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A Novel Procedure for the Synthesis of Libraries Containing Small Organic Molecules
Author(s) -
Carell Thomas,
Wintner Edward A.,
BashirHashemi A.,
Rebek Julius
Publication year - 1994
Publication title -
angewandte chemie international edition in english
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 0570-0833
DOI - 10.1002/anie.199420591
Subject(s) - amide , hydrolysis , chemistry , molecule , combinatorial chemistry , small molecule , organic molecules , organic synthesis , organic chemistry , drug discovery , catalysis , biochemistry
Accelerated drug searches should be possible through the generation and screening of libraries of smaller organic molecules. The reaction of tetracarboxylic acid tetrachloride 1 with a mixture of 21 amines (predominantly amino acids) in solution yields a complex mixture, which can theoretically contain 97461 compounds. Compound 2 , an inhibitor of trypsin‐catalyzed amide hydrolysis ( K 1 = (9 ± 2) × 10 −6 M ), was selected by four‐step screening procedure. This result demonstrates the usefulness of libraries of molecules and the screening of these complex mixtures.