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On the inhibition of capsaicin response in dorsal root ganglion neurons by nobilamide B and analogues: a structure–activity relationship study

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Abstract

Nobilamide B, a TRPV1 antagonist, and a series of Ala-substituted analogues were synthesized and their neuroactivity was assessed in a primary culture of dorsal root ganglion (DRG) neurons. Analogues 4, 6, and 7 showed comparable activity, affecting capsaicin response in neurons, in contrast to 2, 3, and 5 which showed minimal blocking. Compounds 2, 3, and 5 correspond to analogues in which D-Phe, D-Leu and D-allo-Thr have been substituted with Ala, respectively. The observed loss of bioactivity in these three analogues highlights the importance of D amino acids in the primary structure of nobilamide B.

Graphical abstract: On the inhibition of capsaicin response in dorsal root ganglion neurons by nobilamide B and analogues: a structure–activity relationship study

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Publication details

The article was received on 18 Jun 2018, accepted on 14 Aug 2018 and first published on 15 Aug 2018


Article type: Research Article
DOI: 10.1039/C8MD00304A
Citation: Med. Chem. Commun., 2018, Advance Article
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    On the inhibition of capsaicin response in dorsal root ganglion neurons by nobilamide B and analogues: a structure–activity relationship study

    O. J. V. Belleza, J. O. Tun, G. P. Concepcion and A. J. L. Villaraza, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8MD00304A

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