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作者:... Sarah Skerratt , Edward B. Stevens , Joseph S. Warmus
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2019, Vol.27 (1), pp.230-239
摘要:Abstract(#br)The voltage gated sodium channel Na V 1.8 has been postulated to play a key role in the transmission of pain signals. Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole Na V 1.8 blockers. ...
作者:Chan Woo Huh , Bruce M. Bechle , Joseph S. Warmus
来源:[J].Tetrahedron Letters(IF 2.397), 2018, Vol.59 (19), pp.1808-1812
摘要:Abstract(#br)A scalable synthetic route towards a chiral 2,2,6-trisubstituted chiral morpholine, which is a known opioid antagonist, was developed. The synthetic route involves incorporating an aryl group via Suzuki-Miyaura coupling and stereoselective hydroalkoxylation catalyzed...
作者:... Rubben Torella , Elaine Tseng , Joseph S. Warmus
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2017, Vol.27 (21), pp.4805-4811
摘要:Abstract(#br)The discovery and selection of a highly potent and selective Na V 1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is disclosed. Extensive in vitro pharmacology and ADME profiling followed by in vivo preclinical PK and efficacy model da...
作者:Joseph S. Warmus , Cheryl L. Quinn ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2012, Vol.22 (7), pp.2536-2543
摘要:Abstract(#br)Lipid A is an essential component of the Gram negative outer membrane, which protects the bacterium from attack of many antibiotics. The Lipid A biosynthesis pathway is essential for Gram negative bacterial growth and is unique to these bacteria. The first committed ...
作者:Joseph S. Warmus , Cathlin Flamme ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2008, Vol.18 (23), pp.6171-6174
摘要:Abstract(#br)This paper reports a second generation MEK inhibitor. The previously reported potent and efficacious MEK inhibitor, PD-184352 (CI-1040), contains an integral hydroxamate moiety. This compound suffered from less than ideal solubility and metabolic stability. An oxadia...
作者:Joseph S. Warmus , Todd R. Ryder ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 1998, Vol.8 (17), pp.2309-2314
摘要:Abstract(#br)Optimization of a 2-step reaction sequence was accomplished in 3–4 days , with over 200 different reaction conditions evaluated. Combinatorial arrays were performed using the optimized conditions to synthesize 590 new compounds which were tested for inhibition a...
作者:Joseph S. Warmus , Markus Boehm ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2013, Vol.23 (5), pp.1407-1411
摘要:Abstract(#br)Optimization of a high-throughput screening hit led to the discovery of a new series of 5-phenoxy-1,3-dimethyl-1 H -pyrazole-4-carboxamides as highly potent agonists of TGR5. This novel chemotype was rapidly developed through iterative combinatorial library synthesis...
作者:... Yvonne Smith , Joseph S. Warmus , Haile Tecle
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2008, Vol.18 (24), pp.6501-6504
摘要:Abstract(#br)A novel series of benzhydroxamate esters derived from their precursor anthranilic acids have been prepared and have been identified as potent MEK inhibitors. 2-(2-Chloro-4-iodo-phenylamino)- N -cyclopropylmethoxy-3,4-difluoro-benzamide, CI-1040 , was the first MEK in...
作者:Joseph S. Warmus , Paul D. Bonin
来源:[J].Tetrahedron Letters(IF 2.397), 2012, Vol.53 (7), pp.852-853
摘要:Abstract(#br)A straightforward synthesis of a 2,6-disubstituted-7,8-dihydro-6 H -pyrano[2,3-6]pyrazine is described. The synthesis relies on a versatile dichloropyrazine–aldehyde intermediate and an olefination partner.

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