Hg, Baek R, Liu Ks, Lam
Published in
Journal of Combinatorial Chemistry
The one-bead one-compound (OBOC) combinatorial library method enables the rapid generation and screening of millions of discrete chemical compounds on beads. Most of the OBOC screening methods require the library compounds to remain tethered to the bead during screening process. Methods have also been developed to release library compounds from imm...
Juskowiak, Gary L. McGee, Christopher J. Greaves, John Van Vranken, David L.
Published in
Journal of Combinatorial Chemistry
Cysteine-rich peptides are valued as tags for biarsenical fluorophores and as environmentally important reagents for binding toxic heavy metals. Due to the inherent difficulties created by cysteine, the power of one-bead one-compound (OBOC) libraries has never been applied to the discovery of short cysteine-rich peptides. We have developed the firs...
Dominique Bonnet Ganesan, A
Published in
Journal of Combinatorial Chemistry
Liu, G Fan, Y Carlson, Jr Zhao, Zg Kit S. Lam
Published in
Journal of Combinatorial Chemistry
In this report we demonstrate that a 1,5-dialkylamino-2,4-dinitrobenzene small molecule library can be generated by a highly efficient solution-phase synthesis method. From this 2485-member library, a series of novel compounds with antibacterial activity were isolated. The significance of this report is that the synthetic scheme is extremely simple...
Carpenter, Rd Deberdt, Pb Kit S. Lam Kurth, Mj
Published in
Journal of Combinatorial Chemistry
Using carbodiimide reagents [1,3-diisopropylcarbodiimide or N-(3-dimethylaminopropyl)-N -ethylcarbodiimide hydrochloride (EDC)], we have developed a mild, generalized, one-pot method that delivers N-2-arylaminobenzimidazole esters from commercially available aryl isothiocyanates and o-phenylenediamines. Following saponification and acidifying, the ...
Song, A Zhang, J Lebrilla, Cb Kit S. Lam
Published in
Journal of Combinatorial Chemistry
The solid-phase synthesis of 2-alkylthio-6H-pyrano[2,3-f]benzimidazole-6-ones (2-alkylthioimidazocoumarins) is described. 7-Fluoro-4-methyl-6-nitro-2-oxo-2H-1-benzopyran-3-carboxylic acid was coupled to Rink amide resin via its carboxyl group. The resin-bound scaffold then underwent aromatic nucleophilic substitution with primary amines, followed b...
Ying, L Ruiwu (Ray) Liu Zhang, J Kit S. Lam Lebrilla, Cb Gervay-Hague, J
Published in
Journal of Combinatorial Chemistry
A glycopeptide library containing more than 500,000 compounds has been constructed from a combination of Asn-linked carbohydrates using one-bead-one-compound combinatorial methodologies. The library was encoded with peptide markers that were topologically segregated on the interior of the solid support to negate interference with carbohydrate/prote...
Simon, Ra Schuresko, L Dendukuri, N Goers, E Murphy, B Lokey, Rs
Published in
Journal of Combinatorial Chemistry
As part of our program to identify novel small molecules with interesting biological activity, we have designed and synthesized a library of end-capped dipeptides with an emphasis on compound diversity, complexity, and membrane permeability. An approximately 1500-member library was synthesized manually on large polystyrene beads using the mix-and-s...
Yao, Nh He, Wy Kit S. Lam Liu, G
Published in
Journal of Combinatorial Chemistry
Direct O-glycosylation of amino acids bound to TentaGel resin with a number of glycosyl trichloroacetimidate donors results in high yields. The glycosylation reaction can be easily monitored by analyzing the bead-bound amino acids with high-resolution magic angle spinning (HR-MAS) NMR. These studies pave a new way for the construction of "one-bead ...
Franz, Ah Ruiwu (Ray) Liu Song, A Kit S. Lam Lebrilla, Cb
Published in
Journal of Combinatorial Chemistry
The identification of pharmacologically promising compounds (lead compounds) from combinatorial libraries is frequently limited by the throughput of the analytical technique employed. Fourier transform mass spectrometry (FTMS) offers high sensitivity, mass accuracy (m/Deltam > 500 000), and sequencing capabilities. A rapid and efficient method for ...
