Journal
EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 28, Issue 8, Pages 647-651Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/13543776.2018.1508451
Keywords
HDAC6; inhibitors; 134-oxadiazole; sulfamide; zinc-binding group
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Funding
- Major Project of Science and Technology of Shandong Province [2015ZDJS04001]
- Key Research and Development Program of Shandong Province [2017CXGC1401]
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Introduction: There are great potential in the development of selective HDAC6 inhibitors for the treatment of infectious diseases, neoplasms, endocrine diseases, and other diseases associated with HDAC6 activity. Areas covered: The application claims 1,3,4-oxadiazole sulfamide derivatives as selective HDAC6 inhibitors for the treatment of infectious diseases, neoplasms, endocrine, nutritional, and metabolic diseases; mental and behavioral disorders; neurological diseases; diseases of the eye and adnexa; cardiovascular diseases; respiratory diseases; digestive diseases; diseases of the skin and subcutaneous tissue; disease of the musculoskeletal system and connective tissue; or congenital malformations, deformations and chromosomal abnormalities. Many of the exemplified compounds showed nanomole potency against HDAC6 and were more than 5000-fold selectivity for HDAC6 over HDAC1. Expert opinion: These 1,3,4-oxadiazole sulfamide derivatives have a unique zinc-binding group (ZBG) that provide good leads for the discovery of potent selective HDAC6 inhibitors for the treatment of a variety of diseases associated with HDAC6 activity.
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