Studies in the time course of the response of rabbit polymorphonuclear leukocytes (PMN's) to the complement-associated chemotactic factor have revealed that the response is virtually complete by 60 min with less than 15% additionally responding cells thereafter. Phosphonate esters with a well defined capacity to inhibit serine esterases have been used to study the cell-associated enzymes of the...

The p-nitrophenyl ethyl phosphonate esters have been shown to inhibit complement-dependent erythrophagocytosis when exposed to guinea pig polymorphonuclear leukocytes prior to the initiation of phagocytosis. Inhibition of phagocytosis occurred in a manner characteristic of the well-defined capacity of phosphonate esters to inactivate serine esterases: inhibition was irreversible, dependent upon...

reaction of dialkyl acetylenedicarboxylates 1a-c andpyrrole derivatives 2a-e in the presence of triphenylphosphite (tpp) was investigated and the effect of the pyrrole substitution was established. diastereoselectivity is observed with pyrroles, 2a,b, yieldingphosphonate ester derivatives 3a-f and 4,and their relative configuration is determined by 1h/13c and 31p nmr and confirmed by single x-r...

It was shown in the preceding paper that incubation of the rabbit polymorphonuclearleukocyteswith phosphonate esters leads to an irreversible inhibition of the ability of the leukocyte to respond to the chemotactic factor. This "cell-dependent inhibition" was attributed to the inactivation by the phosphonates of an esterase existing in or on the leukocyte in an already activated state. As shown...

Monoaryl phosphonate esters, designated as analogs of the transition state in the hydrolysis of carboxylic esters, were synthesized and used as haptens to generate specific monoclonal antibodies. Some of these antibodies react with cognate aryl carboxylic esters to release a fluorescent alcohol. The reaction appears to be stoichiometric; however, the activity is slowly regenerated under alkalin...

A continuous protocol for the two-carbon homologation of esters to α,β-unsaturated esters is described. This multireactor homologation telescopes an ester reduction, phosphonate deprotonation, and Horner-Wadsworth-Emmons olefination, thus converting a three-operation procedure into a single, uninterrupted system that eliminates the need for isolation or purification of the aldehyde intermediate...

Radical reaction of [60]fullerene with phosphonate esters mediated by manganese(III) acetate in chlorobenzene afforded singly-bonded fullerene dimers, of which the individual meso and racemic isomers could be unexpectedly separated out for the first time.

Fresh normal serum treated with immune complexes is chemotactic for polymorphonudear leukocytes (PMN's) from a variety of species (1, 2). The factor in treated serum causing specific directional migration of PMN's has been identified as a molecular complex consisting of the fifth (C'5), sixth (C~6), and probably seventh (CtT) components of complement (2, 3). The manner by which the chemotactic ...

Theoretical insights elucidate a series of active phosphonate esters application in preparation of Cephalosporin antibiotics’ intermediate. The B3LYP/6-311+G(d,p) method was employed to obtain the stable equilibrium geometries including comparing to the AE-active ester. It was found that the Ethyl-aminothiazoly Loximate (AT) molecule fragment is almost planar sheet, but it is almost perpendicul...

Phosphonodepsipeptides are phosphorus analogues of depsipeptides and phosphonate-linked naturally occurring peptides. They more stable than phosphonopeptides have been widely applied as enzyme inhibitors, haptens for the production antibodies, biological agents, prodrugs. The synthetic strategies towards phosphonodepsipeptides reviewed, including phosphonylation hydroxy esters with phosphonochl...