Synthesis and antiallergic activity of some acidic derivatives of 4H-pyrimido[2,1-b]benzazol-4-ones.

doi:10.1021/JM00358A031

Paper

Synthesis and antiallergic activity of some acidic derivatives of 4H-pyrimido[2,1-b]benzazol-4-ones.

Published Apr 1, 1983 · J. J. Wade, C. Toso, C. Matson

Journal of medicinal chemistry

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38

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0

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Abstract

Reactions of 2-aminobenzothiazole, 2-aminobenzoxazole, and 2-amino-1-methylbenzimidazole with dimethyl aminofumarate (DMAF) or diethyl ethoxymethylenemalonate (DEEM) led to 2- or 3-carboxy-4H-pyrimido[2,1-b]-benzazol-4-ones, respectively. Subsequent derivatization of these carboxylic acids gave the corresponding tetrazolylcarboxamides and tetrazoles. These acidic compounds were tested in the rat passive cutaneous anaphylaxis (PCA) assay as potential antiallergic agents. Many of the compounds displayed activity comparable to that shown by disodium cromoglycate (DSCG) when tested by the intraperitoneal route, and some, unlike DSCG, also showed activity when tested orally.

In Vitro Study

Study Snapshot

Acidic derivatives of 4H-pyrimido[2,1-b]benzazol-4-ones show potential antiallergic activity, with some showing activity both orally and intraperitoneally.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and antiallergic activity of some acidic derivatives of 4H-pyrimido[2,1-b]benzazol-4-ones.

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References

Citations

Fe3O4@SiO2‐APA‐Amide/Imid‐NiCl2 as a New Nano‐Magnetic Catalyst for the Synthesis of 4H‐Pyrimido[2,1‐b]benzothiazole Derivatives via MCRs Under Solvent‐Free Conditions

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An efficient organopromotor L‐arginine facilitated synthesis of thiazolo[3,2‐a]pyrimidine derivatives in EtOH:H2O solvent

L-arginine catalyzed synthesis of thiazolo[3,2a]pyrimidines in EtOH:H2O solvent offers recyclability, operational simplicity, wide substrate scope, easy work-up, and high atom economy compared to existing strategies.

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This chiral guanidine-catalyzed cycloaddition process provides a high-yield, efficient, and versatile method for synthesis of benzothiazolopyrimidines with potential utility in various fields.

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NHC-catalyzed Mannich/lactamization domino reaction reveals that the fifth step determines the stereochemistry and regioselectivity, aiding in rational catalyst design for analogous reactions.

Synthesis of A Novel Heterocyclic System of 3,8-Disubstituted-5H-Pyrimido[5’,4’:5,6][1,4]Thiazino[3,2-e][1,2,4]Triazine

This study synthesized a novel heterocyclic system of 3,8-disubstituted-5H-pyrimido[5',4':5,6][1,4]thiazino[3,2-e][1,2,4]triazine ring systems, providing new synthesis

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Novel pyrimido oxazine compounds were synthesized using benzaldehyde, phenyl acetylene, and urea, with potential applications in nucleophilic reactions.

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New pyrimido[5′,4′:5,6][1,4]thiazino[2,3b]quinoxaline derivatives can be synthesized in one step using 5amino6-methylpyrimidine-4-thiols and 2,3-dichloroquino

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