Discovery and pharmacological evaluation of indole derivatives as potent and selective RORγt inverse agonist for multiple autoimmune conditions

[Display omitted] •Identification of indole analogues as potent RORγt inverse agonists, SAR of around 44 compounds is presented.•Potent compounds were evaluated for pharmacokinetic properties and data is presented.•Significant inhibition of anti-CD3/anti-CD28 induced Il17 gene expression in mouse sp...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2019-08, Vol.29 (16), p.2208-2217
Hauptverfasser:	Shaikh, Nadim S., Iyer, Jitesh P., Munot, Yogesh S., Mukhopadhyay, Partha P., Raje, Amol A., Nagaraj, Ranganayaki, Jamdar, Vijay, Gavhane, Ravindra, Lohote, Mahendra, Sherkar, Prasad, Bala, Madhu, Petla, Rajkanth, Meru, Ashwinkumar, Umrani, Dhananjay, Rouduri, Sreekanth, Joshi, Sachin, Reddy, Satyanarayan, Kandikere, Vishwottam, Bhuniya, Debnath, Kulkarni, Bheemashankar, Mookhtiar, Kasim A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Autoimmune diseases IL-17 Indole Psoriasis RORc RORγ
Online-Zugang:	Volltext
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