Výsledky vyhledávání - "Andrew T. Papoulis"

GT160-246, a Toxin Binding Polymer for Treatment of Clostridium difficile Colitis

Autor: Richard Fitzpatrick, E. Pat Cannon, Pamela Kelly, Alex Brezzani, Andrew T. Papoulis, Philip J. Goddard, Jeffrey D. Klinger, Emilie Rinard, Robert H. Barker, David W. K. Acheson, Mary Pitruzzello, Carol Dinardo, Keith K. Shackett, Caroline B. Kurtz, Gerard P. Palace

Publikováno v: Antimicrobial Agents and Chemotherapy. 45:2340-2347

GT160-246, a high-molecular-weight soluble anionic polymer, was tested in vitro and in vivo for neutralization of Clostridium difficile toxin A and B activities. Five milligrams of GT160-246 per ml neutralized toxin-mediated inhibition of protein syn

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d163567891b289e4b94152f0e2c983c4
https://doi.org/10.1128/aac.45.8.2340-2347.2001

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Structure-Based Design of Selective Inhibitors of Dihydrofolate Reductase: Synthesis and Antiparasitic Activity of 2,4-Diaminopteridine Analogues with a Bridged Diarylamine Side Chain

Autor: Andre Rosowsky, and Andrew T. Papoulis, Nikolai Galitsky, Hongning Fu, Sherry F. Queener, Vivian Cody

Publikováno v: Journal of Medicinal Chemistry. 42:4853-4860

As part of a larger search for potent as well as selective inhibitors of dihydrofolate reductase (DHFR) enzymes from opportunistic pathogens found in patients with AIDS and other immune disorders, N-[(2,4-diaminopteridin-6-yl)methyl]dibenz[b,f]azepin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5968967e2c5c379b6d21713a9e7926e
https://doi.org/10.1021/jm990331q

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One-step synthesis of novel 2,4-diaminopyrimidine antifolates from bridged alicyclic ketones and cyanoguanidine

Autor: Andre Rosowsky, Sherry F. Queener, Andrew T. Papoulis

Publikováno v: Journal of Heterocyclic Chemistry. 36:723-728

A convenient one-step reaction with cyanoguanidine was used to convert alicyclic ketones to previously undescribed 2,4-diamino-5,6,7,8-tetrahydroquinazolines with a one-, two-, or three-carbon bridge in the carbocyclic ring. Although the yields of th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a5f7cadca6d94eb2c4b79aae3201f28b
https://doi.org/10.1002/jhet.5570360324

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Synthesis and Antiparasitic and Antitumor Activity of 2,4-Diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline Analogues of Piritrexim

Autor: Ronald A. Forsch, Andrew T. Papoulis, Andre Rosowsky, Sherry F. Queener

Publikováno v: Journal of Medicinal Chemistry. 42:1007-1017

Nineteen previously undescribed 2,4-diamino-6-(arylmethyl)-5,6,7, 8-tetrahydroquinazolines (5a-m, 10-12) were synthesized as part of a larger effort to assess the therapeutic potential of lipophilic dihydrofolate reductase (DHFR) inhibitors against o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a297e3fbcf52de87684dcc3f6d062233
https://doi.org/10.1021/jm980572i

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2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine Analogues of Trimethoprim as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase

Autor: Sherry F. Queener, Andre Rosowsky, and Andrew T. Papoulis

Publikováno v: Journal of Medicinal Chemistry. 41:913-918

Three previously unreported (R,S)-2,4-diamino-5-[(3,4,5-trimethoxyphenyl) alkyl]-6,7-dihydro-5H-cyclopenta[d]pyrimidines 15a-c were synthesized as analogues of trimethoprim (TMP) and were tested as inhibitors of Pneumocystis carinii, Toxoplasma gondi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab1a9777a8421c3a846d966402759a54
https://doi.org/10.1021/jm970614n

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Implications of promiscuous Pim-1 kinase fragment inhibitor hydrophobic interactions for fragment-based drug design

Autor: Tatiana Gladysheva, Yibin Xiang, A.C Good, Bradford H. Hirth, T Fremgen, Gary Asmussen, Renato Skerlj, A Jain, Kimberly Bishop, J.D Stepp, Ronnie Wei, Katherine Jancsics, Maria Fitzgerald, Jinyu Liu, H.P Biemann, Markus Metz, Andrew T Papoulis

Publikováno v: Journal of medicinal chemistry. 55(6)

We have studied the subtleties of fragment docking and binding using data generated in a Pim-1 kinase inhibitor program. Crystallographic and docking data analyses have been undertaken using inhibitor complexes derived from an in-house surface plasmo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c35c78468ba65305e73f208d0e42ebe7
https://pubmed.ncbi.nlm.nih.gov/22339127

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The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors

Autor: Yibin Xiang, Hans-Peter Biemann, Tatiana Gladysheva, Markus Metz, J. David Stepp, Renato Skerlj, Andrew T Papoulis, Andrew C. Good, Kimberly Bishop, Annuradha Jain, Gary Asmussen, Bradford H. Hirth, Katherine Jancsics, Maria Fitzgerald, Ronnie Wei, Jinyu Liu

Publikováno v: Bioorganicmedicinal chemistry letters. 21(10)

Novel benzofuran-2-carboxylic acids, exemplified by 29, 38 and 39, have been discovered as potent Pim-1 inhibitors using fragment based screening followed by X-ray structure guided medicinal chemistry optimization. The compounds demonstrate potent in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0f2a70806999950d2d3da86a2785090
https://pubmed.ncbi.nlm.nih.gov/21507633

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ChemInform Abstract: One-Step Synthesis of Novel 2,4-Diaminopyrimidine Antifolates from Bridged Alicyclic Ketones and Cyanoguanidine

Autor: Andre Rosowsky, Andrew T. Papoulis, Sherry F. Queener

Publikováno v: ChemInform. 30

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9ef28fbd4d0415c52bf9a0ee52a54f88
https://doi.org/10.1002/chin.199944160

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