Abstract
The synthesis of 3-aralkyl-4-aryl-4H-, 3-aralkylamino-4-aryl-4H- and 3-aralkylsulfanyl-4-aryl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1, 1-dioxides is described. Moreover, the affinity of the different compounds towards the cholecystokinin CCK-A and CCK-B receptors was evaluated. For selected compounds, affinity on the two receptor subtypes was expressed in the micromolar range. This was comparable to the affinity observed with the naturally occurring CCK receptor antagonist asperlicin.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Chemical Phenomena
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Chemistry, Physical
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Kinetics
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Ligands
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Male
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Quinazolines / chemistry
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Rats
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Rats, Wistar
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Receptor, Cholecystokinin A
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Receptor, Cholecystokinin B
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Receptors, Cholecystokinin / metabolism*
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Sincalide / metabolism
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Structure-Activity Relationship
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Thiadiazines / chemical synthesis*
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Thiadiazines / metabolism*
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Thiadiazines / pharmacology
Substances
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Ligands
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Quinazolines
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Receptor, Cholecystokinin A
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Receptor, Cholecystokinin B
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Receptors, Cholecystokinin
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Thiadiazines
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Sincalide