High-throughput lead optimization in drug discovery by Tushar Kshirsagar PDF

By Tushar Kshirsagar

ISBN-10: 0849372682

ISBN-13: 9780849372681

A unmarried resource on Parallel Synthesis for Lead Optimization

The finish of the former millennium observed an explosion within the software of parallel synthesis recommendations for making compounds for high-throughput screening. over the years, it grew to become transparent that extra idea within the layout part of library improvement is critical to generate prime quality hits. extra lately, using parallel synthesis innovations has shifted to functions past screening collections. Exploring the nuances of this know-how, High-Throughput Lead Optimization in Drug Discovery describes the appliance of parallel synthesis to guide optimization and the layout and synthesis of specific libraries.

Examine Case experiences that conceal various diversified organic goals

Featuring real-world examples and contributions from recognized scientists, the publication explores the shift to carrying out parallel lead optimization in-house whereas outsourcing lots of the screening libraries synthesis. It contains greater than 15 case experiences that surround a number of organic ambitions for program in several healing components. The textual content comprises examples of strong and solution-phase options for the synthesis of directed libraries. The bankruptcy authors clarify the layout ideas they used to direct the alternative of templates and variety components.

Speed Up Drug Discovery and the Hit-to-Lead technique

Focusing at the program of combinatorial chemistry to medicinal chemistry, this quantity compiles a sequence of optimization initiatives that offer you a photograph of successes and demanding situations within the use of parallel synthesis for lead optimization. It explores how this know-how, whilst utilized to library layout, can accelerate drug discovery.

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34 at GlaxoSmithKline reported the synthesis and optimization of tertiary amines as nonsteroidal liver X receptor (LXR) agonists. LXRs belong to the nuclear hormone receptor superfamily of activated transcription factors.

For the solution-phase approach, the authors synthesized 232 as the key building block for the exploration of the thio ether unit. ) to afford desired products (234). indb 31 2/7/08 9:53:53 AM 32 High-Throughput Lead Optimization in Drug Discovery For the solid-phase approach, the authors used the acid-labile SASRIN resin (235). In this approach, the benzyl alcohol of SASRIN was converted into the chloride using triphosgene and PPh3 in DCM. The resulting SASRIN chloride (236) resin was then alkylated with 2,2,2-trifluoro-N-(5-thiocyanatothiazol-2-yl)acetamide (237) in the presence of DIEA in DCM.

Substitution of the phenyl group with cyclohexyl, 2-naphthyl, and 3- and 4-substituted phenyl groups was very well tolerated, affording potent inhibitors with IC50 < 100 nM (136: IC50 = 81 ± 9 nM, 137: IC50 = 14 ± 3 nM, 138: IC50 = 23 ± 3 nM). Interestingly, it was also discovered that further N-methylation of 133 or exchange of the benzyl group with a phenyl group in all cases was detrimental for activity. R1 HN HN N N N 133 Central Scaffold N 132: IC50 = 127 ± 14 nM Synthesis: Library 1 Cl 2 eq.

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High-throughput lead optimization in drug discovery by Tushar Kshirsagar


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