Review Article

Recent Advances in the Synthesis of Xanthines: A Short Review

Table 2

Reported potent compounds of xanthines and their targets.

S. No.Substituted xanthine derivativeDisease targetPotent compounds reported

11,3,8- and 1,3,7,8-substituted xanthines derivatives [23]A2B and A1 adenosine receptors

28(cyclopentyloxy) phenylxanthines derivatives [24]A1 and A2 adenosine receptors

38-(phenoxymethyl) xanthine and 8-(3-phenylpropyl) xanthine derivatives [25]A2A adenosine receptor antagonistic properties

48-(p-substituted-phenyl/benzyl) xanthines derivatives [26]A2A adenosine receptor

51,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine and 1,3,7-trimethyl-8-(phenoxymethyl)-xanthine derivatives [27]A1 and A2A adenosine receptor antagonists

68-(1-prop-2-ynyl-1H-pyrazol-4-yl)-xanthine derivatives [28]A2B adenosine receptor antagonists

7Tetrahydropyrazino-annelated theophylline derivatives [29]Multi-targeted drugs with adenosine receptor (A1, A2A) and MAO-B antagonistic activity.

88-(2-nitroaryl) xanthines [30]Human A2A adenosine receptor

98-(3-phenylpropyl) xanthines 8-(2-phenylethyl) xanthines and 8-(phenoxymethyl) xanthines [31]Adenosine A1 receptors

10Carboxylate amides of 8-phenyl-1,3-dimethylxanthine [32]Adenosine A2A receptors

116-amino-5-carboxamidouracils [33]

121,3-substituted 8-styrylxanthines [34]A1 and A2A adenosine receptors antagonist

13Tetrahydropyrimido[2,1-f] purinediones derivatives [35]A2B adenosine receptor antagonists

148-benzyltetrahydropyrazino [2,1-f] purinediones derivatives [36]Dual-target-directed A1/A2A adenosine receptor antagonists

151,3-dialkyl-substituted tetrahydropyrimido [1,2-f]purine-2,4-diones [37]Human A2A adenosine receptor antagonists

168-benzyl-substituted tetrahydropyrazino [2,1-f] purinediones [38]Dual A1/A2A adenosine receptor antagonists

17Xanthine derivatives [39]Antimicrobial and antioxidant activities

188-alkylmercaptocaffeine derivatives [40]

198-substituted xanthine derivatives [41]A2A adenosine receptor antagonists

201,2,3-triazole-based xanthine derivatives [42]Dipeptidyl peptidase-4 inhibitors

213-benzyl-8-propylxanthinyl-7-acetic acid [43]

221,3,8-substituted tetrahydropyrazino [2,1-f] purinediones [44]A1 and A2A adenosine receptors and MAO-B