Antiallergy agents. 2. 2-Phenyl-5-(1H-tetrazol-5-yl)pyrimidin-4(3H)-ones

Abstract

Some 2-(2-alkoxyphenyl)-and 2-[2-(alkenyloxy)phenyl]-5-(l/f-tetrazol-5-yl)pyrimidin-4(3fí)-ones were prepared and found to be about 5-10 times more potent than the corresponding pyrimidine-5-carboxylic acids when tested orally against passive cutaneous anaphylaxis in the rat. Structure-activity relationships within the two series are similar. 2-(2-n-Propoxyphenyl)-5-(lH-tetrazol-5-yl)pyrimidin-4(3H)-one is in clinical trial for the prophylactic treatment of asthma.

trans-5,5′-[(2-Butene-1,4-diyl)dithio]bis(1-phenyl-1,2,3,4-tetrazole)

“…To date, a large number of¯exible or rigid chain-linked dithioether ligands containing N-heterocyclic moieties have been synthesized and investigated, due to their diverse coordination capabilities and the important properties of their metal complexes (Zheng et al, 2003;Bu et al, 2002;Hong et al, 2000). Earlier studies reported that several tetrazole derivatives possess diverse pharmacological properties (Juby et al, 1968(Juby et al, , 1982. However, crystallographic studies of only a few complexes of monosubstituted tetrazole derivatives have been reported (van den Heuvel et al, 1983;Lyakhov et al, 2003).…”

Synthesis and Characterization of Diazenyl-1,3-diphenylpropane-1,3-dione and 5-[Hydroxy(phenyl)methyl]-4-phenylpyrimidine Derivatives

“…The N-aminopyrimidine derivatives (1a-f) were used as important materials in the synthesis of the target heterocycles (Scheme-I) [6][7][8][9][10][11] . Briefly, the reactions of 1a-f were carried with 1,3-diketones and NaBH 4 .…”

“…They show various interesting pharmacological properties including antiviral, antibacterial, antitumour and antiflammatory effects. Some of them are frequently encountered in many drugs used for the treatment of hypothyroidy, hypertension, cancer chemotherapy and HIV infection [1][2][3][4][5] . There are published reports about the synthesis of some pyrimidine derivatives from furan-2,3diones [6][7][8][9][10][11] (Scheme-I).…”

A Facile Synthesis of 2-Amino-5-Cyano-4, 6-Disubstitutedpyrimidines under MWI

“…The major approach to the synthesis of mononuclear pyrimidines is the principal synthesis, involving the condensation of N-C-N fragment with an appropriate functionalized 3-carbon unit [3]. Various synthetic methods and reaction conditions have been employed for the synthesis of mononuclear pyrimidines in the literature [4][5][6][7][8][9][10][11][12][13][14][15][16][17].…”