TRPV1 modulators: Structure–activity relationships using a rational combinatorial approach

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• 作者：Laura Zaccaro^a ; ^b ; M. Teresa Garc&#xed ; a-Ló ; pez^c ; Rosario Gonzá ; lez-Muñ ; iz^c ; ; Carolina Garc&#xed ; a-Mart&#xed ; nez^d ; Antonio Ferrer-Montiel^d ; Fernando Albericio^e ; ^f ; ^g ; Miriam Royo^a ; ^f ; ^{mroyo@pcb.ub.cat"" rel=""nofollow}
• 关键词：Hydantoins ; Dipeptides ; Combinatorial library ; TRPV1 ; SAR studies
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 June 2011
• 年：2011
• 卷：21
• 期：12
• 页码：3541-3545
• 全文大小：632 K

文摘

A discrete library of linear and hydantoin-containing dipeptide derivatives, based on the Lys-Trp(Nps) scaffold, was prepared by solid-phase synthesis. SAR studies indicated that potency for TRPV1 blockade and selectivity towards NMDA is mainly dictated by the side-chain length and the basic nature of α, ω-groups in the N-terminal residue. The 2-Nps moiety at position 2 of Trp indole ring is preferred over the 2-pyridine one.