIF‐PH) Inhibitor for the Treatment of Renal Anemia
The discovery, synthesis, structure–activity relationship (SAR), and proposed binding mode of novel 2,4‐diheteroaryl‐1,2‐dihydro‐3H‐pyrazol‐3‐ones as orally bioavailable HIF‐PH inhibitors for the treatment of anemia are described. Expand
Analysis of the changing birth prevalence of neural tube defects in Hungary.
The birth prevalence of neural tube defects had a significant decrease in Hungary from the sixties till 1978 and after this a slight but not significant increase was registered, with only one obvious finding, a negative correlation with the standard of living of the population. Expand
Directed deprotonation-transmetalation as a route to substituted pyridines.
Regioselective C-4 deprotonation of 3-bromopyridine, followed by Li/Zn transmetalation and Pd-mediated coupling processes, provides a flexible entry to 4-substituted and 3,4-disubstituted pyridines.Expand
δ‐Peptide Analogues of Pyranosyl‐RNA, Part 1 , Nucleo‐δ‐peptides Derived from Conformationally Constrained Nucleo‐δ‐amino Acids: Preparation of Monomers
Cyclic nucleo-δ-amino acids that constitute monomers of a conformationally constrained nucleo-δ-peptide base-pairing system have been prepared. Their synthesis starts with an enantioselectivelyExpand
A novel highly stereoselective total synthesis of epothilone B and of its (12R,13R) acetonide
Abstract Stereoselective syntheses of epothilone B ( 1 ) and its novel derivative 2 are described. Key steps are the formation of intermediate 3 via Sharpless AD-reaction andExpand
New Solutions to the C‐12,13 Stereoproblem of Epothilones B and D; Synthesis of a 12,13‐Diol‐Acetonide Epothilone B Analog
New approaches are described to the synthesis of epothilone B and a 12,13-diol-acetonide derivative. Specifically the (12Z) double bond is formed quantitatively by a silicon-tethered ring-closingExpand
Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity.
Four racemic phenyl-substituted analogues 3-6 of the potent nicotinic agonist UB-165 1 have been synthesised and evaluated against the alpha(4)beta(2), alpha(3)beta(4), and alpha(7) neuronalExpand
Directed deprotonation-transmetallation of 4-bromopyridine: Flexible routes to substituted pyridines
Halide-directed deprotonation and Li-Zn exchange of 4-bromopyridine 4 provides organozinc 6, which undergoes Pd-mediated coupling to give the 3-aryl-4-bromopyridines 7. Further substitution isExpand