BIOMAT Database Logo BIOMAT Database Logo

[Synthesis of 4,5-diarylthiazole derivatives as blood platelet aggregation inhibitors]. 1990

S Konno, and M Amano, and M Sagi, and H Yamanaka
Pharmaceutical Institute, Tohoku University, Sendai, Japan.

A number of 2-substituted 4,5-diphenylthiazoles were synthesized by the nucleophilic substitution of 2-methylsulfonyl-4,5-diphenylthiazole with various sodium alkoxides, amines, and carbanions of active methylene compounds. 2-Methylsulfonyl-4,5-diphenylthiazole was obtained by the potassium permanganate oxidation of 2-methylthio-4,5-diphenylthiazole in the presence of a phase-transfer catalyst. 2-Ethoxy-4,5-bis(4-methoxyphenyl) thiazole was prepared in a similar manner. 2-Ethynyl-4,5-diphenylthiazoles were synthesized by the palladium catalyst cross-coupling reaction of 2-iodo-4,5-diphenylthiazole with monosubstituted acetylenes. These compounds were tested for inhibitory activity against blood platelet aggregation in vitro. Among them, 2-alkoxy-, and 2-(4-methylpiperazin-1-yl)-4,5-diphenylthiazole were found to have potent inhibitory activity.

UI MeSH Term Description Entries
D010975 Platelet Aggregation Inhibitors Drugs or agents which antagonize or impair any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. Antiaggregants, Platelet,Antiplatelet Agent,Antiplatelet Agents,Antiplatelet Drug,Blood Platelet Aggregation Inhibitor,Blood Platelet Antagonist,Blood Platelet Antiaggregant,PAR-1 Antagonists,Platelet Aggregation Inhibitor,Platelet Antagonist,Platelet Antagonists,Platelet Antiaggregant,Platelet Antiaggregants,Platelet Inhibitor,Protease-Activated Receptor-1 Antagonists,Antiplatelet Drugs,Blood Platelet Aggregation Inhibitors,Blood Platelet Antagonists,Blood Platelet Antiaggregants,Platelet Inhibitors,Agent, Antiplatelet,Aggregation Inhibitor, Platelet,Antagonist, Blood Platelet,Antagonist, Platelet,Antiaggregant, Blood Platelet,Antiaggregant, Platelet,Drug, Antiplatelet,Inhibitor, Platelet,Inhibitor, Platelet Aggregation,PAR 1 Antagonists,Platelet Antagonist, Blood,Platelet Antiaggregant, Blood,Protease Activated Receptor 1 Antagonists
D002627 Chemistry, Physical The study of CHEMICAL PHENOMENA and processes in terms of the underlying PHYSICAL PHENOMENA and processes. Physical Chemistry,Chemistries, Physical,Physical Chemistries
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001555 Benzene Derivatives Organic compounds derived from BENZENE. Derivatives, Benzene
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D013844 Thiazoles Heterocyclic compounds where the ring system is composed of three CARBON atoms, a SULFUR and NITROGEN atoms. Thiazole
D055598 Chemical Phenomena The composition, structure, conformation, and properties of atoms and molecules, and their reaction and interaction processes. Chemical Concepts,Chemical Processes,Physical Chemistry Concepts,Physical Chemistry Processes,Physicochemical Concepts,Physicochemical Phenomena,Physicochemical Processes,Chemical Phenomenon,Chemical Process,Physical Chemistry Phenomena,Physical Chemistry Process,Physicochemical Phenomenon,Physicochemical Process,Chemical Concept,Chemistry Process, Physical,Chemistry Processes, Physical,Concept, Chemical,Concept, Physical Chemistry,Concept, Physicochemical,Concepts, Chemical,Concepts, Physical Chemistry,Concepts, Physicochemical,Phenomena, Chemical,Phenomena, Physical Chemistry,Phenomena, Physicochemical,Phenomenon, Chemical,Phenomenon, Physicochemical,Physical Chemistry Concept,Physicochemical Concept,Process, Chemical,Process, Physical Chemistry,Process, Physicochemical,Processes, Chemical,Processes, Physical Chemistry,Processes, Physicochemical

Related Publications

S Konno, and M Amano, and M Sagi, and H Yamanaka
New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics.
October 1991, Journal of medicinal chemistry,
S Konno, and M Amano, and M Sagi, and H Yamanaka
Some pyrrolidine and pyrrolizine derivatives as inhibitors of blood platelet aggregation.
January 1980, Arzneimittel-Forschung,
S Konno, and M Amano, and M Sagi, and H Yamanaka
Bicyclic thiophenic derivatives as platelet aggregation inhibitors.
June 1986, Il Farmaco; edizione scientifica,
S Konno, and M Amano, and M Sagi, and H Yamanaka
New pyrazolylhydrazone derivatives as inhibitors of platelet aggregation.
July 1993, The Journal of pharmacy and pharmacology,
S Konno, and M Amano, and M Sagi, and H Yamanaka
Design, synthesis and evaluation of 1,4-benzodioxine derivatives as novel platelet aggregation inhibitors.
February 2018, Future medicinal chemistry,
S Konno, and M Amano, and M Sagi, and H Yamanaka
[Imidazole derivatives, platelet aggregation inhibitors].
January 1997, Annales pharmaceutiques francaises,
S Konno, and M Amano, and M Sagi, and H Yamanaka
[Synthesis of new platelet aggregation inhibitors substituted with pyridylisoxazoles and their 4,5-dihydroanalogs].
December 1995, Bioorganicheskaia khimiia,
S Konno, and M Amano, and M Sagi, and H Yamanaka
Naphthylalkyl lactamimides as inhibitors of blood platelet aggregation.
December 1972, Journal of medicinal chemistry,
S Konno, and M Amano, and M Sagi, and H Yamanaka
2,2'-Dithiodibenzamides as inhibitors of blood platelet aggregation.
March 1985, Chemical & pharmaceutical bulletin,
S Konno, and M Amano, and M Sagi, and H Yamanaka
4-(1H-pyrazol-1-yl)-2-butylamine derivatives as inhibitors of blood platelet aggregation.
May 1989, Farmaco (Societa chimica italiana : 1989),
Copied contents to your clipboard!