New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine

DOI: 10.1016/S0960-894X(98)00181-4

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1133 - 1138 (1998)

Update date:2022-08-04

Topics:

Authors:

Ali, Syed M.

Tedford, Clark E.

Gregory, Rosilyn

Yates, Stephen L.

Phillips, James G.

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Article abstract of DOI:10.1016/S0960-894X(98)00181-4

New histamine H₃ receptor antagonists were developed using an acetylene moiety as a replacement for the amide-oxime functionality of verongamine 5. Optimization of receptor binding was performed by following aliphatic Topliss tree guidelines. These new H₃ ligands demonstrate excellent blood-brain barrier penetration.

Full text of DOI:10.1016/S0960-894X(98)00181-4

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