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Phosphonate Derivatives (phosphonate + derivative)

Distribution by Scientific Domains
Chemistry100%

Selected Abstracts

ChemInform Abstract: Anti-HIV Activity of Novel Phosphonate Derivatives of AZT, d4T, and ddA

CHEMINFORM, Issue 48 2001
A. G. Pokrovsky
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Novel ferrocenyl phosphonate derivatives.

APPLIED ORGANOMETALLIC CHEMISTRY, Issue 10 2010
Inhibition of serine hydrolases by ferrocene azaphosphonates
Abstract Owing to their unique properties, ferrocene compounds are gaining increasing interest for biological applications, particularly as enzyme inhibitors. Phosphonate derivatives including a ferrocenyl moiety were synthesized by reaction of dimethyl- and diphenylphosphite with ferrocenyl methyl maleimide. The ferrocenyl diphenyl phosphonate complex was characterized by X-ray diffraction. The ability of these organometallic compounds to inhibit the enzymatic activity of the serine esterases acetyl- and butyrylcholinesterase was investigated. It appeared that the new ferrocenyl phosphonates inhibited both enzymes by competitive, mixed or non competitve mechanisms with inhibition constants in the range 35,1000 µM. Both compounds also behave as slow time-dependent inactivators of butyrylcholinesterase. The presence of the ferrocenyl entity seems then to have a dramatic effect on the biochemical behavior of the systems. Copyright © 2010 John Wiley & Sons, Ltd. [source]

Synthesis of Conformationally Constrained Glutamic Acid Homologues and Investigation of Their Pharmacological Profiles

CHEMMEDCHEM, Issue 11 2007
Paola Conti Prof.
Abstract Homologation of the glutamic acid chain together with conformational constraint is a commonly used strategy to achieve selectivity towards different types of glutamate receptors. We investigated the effects of a further increase in the distance between the amino acid moiety and the distal carboxylate group of model compounds (±)- 1 and (±)- 2 on their activity/selectivity profiles. We therefore synthesized new derivatives (±)- 3,(±)- 6, which are homologues of glutamic acid containing three additional carbon units. Moreover, because the potency of NMDA antagonists can be markedly increased by replacing the distal carboxylate with the bioisosteric phosphonate group, we also prepared the corresponding phosphonate derivatives (±)- 7,(±)- 10. All new compounds were submitted to binding assays with iGluRs, and derivatives (±)- 3,(±)- 6 were also tested in second messenger assays at representative mGluR subtypes. All the applied structural modifications were detrimental to the interaction with NMDA receptors. Conversely, structural variation of the nonselective mGluR ligand (±)- 2 led to derivative (±)- 5, which behaved as a selective group,I metabotropic receptor antagonist. Notably, upon i.c.v. administration in DBA/2 mice, amino acid (±)- 5 produced a significant protection against audiogenic seizures, whereas it was inactive after i.p. administration. [source]