Search for the pharmacophore in prazosin for Transport-P.
Partial structures of prazosin have been synthesised and tested for inhibition of Transport-P in order to identify the structural features of prazosin, which appear to be involved in binding to the putative transporter. It is shown that the pyrimidinyl 4-amino group is critically important for binding but that the 6,7-dimethoxy and 2-furoyl groups are not essential.
Zunszain
Patricia A
PA
Department of Chemistry, Christopher Ingold Laboratories, University College London, 20 Gordon Street, London WC1H 0AJ, UK.
Federico
Cesare
C
Sechi
Mario
M
Al-Damluji
Saad
S
Ganellin
C Robin
CR
D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D011224:Prazosin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D025262:Vacuolar Proton-Translocating ATPases / Q000037:antagonists & inhibitors* / Q000378:metabolism
D025262:Vacuolar Proton-Translocating ATPases; D011224:Prazosin