Zobrazeno 1 - 10
of 81
pro vyhledávání: '"John P. Mallamo"'
Autor:
Senuri Pathiranage, Iwao Ojima, Maurizio Del Poeta, Julia Zambito, Yi Sun, John P. Mallamo, Cristina Lazzarini, J. Brian McCarthy, Krupanandan Haranahalli
Publikováno v:
J Med Chem
Recently, the fungal sphingolipid glucosylceramide (GlcCer) synthesis has emerged as a highly promising new target for drug discovery of next-generation antifungal agents, and we found two aromatic acylhydrazones as effective inhibitors of GlcCer syn
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5e3017af51d810f95efbec5cef6c066
https://doi.org/10.1021/acs.jmedchem.9b01004
https://doi.org/10.1021/acs.jmedchem.9b01004
Autor:
Caroline Mota Fernandes, Iwao Ojima, Maurizio Del Poeta, J. Brian McCarthy, John P. Mallamo, Krupanandan Haranahalli, Deveney Dasilva
Publikováno v:
Antimicrob Agents Chemother
Fungal infections are a universal problem and are routinely associated with high morbidity and mortality rates in immunocompromised patients. Existing therapies comprise five different classes of antifungal agents, four of which target the synthesis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b30625e3bc366ab7619e982e2bd61b2
https://europepmc.org/articles/PMC7848987/
https://europepmc.org/articles/PMC7848987/
Autor:
Maurizio Del Poeta, Iwao Ojima, John P. Mallamo, Cristina Lazzarini, J. Brian McCarthy, Krupanandan Haranahalli
Publikováno v:
Antimicrob Agents Chemother
The incidence of invasive fungal infections is rising due to the increase in susceptible populations. Current clinically available drugs have therapeutic limitations due to toxicity, a narrow spectrum of activity, and, more importantly, the consisten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7bc405e4ba5c56e9f21e2215c2c2c4c5
https://doi.org/10.1128/aac.00946-20
https://doi.org/10.1128/aac.00946-20
Publikováno v:
ACS Chemical Neuroscience
The central nervous system (CNS) is the major area that is affected by aging. Alzheimer's disease (AD), Parkinson's disease (PD), brain cancer, and stroke are the CNS diseases that will cost trillions of dollars for their treatment. Achievement of ap
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9082302be26311a31e107b9e1fc8d1ef
https://doi.org/10.1021/cn200100h
https://doi.org/10.1021/cn200100h
Autor:
Emir Duzic, Edward R. Bacon, Joanne R. Mathiasen, Michael J. Marino, Donna Bozyczko-Coyne, John A. Gruner, John P. Mallamo, Rita Raddatz, Dorothy G. Flood, Lisa D. Aimone, Hervé Schaffhauser, Siyuan Le, Maciej Gasior, Michael Williams, Mark A. Ator, Robert L. Hudkins
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 340:124-133
CEP-26401 [irdabisant; 6-{4-[3-((R)-2-methyl-pyrrolidin-1-yl)-propoxy]-phenyl}-2H-pyridazin-3-one HCl] is a novel, potent histamine H₃ receptor (H₃R) antagonist/inverse agonist with drug-like properties. High affinity of CEP-26401 for H₃R was d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d821744703207b55845570e2612fea8e
https://doi.org/10.1124/jpet.111.186585
https://doi.org/10.1124/jpet.111.186585
Autor:
Gilbert Moachon, Lars J. S. Knutsen, Nadine C. Becknell, Mark A. Ator, Joanne R. Mathiasen, Lisa D. Aimone, Rita Raddatz, Michael J. Marino, Robert L. Hudkins, Michael Williams, Mehran Yazdanian, Edward R. Bacon, John P. Mallamo, Prouty Catherine P, Ming Tao
Publikováno v:
Journal of Medicinal Chemistry. 54:4781-4792
Optimization of a novel series of pyridazin-3-one histamine H(3) receptor (H(3)R) antagonists/inverse agonists identified 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (8a, CEP-26401; irdabisant) as a lead candidate for poten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9c988d057249d18cfdae4d049a4ca8a
https://doi.org/10.1021/jm200401v
https://doi.org/10.1021/jm200401v
Autor:
Donna Bozyczko-Coyne, Steven C. Almo, Jean Husten, Michael S. Saporito, Richard W. Scott, Alexander A. Fedorov, Mark A. Ator, Chung Ho Park, Diebold James L, Ming Tao, Thelma S. Angeles, Sheryl L. Meyer, John P. Mallamo, Lisa D. Aimone, Elena V. Fedorov, Kurt A. Josef, Beverly P. Holskin, Robert L. Hudkins, Joanne R. Mathiasen, John T. Durkin
Publikováno v:
Journal of Medicinal Chemistry. 51:5680-5689
The optimization of the dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-one R(2) and R(12) positions led to the identification of the first MLK1 and MLK3 subtype-selective inhibitors within the MLK family. Compounds 14 (CEP-5104) and 16 (CEP-6331) di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5006c141cc94502df1d9156dde918c8a
https://doi.org/10.1021/jm8005838
https://doi.org/10.1021/jm8005838
Publikováno v:
Journal of Medicinal Chemistry. 51:5149-5171
toward kinase inhibitor discovery, with the result that several kinase inhibitors have been approved as drugs since 2001. The commercial success of imatinib (N-(4-methyl-3-(4-(pyridin-3yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-l)methyl)b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3cfdacb02a80ba9f72c931b97abe0190
https://doi.org/10.1021/jm800475y
https://doi.org/10.1021/jm800475y
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3551-3555
An immobilized Staurosporine aglycone isostere where one of the indole nitrogen atoms was replaced by carbon has been sequentially functionalized to generate compounds inhibiting TrkA kinase. In the first phase, initial screening of a library of C13-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a748072bfbdac256dd1a25a7ce16018
https://doi.org/10.1016/j.bmcl.2008.05.012
https://doi.org/10.1016/j.bmcl.2008.05.012
Synthesis and Mixed Lineage Kinase Activity of Pyrrolocarbazole and Isoindolone Analogs of (+)K-252a
Publikováno v:
Journal of Medicinal Chemistry. 50:433-441
Structural modification of the indolecarbazole natural product (+)K-252a identified structural requirements for MLK activity and a novel series of potent fused pyrrolocarbazole MLK1/3 inhibitors. The SAR revealed that the lactam regiochemistry, the s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1dc636c6f83eda62f02a594bd566a7a
https://doi.org/10.1021/jm051074u
https://doi.org/10.1021/jm051074u