Biomedical subjects

E G Corley

Publications and source records attributed to E G Corley.

6 recordsLinked to original sources

PubMed2000

A practical synthesis of a COX-2-specific inhibitor.

A number of synthetic strategies to the Cox-2 specific inhibitor 1 have been described. These studies have led to the identification of a novel pyridine construction using annulation of ketone 2 using a vinamidinium species 29 and ammonia in 97% assay yield. Three approaches to the synthesis of ketone 2 are described that allow for its preparation in large quantities in >65% overall yield from methyl 6-methylnicotinate.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMed2000

An efficient preparation of vinamidinium hexafluorophosphate salts.

Substituted acetic acids or acetyl chlorides react with phosphorus oxychloride in DMF to yield the vinamidinium salts 3a-j in moderate to excellent recrystallized yields (28-90%). The cations are conveniently isolated as their hexafluorophosphate salts, which are easily handled nonhygroscopic solids. The nitro compound 3l is prepared in 91% yield by nitration of the parent vinamidinium 3k. The X-ray crystal structure is reported for the 2-phenyl isomer 3e and displays minimal overlap of the two pi-systems.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMed2000

Annulation of ketones with vinamidinium hexafluorophosphate salts: an efficient preparation of trisubstituted pyridines.

alpha-Aryl ketones react with vinamidinium hexafluorophosphate salts to give access to the corresponding 3-arylpyridines. The annulation reactions proceed in good to excellent yields with vinamidinium salts containing electron-withdrawing groups at the beta-position (R(2)). The reaction was applied to the preparation of the COX-2 specific inhibitor 5-chloro-3-(4-methylsulfonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine (1), as well as a series of analogues.

Cyclooxygenase Inhibitors↗

PubMed1999

Interleukin-10-induced CD8 cell proliferation.

Interleukin (IL)-10, a product of T helper 2 (Th2) lymphocytes, has been shown to be an important regulator of lymphoid and myeloid cells, inhibiting mitogen, peptide and alloantigen-induced T-cell proliferation and IL-2 production. The microenvironment at the time of cell activation, notably the presence or absence of cytokines such as IL-10, interferon-gamma (IFN-gamma) and IL-2, is believed to determine the lineage and magnitude of cell-mediated responses. In this study, we show that recombinant human IL-10 (rhIL-10) exerts a dose-dependent inhibitory effect on human peripheral blood mononuclear cells stimulated in vitro, when these cells have not previously been exposed to rhIL-10. Furthermore, incubation of these cells with high doses of rhIL-10, either before or at the time of activation, results in inhibition which is followed several days later by the emergence of a population of CD8 positive cells. This rhIL-10-responsive CD8, positive cell population still emerges even when the cells are washed following incubation with rhIL-10 prior to cell activation. Using purified CD8 populations this was shown to be a direct action of rhIL-10 on CD8 cells and not via CD4 positive cells and monocytes. This finding was only observed when cells were activated with a cross-linking anti-CD3 antibody and not when activated with phorbol-12-mystrate-13-acetate (PMA) and calcium ionophore (CaIon), suggesting that the effect is mediated through cell-surface receptors. Analysis of CD8 positive clones reveal production of Tc2 patterns of cytokines and reduced cell cytotoxicity to allogeneic, natural killer and lymphokine activated cell targets.

Antibodies, Monoclonal↗

PubMed1986

A novel receptive area of key importance for the onset of diving responses in the duck.

We have found that the stimulation of the mucosa of the rhinopharynx elicits apnea and bradycardia in the duck. This appears to be the most important area involved in the production of diving responses. The laryngeal mucosa and other areas, as the external nares, were found to be of lesser relevance. We have also observed that visual and thermal stimuli may participate in the elicitation of the responses to submersion.

Acoustic Stimulation↗

PubMed1982

Localization of abscess with an iodinated synthetic chemotactic peptide.

N-formyl Nle-Leu-Phe-Nle-Tyr-Lys is a potent synthetic chemotactic peptide (CP), which binds to chemotactic receptors of neutrophils with high affinity. Because the peptide contains a tyrosine moiety, it can be readily labeled with a radioactive iodine. In this study, we investigated the possibility of abscess localization by i.v. administration of this radioiodinated CP. The peptide was iodinated with 125I using chloramine-T and purified using Bio-Gel P-2 chromatography. The final preparation had a purity of 88.5 +/- 3.8% (n = 6) and a specific radioactivity of 600-800 ci/mM. The iodinated CP bound to rabbit neutrophils specifically; its binding could be prevented by non-labeled CP. When 4-6 ng of 125-I-CP per kg body weight was injected into abscess-bearing rabbits, there was an immediate, but transient neutropenia, followed by a rebound neutrophilia. The abscess to muscle (A/M) ratio was 11.6 +/- 1.1 at 6 hrs and 11.0 +/- 4.7 at 24 hrs after injection; while the abscess to blood (A/B) ratio was 0.9 +/- 0.2 and 3.7 +/- 0.6 at 6 and 24 hrs post injection, respectively. Control animals injected with Na125I revealed an A/M ratio of 2.9 +/- 0.2 and an A/B ratio of 0.9 +/- 0.3 at 6 hrs after injection. Analysis of the radioactivity in the blood after 125I-CP administration, revealed that the majority (less than 87%) of the radioactivity was present as 125I-CP in the plasma fraction. Our results suggest that radioiodinated synthetic CP shows promise for abscess localization. However, further refinement of the method is required.

Abscess↗