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作者:Samuel Chackalamannil , Darı́o Doller ...
来源:[J].Tetrahedron Letters(IF 2.397), 2000, Vol.41 (21), pp.4043-4047
摘要:Abstract(#br)An efficient, multigram-scale synthesis of dihydronaphthofuranone 1 using a novel aryl intramolecular Diels–Alder reaction of propargyl trans -cinnamate 8 is described. Catalytic reduction of 1 gave the cis -fused tetrahydronaphthofuranone derivative 2 .
作者:Samuel Chackalamannil , Yan Xia ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 1995, Vol.5 (17), pp.2005-2010
摘要:Abstract(#br)The synthesis and CETP inhibitory activity of a series of compounds related to wiedendiols ( 1a,1b ) are reported. It is proposed that a two point pharmacophore consisting of a catechol group and a large hydrophobic anchor is necessary for activity.
作者:Samuel Chackalamannil , Darı́o Doller ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2004, Vol.14 (15), pp.3967-3970
摘要:Abstract(#br)A number of analogs of the natural product himbacine were synthesized employing variations at the heterocyclic unit and the tether that links the heterocyclic unit to the tricyclic motif. Several of these analogs had M 2 affinity and M 1 /M 2 selectivity comparable t...
作者:Samuel Chackalamannil , Yuguang Wang
来源:[J].Tetrahedron(IF 2.803), 1997, Vol.53 (32), pp.11203-11210
摘要:Abstract(#br)The synthesis of ( S )-2-methyl tetrahydropyridine-N-oxide ( 4 ), a key intermediate for the enantioselective construction of trans -2,6-disubstituted piperidines via [3+2] nitrone cycloaddition reaction, is described. Nitrone 4 was elaborated to the fire ant venom a...
作者:Samuel Chackalamannil , Shin Chung ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 1996, Vol.6 (11), pp.1257-1260
摘要:Abstract(#br)Phosphinic acid derivatives, represented by structure 1 , have been synthesized and evaluated as endothelin converting enzyme (ECE) inhibitors. Several of these compounds (for example, 1b , 1c , and 1f ) were found to be potent inhibitors of ECE with a high degree of...
作者:Samuel Chackalamannil , Darı́o Doller , Keith Eagen
来源:[J].Tetrahedron Letters(IF 2.397), 2002, Vol.43 (29), pp.5101-5103
摘要:Abstract(#br)A mechanistic investigation into the recently reported intramolecular aryl Diels–Alder reaction was carried out using deuterium labeling. These studies led to the conclusion that the initial Diels–Alder adduct is isomerized to a highly conjugated tetra-ene inter...
作者:Samuel Chackalamannil , Darı́o Doller ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2001, Vol.11 (21), pp.2851-2853
摘要:Abstract(#br)Several benzimidazole derivatives have been identified as potent thrombin receptor (PAR-1) antagonists as represented by compound 1h , which showed an IC 50 of 33 nM.
作者:Samuel Chackalamannil , Yuguang Wang ...
来源:[J].Tetrahedron Letters(IF 2.397), 1995, Vol.36 (30), pp.5315-5318
摘要:Abstract(#br)An efficient synthesis of Wiedendiol-A ( 1 ) is described starting from commercially available (+)-sclareolide. This synthesis also confirms the absolute stereochemistry of Wiedendiol-A.
作者:Samuel Chackalamannil , William J. Greenlee ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2010, Vol.20 (22), pp.6676-6679
摘要:Abstract(#br)An analog of the thrombin receptor antagonist vorapaxar (SCH 530348) with increased aqueous solubility, compound 9c (SCH 602539), was discovered through incorporation of polar substituents on the pyridine ring of the himbacine-derived lead series. This analog retaine...
作者:Samuel Chackalamannil , Michael Czarniecki ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 1996, Vol.6 (7), pp.919-922
摘要:Abstract(#br)A series of substituted 1,3,5-triazines (represented by 2 ) were synthesized and evaluated for their cholesteryl ester transfer protein (CETP) inhibitory activities. Among the most potent compounds were those with R = benzyl (IC 50 = 9 μM) and R = [(2-naphthalen...

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