Chemical and Pharmaceutical Bulletin, 1992/09/25, Vol.40(9), pp.2391-2398
1992
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and Antiallergy Activity of [1, 3, 4]Thiadiazolo[3, 2-α]-1, 2, 3-triazolo[4, 5-d]pyrimidin-9(3H)-one Derivatives. II. 6-Alkyl- and 6-Cycloalkylalkyl Derivatives
- Ist Teil von
- Chemical and Pharmaceutical Bulletin, 1992/09/25, Vol.40(9), pp.2391-2398
- Ort / Verlag
- Tokyo: The Pharmaceutical Society of Japan
- Erscheinungsjahr
- 1992
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A suries of 6-alkyl- or 6-(cycloalkylalkyl)-[1, 3, 4]thiadiazolo[3, 2-α]-1, 2, 3-triazolo[4, 5-d]pyrimidin-9(3H)-ones 1b-o was synthesized from the corresponding 1, 3, 4-thiadiazol-5-animes 3b-o and the antiallergic activities of the products were evaluated. Among the compounds 6-(2-cyclohexylethyl)-[1, 3, 4]thiadiazolo[3, 2-α]-1, 2, 3-triazolo[4, 5-d]pyrimidin-9(3H)-one 1h, whose X-ray crystallographic stereostructure is shown, was found to be a promising new antiallergic agent, which has low toxicity and dual activity as a leukotriene D4 receptor antagonist and as an orally active mast cell stabilizer.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0009-2363eISSN: 1347-5223DOI: 10.1248/cpb.40.2391Titel-ID: cdi_proquest_journals_1460266181
- Format
- –
- Schlagworte
- [1, 3, 4]thiadiazolo[3, 2-α]-1, 2, 3-triazolo[4, 5-d]pyrimidin-9(3H)-one, Animals, antagonist, antiallergy, Chemistry, Condensed matter: structure, mechanical and thermal properties, Exact sciences and technology, Female, Guinea Pigs, Heterocyclic compounds, Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms, Hypersensitivity - drug therapy, In Vitro Techniques, leukotriene d4, Lung - drug effects, Muscle Contraction - drug effects, Organic chemistry, Organic compounds, Ovalbumin - immunology, passive cutaneous anaphylaxis, Passive Cutaneous Anaphylaxis - drug effects, Physics, Preparations and properties, Pyrimidines - chemical synthesis, Pyrimidines - pharmacology, Rats, Rats, Sprague-Dawley, SRS-A - antagonists & inhibitors, stereostructure, Structure of solids and liquids, crystallography, Structure of specific crystalline solids, Thiadiazoles - chemical synthesis, Thiadiazoles - pharmacology, Triazoles - chemical synthesis, Triazoles - pharmacology, X-ray analysis, X-Ray Diffraction