Stereochemical Pattern Recognition

Antagonists - Recent structure-activity studies of Hj -receptor antihistamines have been concerned with stereochemical aspects, partition characteristics, pattern recognition, affinity contributions to activity and association phenomena. The subject has also been reviewed recently. Undoubtedly, the main focus of attention has been on the H2 receptor histamine antagonists. Three compounds have been widely studied, viz. burimamide (13b), metiamide (13c) and cimetidine (13d), and their pharmacological properties summarized. 3 Their discovery and development at SK F was the culmination of a research programme initiated in 1964. The search for an antagonist and some of the medicinal chemical approaches used in the structure-activity analysis have been outlined in several articles. Concurrently, other researchers had sought... 

Substrate binding by this carrier requires the correct stereochemical placement of three closely spaced hydroxyls for recognition and the existence of a relatively hydrophobic surface of suitable shape and size. The general pattern is very similar to that described by the laboratory of Lemiex (13) for binding of carbohydrate antigens. 

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