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Synthesis, activity, and molecular modeling of new 2, 4-dioxo-5-(naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues as potent aldose reductase inhibitors.
A series of 2,4-dioxo-5-(2-naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues have been prepared as aldose reductase inhibitors. In vitro inhibitory activities of bovine lens aldoseExpand
STUDIES ON SOME para‐SUBSTITUTED CLONIDINE DERIVATIVES THAT EXHIBIT AN α‐ADRENOCEPTOR STIMULANT ACTIVITY
1 α‐Adrenoceptor stimulant activity was determined for noradrenaline (NA), clonidine and a series of para‐substituted derivatives of clonidine on rat aortic strips, a rat brain synaptosomeExpand
Selective reduction of aromatic / aliphatic nitro groups by sodium sulfide.
Abstract Sodium sulfide can be used to reduce selectively aromatic / aliphatic nitro groups. In the absence of water, the aromatic nitro group can be reduced selectively in the presence of aExpand
A convenient synthesis of cis‐4‐(sulfomethyl)‐piperidine‐2‐carboxylic acid: NMR assignment
cis-4-(Sulfomethyl)piperidine-2-carboxylic acid was obtained in 22 to overall yield from 4-(hydroxymethyl) pyridine via the o-silyl N-oxide and trimethylsilylcyanide. The cis configuration of 5 wasExpand
Cardiotonic agents. 2. Synthesis and structure-activity relationships in a new class of 6-, 7-, and 8-pyridyl-2(1H)-quinolone derivatives.
A series of 6-, 7-, and 8-pyridyl-2(1H)-quinolone derivatives with various quinolone substitutents (CH3, Cl, OH, OCH3) was prepared by arylation of pyridine with quinolone via a diazotizedExpand
New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent beta-adrenergic blocking properties.
The synthesis of R-(+) and S-(-) isomers of O-[3-tert-butylamino)-2-hydroxypropyl] cyclopropyl methyl ketone oxime (falintolol) is described. The syn and anti isomers of falintolol were obtained inExpand
Synthesis and beta-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers.
We describe the synthesis and pharmacological properties of two new series of aliphatic and alicyclic beta-adrenergic blockers, most of them containing a cyclopropyl ring. They belong either toExpand
Clonidine and related analogues. Quantitative correlations.
Twenty-two structural derivatives of clonidine [2-(2,6-dichlorophenylimino)imidazolidine] have been synthesized and their main physicochemical parameters (log P, deltaRM, pKa) determined.Expand
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