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(E)-3-[[[[6-(2-Carboxyethenyl)-5-[[8-(4-methoxyphenyl)octyl]oxy]-2-pyridinyl]methyl]thio]methyl]benzoic Acid and Related Compounds: High Affinity Leukotriene B4 Receptor Antagonists

Autor: R A, Daines, P A, Chambers, D S, Eggleston, J J, Foley, D E, Griswold, R C, Haltiwanger, D R, Jakas, W D, Kingsbury, L D, Martin, I, Pendrak

Publikováno v: Journal of Medicinal Chemistry. 37:3327-3336

(E)-3-[[[[6-(2-Carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]methyl]thio]methyl]benzoic acid (11, SB 201993) is a novel, potent LTB4 receptor antagonist. Compound 11 arose from a structure-activity study of a series of trisubstituted

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49b1deca0554311ece95c563c1e51085
https://doi.org/10.1021/jm00046a017

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Preclinical pharmacokinetics and interspecies scaling of a novel vitronectin receptor antagonist

Autor: K W, Ward, L M, Azzarano, W E, Bondinell, R D, Cousins, W F, Huffman, D R, Jakas, R M, Keenan, T W, Ku, D, Lundberg, W H, Miller, J A, Mumaw, K A, Newlander, J L, Pirhalla, T J, Roethke, K L, Salyers, P R, Souder, G J, Stelman, B R, Smith

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 27(11)

Allometric scaling may be used in drug development to predict the pharmacokinetics of xenobiotics in humans from animal data. Although allometry may be successful for compounds that are excreted unchanged or that are oxidatively metabolized (with cor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e030481b63061d6287d5df04c74a5102
https://pubmed.ncbi.nlm.nih.gov/10534306

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Reaction of 2-aminobenzimidazole with bifunetional carboxylie acid derivatives. Formation of pyrimido[1,2-a] benzimidazolones

Autor: N. M. Hall, D. R. Jakas, A. W. Chow, B. P. Trotter, J. R. E. Hoover

Publikováno v: Journal of Heterocyclic Chemistry. 10:71-75

2-Aminobenzimidazole reacts with α,β-unsaturated carboxylic acid chlorides or esters to give only pyrimido [1,2-a] benzimidazol-2-(1H) ones. β-Ethoxymethylenemalonie acid derivatives or β-ketocarboxylic acid derivatives give only pyrimido [1,2-a]

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::477f6e4727d81cc405595db3d43471a4
https://doi.org/10.1002/jhet.5570100116

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Antimicrobial activity of SKF 88070, an expanded-spectrum cephalosporin with high and prolonged levels in blood

Autor: D. R. Jakas, Donald Pitkin, Lillian Phillips, Paul Actor, Sarah F. Grappel, George L. Dunn

Publikováno v: Antimicrobial agents and chemotherapy. 25(6)

SK&F 88070 (7-[[(2-amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3- [[[1-(2-sulfaminoethyl)-1H-tetrazol-5-yl]thio] methyl]-3-cephem-4-carboxylic acid) is a new parenteral cephalosporin with an expanded-spectrum profile of antibacterial activity, incl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ac9c88e1f5d80c945a84df2238020ef
https://pubmed.ncbi.nlm.nih.gov/6742815

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Orally active 7-phenylglycyl cephalosporins. Structure-activity studies related to cefatrizine (SKF 60771)

Autor: D. R. Jakas, Jerry A. Weisbach, L.D. Davis, George L. Dunn, Joseph V. Uri, John R. E. Hoover, Paul Actor, E.M. Dietz, David A. Berges, John J. Taggart, N. Yim

Publikováno v: The Journal of antibiotics. 29(1)

The synthesis of a series of related broad-spectrum 7-phenylglycyl cephalosporins with 3-heterocyclicthiomethyl substituents is described. The effects of benzene-ring hydroxylation and 3-substituent variation on the in vitro antibacterial activity, h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1a57b79096b705dab3872ba4d73b293
https://pubmed.ncbi.nlm.nih.gov/776915

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