On the bioactive conformation of the GABA uptake inhibitor SK and F 89976-A

DOI: 10.1016/S0960-894X(96)00268-5

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1535 - 1540 (1996)

Update date:2022-08-03

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Authors:

Dhar, T. G. Murali

Nakanishi, Hiroshi

Borden, Laurence A.

Gluchowski, Charles

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Article abstract of DOI:10.1016/S0960-894X(96)00268-5

SK and F 89976-A (3) is a potent GABA uptake inhibitor, with a flexible diphenylbutenyl side chain. Conformationally restrained analogues of this compound, 14, 16, 18 and 20 were designed and synthesized to study the conformational preferences for binding to cloned GABA transporters. We conclude from this study that SK and F 89976-A probably binds to the GABA transporter in its fully extended conformation.

Full text of DOI:10.1016/S0960-894X(96)00268-5

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