BIOMAT Database Logo BIOMAT Database Logo

Potential histamine H2-receptor antagonists. Synthesis, conformational studies and activity of novel 3-oxo-1,2,5-thiadiazole 1,1-dioxide derivatives. 1990

V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
Instituto de Química Médica (CSIC), Madrid, Spain.

New histamine H2-receptor antagonists bearing a novel "urea equivalent", the 3-oxo-1,2,5-thiadiazole 1,1-dioxide ring, have been synthesized in a transamination reaction. Open chain derivatives have also been obtained. Theoretical conformational analysis of the compounds has been carried out using a molecular modelling program. Semiempirical CNDO/2 calculations have also been performed. The antisecretory and cytoprotective activities of the compounds have been evaluated.

UI MeSH Term Description Entries
D008297 Male Males
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D008968 Molecular Conformation The characteristic three-dimensional shape of a molecule. Molecular Configuration,3D Molecular Structure,Configuration, Molecular,Molecular Structure, Three Dimensional,Three Dimensional Molecular Structure,3D Molecular Structures,Configurations, Molecular,Conformation, Molecular,Conformations, Molecular,Molecular Configurations,Molecular Conformations,Molecular Structure, 3D,Molecular Structures, 3D,Structure, 3D Molecular,Structures, 3D Molecular
D009682 Magnetic Resonance Spectroscopy Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING). In Vivo NMR Spectroscopy,MR Spectroscopy,Magnetic Resonance,NMR Spectroscopy,NMR Spectroscopy, In Vivo,Nuclear Magnetic Resonance,Spectroscopy, Magnetic Resonance,Spectroscopy, NMR,Spectroscopy, Nuclear Magnetic Resonance,Magnetic Resonance Spectroscopies,Magnetic Resonance, Nuclear,NMR Spectroscopies,Resonance Spectroscopy, Magnetic,Resonance, Magnetic,Resonance, Nuclear Magnetic,Spectroscopies, NMR,Spectroscopy, MR
D011708 Pylorus The region of the STOMACH at the junction with the DUODENUM. It is marked by the thickening of circular muscle layers forming the pyloric sphincter to control the opening and closure of the lumen. Pyloric Sphincter,Pyloric Sphincters,Sphincter, Pyloric,Sphincters, Pyloric
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
D002470 Cell Survival The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability. Cell Viability,Cell Viabilities,Survival, Cell,Viabilities, Cell,Viability, Cell
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
D000897 Anti-Ulcer Agents Various agents with different action mechanisms used to treat or ameliorate PEPTIC ULCER or irritation of the gastrointestinal tract. This has included ANTIBIOTICS to treat HELICOBACTER INFECTIONS; HISTAMINE H2 ANTAGONISTS to reduce GASTRIC ACID secretion; and ANTACIDS for symptomatic relief. Anti-Ulcer Drugs,Agents, Anti-Ulcer,Anti Ulcer Agents,Anti Ulcer Drugs,Drugs, Anti-Ulcer

Related Publications

V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
1,2,5-thiadiazole 1-oxide and 1,1-dioxide derivatives. A new class of potent histamine H2-receptor antagonists.
March 1982, Journal of medicinal chemistry,
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
Potential histamine H2-receptor antagonists: synthesis and pharmacological activity of derivatives containing acylamino-furazan moieties.
March 1992, Archiv der Pharmazie,
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
Potential histamine H2-receptor antagonists. 3. Methylhistamines.
July 1976, Journal of medicinal chemistry,
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
Synthesis and H2-antagonist properties of some 1,2,5-thiadiazole-1-oxide derivatives.
December 1992, Farmaco (Societa chimica italiana : 1989),
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
March 1982, Journal of medicinal chemistry,
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
Conformational analyses on histamine H2-receptor antagonists.
December 1990, Journal of computer-aided molecular design,
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
In vitro cytogenetic activity of 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide.
November 2021, Drug and chemical toxicology,
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
Potential histamine H2-receptor antagonists. Synthesis, structure and activity of a few open models related to classical H2-antagonists.
September 1989, Arzneimittel-Forschung,
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
A conformational approach to histamine H2-receptor antagonists.
August 1984, Il Farmaco; edizione scientifica,
V J Arán, and E Dávila, and M Francés, and P Goya, and J Gras, and A Martínez, and N Mylonakis, and I Pardo
Synthesis and activity of pyridine analogues of histamine H2-receptor antagonists.
December 1988, Drug design and delivery,
Copied contents to your clipboard!