Search

Your search keyword '"Boswell G"' showing total 206 results
Start Over Author "Boswell G"
206 results on '"Boswell G"'

6. Dedication: William B. Leffler.

Author

Kennedy, David S., Moriarty, Herbert B., Jr., Marr, Freeman C., and Boswell, G. Harvey

Subjects
Judges -- Testimonials
Published
1998

11. A convenient large-scale synthesis of 4-fluoro-1-naphthaldehyde and its aromatic nucleophilic substitution reactions

Author

Boswell, G. Evan and Licause, Joseph F.

Subjects
Naphthalene -- Research, Substitution reactions -- Analysis, Biological sciences, Chemistry
Abstract

Regiospecific formylation of 1-fluoronaphtalene results in the formation of 4-fluoro-1-naphthaldehyde (2). The resulting compound can be used for the synthesis of various substituted naphthalenes. Baeyer-Villiger oxidation of compound 2 followed by hydrolysis of formate ester results in the formation of 4-fluoro-1-naphthol. Synthesis of naphthalene derivative is discussed.

Published
1995

24. Neuromuscular Blocking Activity and Therapeutic Potential of Mixed-Tetrahydroisoquinolinium Halofumarates and Halosuccinates in Rhesus Monkeys

Author

Boros, Eric E., primary, Samano, Vicente, additional, Ray, John A., additional, Thompson, James B., additional, Jung, David K., additional, Kaldor, Istvan, additional, Koble, Cecilia S., additional, Martin, Michael T., additional, Styles, Virgil L., additional, Mook, Robert A., additional, Feldman, Paul L., additional, Savarese, John J., additional, Belmont, Matthew R., additional, Bigham, Eric C., additional, Boswell, G. Evan, additional, Hashim, Mir A., additional, Patel, Sanjay S., additional, Wisowaty, James C., additional, Bowers, Gary D., additional, Moseley, Caroline L., additional, Walsh, John S., additional, Reese, Mindy J., additional, Rutkowske, Randy D., additional, Sefler, Andrea M., additional, and Spitzer, Timothy D., additional

Published
2003
Full Text
View/download PDF

30. Bis- and Mixed-Tetrahydroisoquinolinium Chlorofumarates: New Ultra-Short-Acting Nondepolarizing Neuromuscular Blockers

Author

Boros, Eric E., primary, Bigham, Eric C., additional, Boswell, G. Evan, additional, Mook, Robert A., additional, Patel, Sanjay S., additional, Savarese, John J., additional, Ray, John A., additional, Thompson, James B., additional, Hashim, Mir A., additional, Wisowaty, James C., additional, Feldman, Paul L., additional, and Samano, Vicente, additional

Published
1999
Full Text
View/download PDF

31. N-(2-Benzoylphenyl)-l-tyrosine PPARγ Agonists. 2. Structure−Activity Relationship and Optimization of the Phenyl Alkyl Ether Moiety

Author

Collins, Jon L., primary, Blanchard, Steven G., additional, Boswell, G. Evan, additional, Charifson, Paul S., additional, Cobb, Jeff E., additional, Henke, Brad R., additional, Hull-Ryde, Emily A., additional, Kazmierski, Wieslaw M., additional, Lake, Debra H., additional, Leesnitzer, Lisa M., additional, Lehmann, Jürgen, additional, Lenhard, James M., additional, Orband-Miller, Lisa A., additional, Gray-Nunez, Yolanda, additional, Parks, Derek J., additional, Plunkett, Kelli D., additional, and Tong, Wei-Qin, additional

Published
1998
Full Text
View/download PDF

46. Tacrolimus pharmacokinetics in BMT patients.

Author

Boswell, G W, Bekersky, I, Fay, J, Wingard, J, Antin, J, Weisdorf, D, Maher, R, Fitzsimmons, W, and Nash, R

Subjects
*TACROLIMUS, *PHARMACOKINETICS, *BONE marrow transplantation
Abstract

The pharmacokinetics of tacrolimus following its administration as monotherapy or in combination with corticosteroids or methotrexate to 31 BMT patients are presented. All patients received i.v. tacrolimus initially and were subsequently switched to p.o. dosing. Patients received methotrexate by i.v. bolus on post-transplantation days 1, 3, 6 and 11. Patients were started on i.v. corticosteroids beginning on post-transplantation day 7. The noncompartmental pharmacokinetics of tacrolimus based on whole blood concentrations were determined following the i.v. and p.o. doses and were not different at steady-state compared to a single dose. The mean terminal elimination half-life of tacrolimus was 18.2 h following i.v. administration; the total body clearance was 71 ml/h/kg, the volume of distribution was 1.67 l/kg. Co-administration of methylprednisolone or methotrexate did not significantly alter tacrolimus pharmacokinetics. The p.o. bioavailability was 31–49%. Trough blood concentrations (Cmin) at 0 h (pre-dose) and 12 h (post-dose) correlated well to AUC0–12 indicating that, as in solid organ transplantation, Cmin was a good index of drug exposure. Correlation at 0 h (r = 0.92) and at 12 h (r = 0.93) indicate that either time point can be used for therapeutic drug monitoring in patient management. [ABSTRACT FROM AUTHOR]

Published
1998
Full Text
View/download PDF

48. N-(2-Benzoylphenyl)-<SCP>l</SCP>-tyrosine PPARγ Agonists. 2. Structure−Activity Relationship and Optimization of the Phenyl Alkyl Ether Moiety

Author

Collins, J. L., Blanchard, S. G., Boswell, G. E., Charifson, P. S., Cobb, J. E., Henke, B. R., Hull-Ryde, E. A., Kazmierski, W. M., Lake, D. H., Leesnitzer, L. M., Lehmann, J., Lenhard, J. M., Orband-Miller, L. A., Gray-Nunez, Y., Parks, D. J., Plunkett, K. D., and Tong, W.-Q.

Abstract

We previously reported the identification of (2S)-((2-benzoylphenyl)amino)-3-{4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phenyl}propanoic acid (2) (PPARγ pKi = 8.94, PPARγ pEC50 = 9.47) as a potent and selective PPARγ agonist. We now report the expanded structure−activity relationship around the phenyl alkyl ether moiety by pursuing both a classical medicinal chemistry approach and a solid-phase chemistry approach for analogue synthesis. The solution-phase strategy focused on evaluating the effects of oxazole and phenyl ring replacements of the 2-(5-methyl-2-phenyloxazol-4-yl)ethyl side chain of 2 with several replacements providing potent and selective PPARγ agonists with improved aqueous solubility. Specifically, replacement of the phenyl ring of the phenyloxazole moiety with a 4-pyridyl group to give 2(S)-((2-benzoylphenyl)amino)-3-{4-[2-(5-methyl-2-pyridin-4-yloxazol-4-yl)ethoxy]phenyl}propionic acid (16) (PPARγ pKi = 8.85, PPARγ pEC50 = 8.74) or a 4-methylpiperazine to give 2(S)-((2-benzoylphenyl)amino)-3-(4-{2-[5-methyl-2-(4-methylpiperazin-1-yl)thiazol-4-yl]ethoxy}phenyl)propionic acid (24) (PPARγ pKi = 8.66, PPARγ pEC50 = 8.89) provided two potent and selective PPARγ agonists with increased solubility in pH 7.4 phosphate buffer and simulated gastric fluid as compared to 2. The second strategy took advantage of the speed and ease of parallel solid-phase analogue synthesis to generate a more diverse set of phenyl alkyl ethers which led to the identification of a number of novel, high-affinity PPARγ ligands (PPARγ pKi's 6.98−8.03). The combined structure−activity data derived from the two strategies provide valuable insight on the requirements for PPARγ binding, functional activity, selectivity, and aqueous solubility.

Published
1998

Catalog

Books, media, physical & digital resources
See catalog results