Chem167_L13_May16

Which is spider like strategizing comp med chem can

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Unformatted text preview: You want to synthesize all the possible dipepAdes of 5 different amino acids How many reacAons would you need to carry out to do this using tradiAonal chem? 25: GAFVS GG, GA, GF, GV, GS, AG, AA, AF, AV, AS,… Split and mix Designed to produce a mixture of products in each reacAon vessel Same 5 amino acid dipepAde experiment can yield 25 dipepAdes in 5 mixtures These strategies are used to make VERY LARGE LIBRARIES OF COMPOUNDS (1k – 10k per library) Photolithography MiniaturizaAon & spaAal resoluAon Products made on plate of immobilized solid support Nitroveratryloxycarbonyl (NHX) protecAng group (photolabile) Light removes the NVOC/NHX Treatment with protected aa Coupling reacAon only occurs where light has deprotected constructs IncubaAon of plate with fluorescent tagged receptor enables easy detecAon of acAve compounds Strategizing: Basic scaffolds More basic scaffolds Which is “tadpole’- like? Which is “spider”- like? Strategizing: comp med chem Can use computers to help design focused combichem compound libraries Can be filtered for “drug- like ness” Chemical space is VAST… 1060...
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This note was uploaded on 01/15/2014 for the course CHEM 167 taught by Professor Amaro during the Winter '13 term at UCSD.

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