Joseph Sanchez - Academia.edu (original) (raw)
Papers by Joseph Sanchez
The William and Mary Quarterly, 1993
The Western Historical Quarterly, 1999
Pacific Historical Review, 2000
The Hispanic American Historical Review, 1981
The Hispanic American Historical Review, 1976
The American Historical Review, 2008
... It was truly a pleasure to review. charles ewen, East Carolina University doi 10.1215/0018216... more ... It was truly a pleasure to review. charles ewen, East Carolina University doi 10.1215/00182168-2009-010 No Settlement, No Conquest: A History of the Coronado Entrada. By richard flint. ... This is exactly what Richard Flint's narrative of the Coronado expedition does. ...
Hispanic Review, 1936
... Later on, the idea occurred to Castillejo to use the third and fourth acts of his play as the... more ... Later on, the idea occurred to Castillejo to use the third and fourth acts of his play as the basis of a new composition which far outgrew the setting which it had in the Farsa de la Constanza. JP WICKERSHAM CRAWFORD University of Pennsylvania ... JOSEPH SANCHEZ ...
ChemInform, 2008
Simple Synthesis of 4-Substituted 1(2H)-Isoquinolinones via Electrophilic Trapping of Lithiated M... more Simple Synthesis of 4-Substituted 1(2H)-Isoquinolinones via Electrophilic Trapping of Lithiated Mono-and Dianion Precursors. -Simple and convenient routes to the title 4-substituted isoquinolinones [cf. (VI), (IX)] from readily available precursors are developed. These products are found to be inhibitors of poly (ADP-ribose)polymerase. -(SERCEL
Journal of Organic Chemistry, 1973
Journal of Organic Chemistry, 1974
A series of phenylpyrazole and -triazole diphenylcarbinols have been converted to the hydrochlori... more A series of phenylpyrazole and -triazole diphenylcarbinols have been converted to the hydrochloride salts of the carbinyl chlorides and thence to the corresponding azafulvenes by dehydrohalogenation with triethylamine at -78". Irradiation of the triazafulvenes at this temperature gave a mixture of isolable products which implicate azatriafulvene and azete as possible unstable precursors. The latter intermediate may also be involved in the photochemical decomposition of triphenvltriazine, which was also examined. The diazafulvenes prepared proved isolable but photochemically inert.
Journal of Heterocyclic Chemistry, 1994
Starting with 1,1-dimethoxy-2-propanone (1), 6-formyl-1,2-dihydro-2-oxo-3-pyridinecarboxylic acid... more Starting with 1,1-dimethoxy-2-propanone (1), 6-formyl-1,2-dihydro-2-oxo-3-pyridinecarboxylic acid (5a) has been prepared in large quantities by a highly efficient, 4-step synthesis. This compound, along with its one carbon homologue, 6-acetyl-1,2-dihydro-2-oxo-3-pyridinecarboxylic acid (5b) has been reacted with several carbonyl derivative forming reagents to provide a series of side chains for β-lactams. Among these carbonyl derivatives are styrylamides which were prepared from Wittig and Horner-Emmons reagents. The preparation of the phosphonium salts and phosphonate esters is also described.
Journal of Medicinal Chemistry, 1995
The dramatic increase in drug resistant Mycobacterium tuberculosis has caused a resurgence in res... more The dramatic increase in drug resistant Mycobacterium tuberculosis has caused a resurgence in research targeted toward these organisms. As part of a systematic study to optimize the quinolone antibacterials against mycobacteria, we have prepared a series of N-1-phenyl-substituted derivatives to explore the effect of increasing lipophilicity on potency at this position. The compounds, synthesized by the modification of a literature procedure, were evaluated for activity against Gram-negative and Gram-positive bacteria, Mycobacterium fortuitum and Mycobacterium smegmatis, and the results correlated with log P, pKa, and other attributes. The activity of the compounds against the rapidly growing, less hazardous organism M. fortuitum was used as a measure of M. tuberculosis activity. The results demonstrate that increasing lipophilic character by itself does not correlate with increased potency against mycobacteria. Rather, intrinsic activity against Gram-negative and/or Gram-positive bacteria is the governing factor for corresponding activity against mycobacteria.
Journal of Medicinal Chemistry, 1996
The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has ... more The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has demonstrated the need for alternative chemotherapy against Mycobacterium tuberculosis. As part of a study to optimize the quinolone antibacterials against M. tuberculosis, we have prepared a series of N-1- and C-7-substituted quinolones to examine specific structure-activity relationships between modifications of the quinolone at these two positions and activity against mycobacteria. The compounds, synthesized by literature procedures, were evaluated for activity against Mycobacterium fortuitum and Mycobacterium smegmatis as well as Gram-negative and Gram-positive bacteria. The activity of the compounds against M. fortuitum was used as a barometer of M. tuberculosis activity. The results demonstrate that (i) the activity against mycobacteria was related more to antibacterial activity than to changes in the lipophilicity of the compounds, (ii) the antimycobacterial activity imparted by the N-1 substituent was in the order tert-butyl > or = cyclopropyl > 2,4-difluorophenyl > ethyl approximately cyclobutyl > isopropyl, and (iii) substitution with either piperazine or pyrrolidine heterocycles at C-7 afforded similar activity against mycobacteria.
Journal of Medicinal Chemistry, 1995
A series of 1-cyclopropyl-6-fluoro-8-alkoxy (8-methyoxy and 8-ethoxy)-quionoline-3-carboxylic aci... more A series of 1-cyclopropyl-6-fluoro-8-alkoxy (8-methyoxy and 8-ethoxy)-quionoline-3-carboxylic acids and 1-cyclopropyl-5-amino-6-fluoro-8-alkoxyquinoline-3-carboxylic acids has been prepared and evaluated for antibacterial activity. In addition, they were also compared to quinolones with classic substitution at C8 (H, F, Cl) and the naphthyridine nucleus in a phototoxicity and mammalian cell cytotoxicity assay. The series of 8-methoxyquinolones had antibacterial activity against Gram-positive, Gram-negative, and anaerobic bacteria equivalent to the most active 8-substituted compounds (8-F and 8-Cl). There was also a concomitant reduction in several of the potential side effects (i.e., phototoxicity and clonogenicity) compared to the most active quinolones with classic substitution at C-8. The 8-ethoxy derivatives had an even better safety profile but were significantly less active (2-3 dilutions) in the antibacterial assay.
The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has ... more The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has demonstrated the need for alternative chemotherapy against Mycobacterium tuberculosis. As part of a study to optimize the quinolone antibacterials against M. tuberculosis, we have prepared a series of N-1- and C-7-substituted quinolones to examine specific structure-activity relationships between modifications of the quinolone at these two positions and activity against mycobacteria. The compounds, synthesized by literature procedures, were evaluated for activity against Mycobacterium fortuitum and Mycobacterium smegmatis as well as Gram-negative and Gram-positive bacteria. The activity of the compounds against M. fortuitum was used as a barometer of M. tuberculosis activity. The results demonstrate that (i) the activity against mycobacteria was related more to antibacterial activity than to changes in the lipophilicity of the compounds, (ii) the antimycobacterial activity imparted by the N-1 substituent was in the order tert-butyl > or = cyclopropyl > 2,4-difluorophenyl > ethyl approximately cyclobutyl > isopropyl, and (iii) substitution with either piperazine or pyrrolidine heterocycles at C-7 afforded similar activity against mycobacteria.
The William and Mary Quarterly, 1993
The Western Historical Quarterly, 1999
Pacific Historical Review, 2000
The Hispanic American Historical Review, 1981
The Hispanic American Historical Review, 1976
The American Historical Review, 2008
... It was truly a pleasure to review. charles ewen, East Carolina University doi 10.1215/0018216... more ... It was truly a pleasure to review. charles ewen, East Carolina University doi 10.1215/00182168-2009-010 No Settlement, No Conquest: A History of the Coronado Entrada. By richard flint. ... This is exactly what Richard Flint's narrative of the Coronado expedition does. ...
Hispanic Review, 1936
... Later on, the idea occurred to Castillejo to use the third and fourth acts of his play as the... more ... Later on, the idea occurred to Castillejo to use the third and fourth acts of his play as the basis of a new composition which far outgrew the setting which it had in the Farsa de la Constanza. JP WICKERSHAM CRAWFORD University of Pennsylvania ... JOSEPH SANCHEZ ...
ChemInform, 2008
Simple Synthesis of 4-Substituted 1(2H)-Isoquinolinones via Electrophilic Trapping of Lithiated M... more Simple Synthesis of 4-Substituted 1(2H)-Isoquinolinones via Electrophilic Trapping of Lithiated Mono-and Dianion Precursors. -Simple and convenient routes to the title 4-substituted isoquinolinones [cf. (VI), (IX)] from readily available precursors are developed. These products are found to be inhibitors of poly (ADP-ribose)polymerase. -(SERCEL
Journal of Organic Chemistry, 1973
Journal of Organic Chemistry, 1974
A series of phenylpyrazole and -triazole diphenylcarbinols have been converted to the hydrochlori... more A series of phenylpyrazole and -triazole diphenylcarbinols have been converted to the hydrochloride salts of the carbinyl chlorides and thence to the corresponding azafulvenes by dehydrohalogenation with triethylamine at -78". Irradiation of the triazafulvenes at this temperature gave a mixture of isolable products which implicate azatriafulvene and azete as possible unstable precursors. The latter intermediate may also be involved in the photochemical decomposition of triphenvltriazine, which was also examined. The diazafulvenes prepared proved isolable but photochemically inert.
Journal of Heterocyclic Chemistry, 1994
Starting with 1,1-dimethoxy-2-propanone (1), 6-formyl-1,2-dihydro-2-oxo-3-pyridinecarboxylic acid... more Starting with 1,1-dimethoxy-2-propanone (1), 6-formyl-1,2-dihydro-2-oxo-3-pyridinecarboxylic acid (5a) has been prepared in large quantities by a highly efficient, 4-step synthesis. This compound, along with its one carbon homologue, 6-acetyl-1,2-dihydro-2-oxo-3-pyridinecarboxylic acid (5b) has been reacted with several carbonyl derivative forming reagents to provide a series of side chains for β-lactams. Among these carbonyl derivatives are styrylamides which were prepared from Wittig and Horner-Emmons reagents. The preparation of the phosphonium salts and phosphonate esters is also described.
Journal of Medicinal Chemistry, 1995
The dramatic increase in drug resistant Mycobacterium tuberculosis has caused a resurgence in res... more The dramatic increase in drug resistant Mycobacterium tuberculosis has caused a resurgence in research targeted toward these organisms. As part of a systematic study to optimize the quinolone antibacterials against mycobacteria, we have prepared a series of N-1-phenyl-substituted derivatives to explore the effect of increasing lipophilicity on potency at this position. The compounds, synthesized by the modification of a literature procedure, were evaluated for activity against Gram-negative and Gram-positive bacteria, Mycobacterium fortuitum and Mycobacterium smegmatis, and the results correlated with log P, pKa, and other attributes. The activity of the compounds against the rapidly growing, less hazardous organism M. fortuitum was used as a measure of M. tuberculosis activity. The results demonstrate that increasing lipophilic character by itself does not correlate with increased potency against mycobacteria. Rather, intrinsic activity against Gram-negative and/or Gram-positive bacteria is the governing factor for corresponding activity against mycobacteria.
Journal of Medicinal Chemistry, 1996
The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has ... more The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has demonstrated the need for alternative chemotherapy against Mycobacterium tuberculosis. As part of a study to optimize the quinolone antibacterials against M. tuberculosis, we have prepared a series of N-1- and C-7-substituted quinolones to examine specific structure-activity relationships between modifications of the quinolone at these two positions and activity against mycobacteria. The compounds, synthesized by literature procedures, were evaluated for activity against Mycobacterium fortuitum and Mycobacterium smegmatis as well as Gram-negative and Gram-positive bacteria. The activity of the compounds against M. fortuitum was used as a barometer of M. tuberculosis activity. The results demonstrate that (i) the activity against mycobacteria was related more to antibacterial activity than to changes in the lipophilicity of the compounds, (ii) the antimycobacterial activity imparted by the N-1 substituent was in the order tert-butyl > or = cyclopropyl > 2,4-difluorophenyl > ethyl approximately cyclobutyl > isopropyl, and (iii) substitution with either piperazine or pyrrolidine heterocycles at C-7 afforded similar activity against mycobacteria.
Journal of Medicinal Chemistry, 1995
A series of 1-cyclopropyl-6-fluoro-8-alkoxy (8-methyoxy and 8-ethoxy)-quionoline-3-carboxylic aci... more A series of 1-cyclopropyl-6-fluoro-8-alkoxy (8-methyoxy and 8-ethoxy)-quionoline-3-carboxylic acids and 1-cyclopropyl-5-amino-6-fluoro-8-alkoxyquinoline-3-carboxylic acids has been prepared and evaluated for antibacterial activity. In addition, they were also compared to quinolones with classic substitution at C8 (H, F, Cl) and the naphthyridine nucleus in a phototoxicity and mammalian cell cytotoxicity assay. The series of 8-methoxyquinolones had antibacterial activity against Gram-positive, Gram-negative, and anaerobic bacteria equivalent to the most active 8-substituted compounds (8-F and 8-Cl). There was also a concomitant reduction in several of the potential side effects (i.e., phototoxicity and clonogenicity) compared to the most active quinolones with classic substitution at C-8. The 8-ethoxy derivatives had an even better safety profile but were significantly less active (2-3 dilutions) in the antibacterial assay.
The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has ... more The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has demonstrated the need for alternative chemotherapy against Mycobacterium tuberculosis. As part of a study to optimize the quinolone antibacterials against M. tuberculosis, we have prepared a series of N-1- and C-7-substituted quinolones to examine specific structure-activity relationships between modifications of the quinolone at these two positions and activity against mycobacteria. The compounds, synthesized by literature procedures, were evaluated for activity against Mycobacterium fortuitum and Mycobacterium smegmatis as well as Gram-negative and Gram-positive bacteria. The activity of the compounds against M. fortuitum was used as a barometer of M. tuberculosis activity. The results demonstrate that (i) the activity against mycobacteria was related more to antibacterial activity than to changes in the lipophilicity of the compounds, (ii) the antimycobacterial activity imparted by the N-1 substituent was in the order tert-butyl > or = cyclopropyl > 2,4-difluorophenyl > ethyl approximately cyclobutyl > isopropyl, and (iii) substitution with either piperazine or pyrrolidine heterocycles at C-7 afforded similar activity against mycobacteria.