Biological discoveries, chemistry

The Traditional Interplay between Biology and Chemistry in the Drug Discovery Process... 

Having identified the (+)-stereoisomer as the biologically active isomer, several independent enantioselective syntheses of this stereoisomer were developed. The initial synthesis developed in discovery chemistry employed the diastereoselective aldol condensation pioneered by Braun as the key component. Thus, treatment of aldehyde 13 from the racemic synthesis with the magnesium enolate of (5)-(+)-2-acetoxy-l,l,2-triphenylethanol at -70 °C, afforded 17 in 60% yield as a 97 3 mixture of the / ,5 5,5-diastereomers by HPLC (Scheme 3). Ester exchange employing sodium methoxide provided the methyl ester in quantitative yield. Reaction of this ester with three equivalents of lithio-f-butylacetate at -40 °C afforded the nearly enantiomerically pure r-butyl ester analog of racemic 14 in 75% yield. 

It may not be easy to duplicate the series of events that led to the discovery and development of daptomycin today, but there is reason to believe that other important molecules are yet to be discovered and there are approaches that integrate new biology and chemistry not available at the time of daptomycin discovery.23,77... 

Aqueous Solubility in Drug Discovery Chemistry, DMPK, and Biological Assays... 

Profile Founded in 1994, this privately held company develops and provides integrated discovery chemistry technologies and services in collaboration with pharmaceutical, biotechnology, and fine-chemical companies to accelerate the drug discovery process. In these partnerships, the companies provide the biological capabilities and Combichem provides the chemical expertise of the discovery process. Its mission is to provide a highly efficient and successful approach to the discovery of new drug molecules. 

The science that deals with the discovery, chemistry, composition, identification, biological and physiological effects, uses, and manufacture of drugs. 

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