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- Title
DNA‐Encoded Libraries: Hydrazide as a Pluripotent Precursor for On‐DNA Synthesis of Various Azole Derivatives.
- Authors
Ma, Fei; Li, Jie; Zhang, Shuning; Gu, Yuang; Tan, Tingting; Chen, Wanting; Wang, Shuyue; Ma, Peixiang; Xu, Hongtao; Yang, Guang; Lerner, Richard A.
- Abstract
DNA‐encoded combinatorial chemical library (DEL) technology, an approach that combines the power of genetics and chemistry, has emerged as an invaluable tool in drug discovery. Skeletal diversity plays a fundamental importance in DEL applications, and relies heavily on novel DNA‐compatible chemical reactions. We report herein a phylogenic chemical transformation strategy using DNA‐conjugated benzoyl hydrazine as a common versatile precursor in azole chemical expansion of DELs. DNA‐compatible reactions deriving from the common benzoyl hydrazine precursor showed excellent functional group tolerance with exceptional efficiency in the synthesis of various azoles, including oxadiazoles, thiadiazoles, and triazoles, under mild reaction conditions. The phylogenic chemical transformation strategy provides DELs a facile way to expand into various unique chemical spaces with privileged scaffolds and pharmacophores.
- Subjects
CHEMICAL amplification; CHEMICAL precursors; DNA synthesis; CHEMICAL reactions; CHEMICAL libraries; AZOLES; THIADIAZOLES
- Publication
Chemistry - A European Journal, 2021, Vol 27, Issue 31, p8214
- ISSN
0947-6539
- Publication type
Academic Journal
- DOI
10.1002/chem.202100850