Download e-book for iPad: High-throughput lead optimization in drug discovery by Tushar Kshirsagar

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 innovations for making compounds for high-throughput screening. through 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 thoughts 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 special libraries.

Examine Case reports that conceal quite a number assorted organic ambitions

Featuring real-world examples and contributions from famous scientists, the publication explores the shift to accomplishing parallel lead optimization in-house whereas outsourcing lots of the screening libraries synthesis. It contains greater than 15 case stories that surround various organic goals for program in numerous healing components. The textual content includes examples of reliable and solution-phase concepts for the synthesis of directed libraries. The bankruptcy authors clarify the layout rules they used to direct the alternative of templates and variety components.

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

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

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The final products were cleaved using a combination of aqueous NaOH in MeOH at 40°C for 3 days. The crude mixtures were then neutralized with HCl and filtered through silica-packed cartridges. This methodology afforded a 1012-compound library (220 and 221), isolating about 10 to 40 mg of final product. The authors also used a nearly identical solution-phase approach where the resin was changed with COOEt. 24 O IC50 = 5 nM (Aur-A) IC50 = 100 nM (Aur-A) Aurora targeted library 1. 2/7/08 9:53:53 AM 31 Introduction and Review Screening the library against Aurora-A clearly indicated that acylation of the 3-amino group with 4′-tert-butyl-substituted benzamido groups was favored for potency.

The next efforts centered on the optimization of the aryl group at the 2-position, keeping the racemic benzyl bis-pyrrolidine unit constant. More than 60 biaryl compounds and 100 amides were made. The SAR on the biaryl compounds revealed that substitution at the para-position provided better activity compared to meta-substitution (192: IC50 = 90 nM ± 40 nM). indb 26 2/7/08 9:53:49 AM 27 Introduction and Review When optimizing the amide analogs, it was also noticed that para-amides were more potent than the meta-amides (193: IC50 = 30 nM ± 80 nM).

RGD peptidomimetics have been found to be potent inhibitors of αvβ3 where many of them possess a 2,3-diaminopropionic acid core. However, the methodologies used for their synthesis only allow the variation of one functionality at a time. Gopalsamy and co-workers22 devised a combinatorial solid-phase synthesis that allowed the chemical modification of both the N-terminus region as well as the α-amino group of the 2,3-diaminopropionic acid. Using β-N-dde-α-N-Fmoc-L-diaminopropionic acid as the starting material, this orthogonally protected diamino acid was anchored to Wang resin using peptide coupling conditions (152).

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High-throughput lead optimization in drug discovery by Tushar Kshirsagar


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