Structure-activity relationship of BMS906024 derivatives for Cryptosporidium parvum growth inhibition.
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ABSTRACT:
SUBMITTER: Lee S
PROVIDER: S-EPMC10290938 | biostudies-literature | 2023 Jun
REPOSITORIES: biostudies-literature
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Structure-activity relationship of BMS906024 derivatives for Cryptosporidium parvum growth inhibition.
Lee Seungheon S Love Melissa S MS Modukuri Ramkumar R Chatterjee Arnab K AK Huerta Lauren L Lawson Ann P AP McNamara Case W CW Mead Jan R JR Hedstrom Lizbeth L Cuny Gregory D GD
Bioorganic & medicinal chemistry letters 20230515
BMS906024, a γ-secretase inhibitor that blocks Notch signaling, was previously shown to inhibit Cryptosporidium parvum growth in vitro. A structure-activity relationship (SAR) analysis of BMS906024 reported herein demonstrates the importance of the stereochemistry of the C-3 benzodiazepine and the succinyl β-substituent. However, concomitant removal of the succinyl α-substituent and switching the primary amide with secondary amides was tolerated. For example, 32 (SH287) inhibited C. parvum growt ...[more]
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