Synthesis and pharmacological evaluation of novel N-aryl-3, 4-dihydro-1′ H-spiro [chromene-2, 4′-piperidine]-1′-carboxamides as TRPM8 antagonists

…, N Khairatkar-Joshi, I Mukhopadhyay, PV Karnik…

文献索引：Chaudhari, Sachin S.; Kadam, Ashok B.; Khairatkar-Joshi, Neelima; Mukhopadhyay, Indranil; Karnik, Pallavi V.; Raghuram, Anupindi; Rao, Shobha S.; Vaiyapuri, Thamil Selvan; Wale, Dinesh P.; Bhosale, Vikram M.; Gudi, Girish S.; Sangana, Ramchandra R.; Thomas, Abraham Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 21 p. 6542 - 6553

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被引用次数: 11

摘要

Abstract A novel series of N-aryl-3, 4-dihydro-1′ H-spiro [chromene-2, 4′-piperidine]-1′- carboxamides was identified as transient receptor potential melastatin 8 (TRPM8) channel blockers through analogue-based rational design, synthesis and screening. Details of the synthesis, effect of aryl groups and their substituents on in-vitro potency were studied. The effects of selected functional groups on the 4-position of the chromene ring were also ...