Cocaine structure-activity relationships

Singh, S. 2000. Chemistry, design, and structure - Activity relationship of cocaine antagonists. Chemistry Revue, 100 925-1024. 

A consideration of the structure-activity relationships of cocaine can focus on a number of key elements in the structure, as indicated below. Each of the following sections includes a discussion of the particular numbered structural element. 

Iso Y, Grajkowska E, Wroblewski JT et al (2006) Synthesis and structure-activity relationships of 3-[(2-methyl-1, 3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists search for cocaine medications. J Med Chem 49 1080-1100... 

Cocaine-like structure-activity relationships and cocaine-like agents... 

Carroll FI, Lewin AH, Boja JW, et al. Cocaine receptor biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter. J Med Chem 35 969-981. 

Deutsch HM, Shi Q, Gruszecka-Kowalik E, et al. Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogues. J Med Chem 1996 39 1201-1209. 

A chance observation made some time prior to the full structural elucidation of cocaine in fact led to one of the more important lasses of local anesthetics. It was found that the simple ethyl e. ter of p-aminobenzoic acid, benzocaine (25), showed activity. 1-. a local anesthetic. It is of interest to note that this drug, I 1rst introduced in 1903, is still in use today. Once the struc-iiire of cocaine was established, the presence of an alkanolamine iiiniety in cocaine prompted medicinal chemists to prepare esters "I aminobenzoic acids with acyclic alkanolamines. Formula 26 11 presents the putative relationship of the target substances with cocaine. 

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