[Synthesis of benzofuran derivatives with H2 antagonist activity]. 1983

A Leonardi, and G Nava, and D Nardi

N-[2-(7-Dimethylaminomethyl-5-methyl-2-benzofuranmethylthio)ethyl]-N'-methyl-2-nitro-1,1-ethenediamine (III) and N-cyano-N'-[2-(7-dimethylaminomethyl-5-methyl-2-benzofuranmethylthio)ethyl]-N"-methylguanidine (IV) were synthesized. The direct transformation of 2,2-dicarbethoxy-3-hydroxy-5-methyl-7-dimethylaminomethylcoumaran (VII) and of 2,2-dicarbethoxy-3-hydroxycoumaran (XVI) to the corresponding ethyl 2-benzofurancarboxylates (IX) and (XV) is also reported. A mechanism for this reaction is proposed. Compounds (III) and (IV) showed hystamine H2 receptor antagonist activity, but were less potent than cimetidine and ranitidine.

UI MeSH Term Description Entries
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D005260 Female Females
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006635 Histamine H2 Antagonists Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood. Antihistaminics, H2,H2 Receptor Blockader,Histamine H2 Antagonist,Histamine H2 Blocker,Histamine H2 Receptor Antagonist,Histamine H2 Receptor Antagonists,Histamine H2 Receptor Blockader,Histamine H2 Receptor Blockaders,Antagonists, Histamine H2,Blockaders, Histamine H2 Receptor,H2 Receptor Blockaders,Histamine H2 Blockers,Receptor Antagonists, Histamine H2,Receptor Blockaders, H2,Antagonist, Histamine H2,Blockader, H2 Receptor,Blockaders, H2 Receptor,Blocker, Histamine H2,Blockers, Histamine H2,H2 Antagonist, Histamine,H2 Antagonists, Histamine,H2 Antihistaminics,H2 Blocker, Histamine,H2 Blockers, Histamine,Receptor Blockader, H2
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001572 Benzofurans Compounds that contain a BENZENE ring fused to a furan ring. Coumarones,Diphenylbenzofuran
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D066298 In Vitro Techniques Methods to study reactions or processes taking place in an artificial environment outside the living organism. In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In

Related Publications

A Leonardi, and G Nava, and D Nardi
August 1988, Chemical & pharmaceutical bulletin,
A Leonardi, and G Nava, and D Nardi
February 1981, Journal of medicinal chemistry,
A Leonardi, and G Nava, and D Nardi
January 1985, Arzneimittel-Forschung,
A Leonardi, and G Nava, and D Nardi
December 1993, Arzneimittel-Forschung,
A Leonardi, and G Nava, and D Nardi
January 1989, Acta poloniae pharmaceutica,
A Leonardi, and G Nava, and D Nardi
July 1971, Arzneimittel-Forschung,
A Leonardi, and G Nava, and D Nardi
May 1970, Arzneimittel-Forschung,
A Leonardi, and G Nava, and D Nardi
September 1982, Journal of pharmaceutical sciences,
A Leonardi, and G Nava, and D Nardi
December 1992, Farmaco (Societa chimica italiana : 1989),
Copied contents to your clipboard!