Hashimoto, K.; Yanagida, M.; Horikawa, M.; Shirahama, H. published an article in 1989, the title of the article was Syntheses and neuroexcitatory activity of kainoids.Category: alcohols-buliding-blocks And the article contains the following content:
Kainoids, such as kainic acid, domoic acid, acromelic acids A and B, cause marked depolarization against L-glutamate receptor in vertebrates and invertebrates. To find the more potent kainoids and to reveal the structure-activity relationship, efforts were made toward the syntheses of kainoids and related compounds The most rational synthesis of kainoid, i.e., introduction of various substituents to a common intermediate, was achieved by the use of diaryl copper lithium reagent for the substitution reaction of trans-4-tosyloxyproline with retention of configuration. Neuroexcitatory activity of the synthetic compounds was also examined Among the 6 acyclic analogs of kainoid, only the (2S,3R)-isomers, which have π-electrons on the β-substituent, showed neuroexcitatory activity. In the newly synthesized kainoids, the Ph derivative (I) showed comparable activity to kainic acid, the phenol derivative (II) exhibited more potent activity than acromelic acid B or domoic acid, and the methoxyphenyl derivative (III) was 3- to 5-fold more potent than acromelic acid A, and the most potent excitatory reagent known so far. The experimental process involved the reaction of Isochroman-3-ol(cas: 42900-89-0).Category: alcohols-buliding-blocks
The Article related to kainoid preparation neuroexcitatory, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Category: alcohols-buliding-blocks
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts