
Bioorganic and Medicinal Chemistry Letters p. 887 - 892 (2015)
Update date:2022-08-04
Topics:
Sasmal, Pradip K.
Krishna, C. Vamsee
Adabala, S. Sudheerkumar
Roshaiah
Rawoof, Khaji Abdul
Thadi, Emima
Sukumar, K. Pavan
Cheera, Srisailam
Abbineni, Chandrasekhar
Rao, K.V.L. Narasimha
Prasanthi
Nijhawan, Kamal
Jaleel, Mahaboobi
Iyer, Lakshmi Ramachandran
Chaitanya, T. Krishna
Tiwari, Nirbhay Kumar
Krishna, N. Lavanya
Potluri, Vijay
Khanna, Ish
Frimurer, Thomas M.
Lückmann, Michael
Rist, ystein
Elster, Lisbeth
H?gberg, Thomas
Kappa opioid receptor (KOR) is an important mediator of pain signaling and it is targeted for the treatment of various pains. Pharmacophore based mining of databases led to the identification of 2-aminobenzimidazole derivative as KOR agonists with selectivity over the other opioid receptors DOR and MOR. A short SAR exploration with the objective of identifying more polar and hence less brain penetrant agonists is described herewith. Modeling studies of the recently published structures of KOR, DOR and MOR are used to explain the receptor selectivity. The synthesis, biological evaluation and SAR of novel benzimidazole derivatives as KOR agonists are described. The in vivo proof of principle for anti-nociceptive effect with a lead compound from this series is exemplified.
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