Steroidal C-21 mercapto derivatives as dissociated steroids: Discovery of an inhaled dissociated steroid

Autor:	Rema Bitar, John C. Anthes, Jonathan E. Phillips, Purakkattle Biju, Robert G. Aslanian, Aileen House, Michael Berlin, Stephen Eckel, Daniel M. Solomon, George Kelly, Robbie L. McLeod, Richard Chapman, Xiomara Fernandez, Michelle Natiello, Daniel Prelusky, Kevin D. McCormick
Rok vydání:	2011
Předmět:	medicine.medical_treatment Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry Cell Line Steroid Structure-Activity Relationship Transactivation chemistry.chemical_compound Therapeutic index Administration Inhalation Drug Discovery medicine Animals Structure–activity relationship Sulfhydryl Compounds Lung Molecular Biology Transrepression Chemistry Organic Chemistry Asthma In vitro Rats Benzothiazole Cell culture Molecular Medicine Steroids
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:6343-6347
ISSN:	0960-894X
Popis:	A series of C-21 mercapto derivatives of hydrocortisone have been synthesized and evaluated in cell based transrepression and transactivation assays. The benzothiazole derivative, compound 6 not only showed a dissociated profile in vitro functional assays but also a pharmacological profile in a Brown-Norway rat therapeutic index model of asthma that dissociated side effects (thymolysis) while maintaining efficacy against pulmonary inflammation and lung function.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ea94f04fce9e8206ef5e2b21f1f0210 https://doi.org/10.1016/j.bmcl.2011.08.108 Zobrazit plný text záznamu Full Text from ScienceDirect