Search Results - "Heifetz, Carl L."

1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure activity relationships at N1 for the quinolone antibacterials by Domagala, John M, Heifetz, Carl L, Hutt, Marland P, Mich, Thomas F, Nichols, Jeffry B, Solomon, Marjorie, Worth, Donald F

“…A series of 18 1-substituted 7-[3-[(ethylamino)methyl]-1- pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinoline- carboxylic acids (N1 analogues of CI-934)…”
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New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids by Hagen, Susan E, Domagala, John M, Heifetz, Carl L, Sanchez, Joseph P, Solomon, Marjorie

“…A series of 7-(3-amino- or 3-aminomethyl-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-o xo-3-quinolinecarboxylic acids was synthesized and tested…”
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New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay by Domagala, John M, Hanna, Lori Doyle, Heifetz, Carl L, Hutt, Marland P, Mich, Thomas F, Sanchez, Joseph P, Solomon, Marjorie

“…A series of 60 newly synthesized and known quinolone antibacterials, including quinoline- and 1,8-naphthyridine-3-carboxylic acids,…”
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Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids by Sanchez, Joseph P, Domagala, John M, Hagen, Susan E, Heifetz, Carl L, Hutt, Marland P, Nichols, Jeffry B, Trehan, Ashok K

“…A series of 7,8-disubstituted 1-cyclopropyl-6-fluoroquinoline-3-carboxylic acids, 7-substituted 1-cyclopropyl-6-fluoro-1,8-naphthyridine-3-carboxylic acids,…”
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Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids by Hagen, Susan E, Domagala, John M, Heifetz, Carl L, Johnson, Judith

“…A series of 5-alkyl-1,7,8-trisubstituted-6-fluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids was prepared and evaluated for in vitro and in vivo…”
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Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity by Sanchez, Joseph P, Domagala, John M, Heifetz, Carl L, Priebe, Stephen R, Sesnie, Josephine A, Trehan, Ashok K

“…A series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)-6-fluoro-1,8-naphthyridine-3-carboxylic acids,…”
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7-Substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials by Domagala, John M, Hagen, Susan E, Heifetz, Carl L, Hutt, Marland P, Mich, Thomas F, Sanchez, Joseph P, Trehan, Ashok K

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1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid. New quinolone antibacterial with potent gram-positive activity by Domagala, John M, Heifetz, Carl L, Mich, Thomas F, Nichols, Jeffrey B

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Semisynthetic penicillins and cephalosporins containing the substituted 6-vinyl-1,2-dihydro-2-oxo- and 1,4-dihydro-4-oxo-3-pyridinecarboxylic acid side chains. Synthesis and structure-activity relationships by DeJohn, D, Domagala, J M, Haskell, T H, Heifetz, C L, Huang, G G, Kaltenbronn, J S, Krolls, U

“…A series of penicillins and cephalosporins containing the substituted 6-vinyl-1,2-dihydro-2-oxo- and 1,4-dihydro-4-oxo-3-pyridinecarboxylic acid side chains…”
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CI-867, a new broad-spectrum semisynthetic penicillin by Kaltenbronn, J S, Haskell, T H, Doub, L, Knoble, J, DeJohn, D, Krolls, U, Jenesel, N, Huang, G G, Heifetz, C L, Fisher, M W

“…The synthesis and antimicrobial activity of a new semisynthetic penicillin are described. Both in vitro and in vivo, the compound shows promising antibacterial…”
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Disc-agar diffusion microbiological assay procedure for determining serum and urine levels of sulfacytine and other sulfonamides by Heifetz, C L, Chodubski, J A, DeCarlo, M O, Fisher, M W

“…A reasonably precise, reproducible, and sensitive microbiological procedure for directly assaying sulfacytine and other sulfonamides as antibacterially active…”
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Treatment of experimental Pseudomonas corneal ulcers with enoxacin, a quinolone antibiotic by Sugar, A, Cohen, M A, Bien, P A, Griffin, T J, Heifetz, C L, Mehta, S

“…Enoxacin is a broad-spectrum quinolone-derivative antibiotic. In a rabbit model of keratitis caused by a Pseudomonas species, enoxacin (3 mg/mL) was as…”
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Comparative therapeutic efficacy of clinafloxacin in a Pseudomonas aeruginosa mouse renal abscess model by SHAPIRO, M. A, SESNIE, J. C, DESATY, T. M, GRIFFIN, T. J, HEIFETZ, C. L

“…A deep-seated Pseudomonas aeruginosa mouse kidney abscess model was used to compare the therapeutic efficacy of clinafloxacin, a fluoroquinolone in clinical…”
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In vitro evaluation of cefdinir (FK482), a new oral cephalosporin with enhanced antistaphylococcal activity and beta-lactamase stability by Cohen, M A, Joannides, E T, Roland, G E, Meservey, M A, Huband, M D, Shapiro, M A, Sesnie, J C, Heifetz, C L

“…Cefdinir (FK482), a new oral cephalosporin with enhanced beta-lactamase stability, was tested by microbroth dilution against respiratory, urogenital, and skin…”
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1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity by DOMAGALA, J. M, HEIFETZ, C. L, MICH, T. F, NICHOLS, J. B

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A novel rapid throughput phototolerance screen in mice by Shapiro, Martin A., Sesnie, Josephine C., Joannides, E.Themis, Malta, Thomas E., Dever, Julie A., Heifetz, Carl L.

“…A relatively simple, rapid throughput phototolerance screen in small animals would be very useful in early drug development. It could prioritize or select…”
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In vitro antibacterial activities of the fluoroquinolones PD 117596, PD 124816, and PD 127391 by Cohen, M A, Huband, M D, Mailloux, G B, Yoder, S L, Roland, G E, Heifetz, C L

“…Three new aminopyrrolidine-substituted fluorocyclopropyl quinolones--PD 117596, PD 124816, and PD 127391--were tested for in vitro antibacterial activity…”
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In vitro activity of sparfloxacin (CI-978, AT-4140, and PD 131501). A quinolone with high activity against gram-positive bacteria by Cohen, M A, Huband, M D, Mailloux, G B, Yoder, S L, Roland, G E, Heifetz, C L

“…Sparfloxacin (CI-978, AT-4140 and PD 131501) is a new antimicrobial agent of the piperazinyl quinolone class. Relative to other quinolones, it is a potent…”
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In vivo therapeutic efficacy of cefdinir (FK482), a new oral cephalosporin, against Staphylococcus aureus and Haemophilus influenzae in mouse infection models by Cohen, M A, Wold, S A, Meservey, M A, Gage, J W, Heifetz, C L, Mailloux, G B, Roland, G E, Yoder, S L

“…Cefdinir (FK482), a new oral cephalosporin, displayed potent oral activity versus induced infections in mice. In studies using beta-lactamase-nonproducing…”
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Comparative in-vitro activity of enoxacin against penicillinase- and non-penicillinase-producing Neisseria gonorrhoeae by Shapiro, M A, Heifetz, C L, Sesnie, J C

“…The in-vitro antigonococcal activity of enoxacin was measured by a broth microdilution method. Comparisons were made with five clinically relevant marketed…”
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