112088-73-0Relevant academic research and scientific papers
Synthesis and anticonvulsant activity of novel purine derivatives
Wang, Shi-Ben,Jin, Peng,Li, Fu-Nan,Quan, Zhe-Shan
, p. 574 - 583 (2015/03/14)
A series of new purines containing triazole and other heterocycle substituents was synthesized and evaluated for their preliminary anticonvulsant activity and neurotoxicity by using the maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) and rotarod neurotoxicity (TOX) tests. Among the compounds studied, 9-decyl-6-(1H-1,2,4-triazol-1-yl)-9H-purine (5e) was the most potent compound, with a median effective dose of 23.4 mg/kg and a high protective index of more than 25.6 after intraperitoneal administration in mice. Compound 5e showed significant oral activity against MESinduced seizures in mice, with an ED50 of 39.4 mg/kg and a PI above 31.6. These results demonstrate that compound 5e possesses better anticonvulsant activity and is safer than the commercially available drugs carbamazepine and valproate in MES, scPTZ and TOX models.
Metal-free, highly efficient organocatalytic amination of benzylic C-H bonds
Xue, Qicai,Xie, Jin,Li, Huamin,Cheng, Yixiang,Zhu, Chengjian
supporting information, p. 3700 - 3702 (2013/05/09)
A new synthetic approach toward direct C-N bond formation through sp 3 C-H activation has been developed under metal-free conditions. Both primary and secondary benzylic C-H substrates could react smoothly with various amines to give only mono-amination products with good to excellent yields. The Royal Society of Chemistry 2013.
Purine compounds
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Page/Page column 3, (2010/11/28)
The invention provides an antimycobacterial 6-aryl-9-(m- or p-substituted-benzyl) purine and purine analog compounds.
Synthesis, biological activity, and SAR of antimycobacterial 9-aryl-, 9-arylsulfonyl-, and 9-benzyl-6-(2-furyl)purines
Bakkestuen, Anne Kristin,Gundersen, Lise-Lotte,Utenova, Bibigul T.
, p. 2710 - 2723 (2007/10/03)
9-Aryl-, 9-arylsulfonyl- and 9-benzyl-6-(2-furyl)purines were synthesized by N-alkylation or N-arylation of the purine followed by Stille coupling to introduce the furyl substituent in the 6-position and the compounds screened for activity against Mycobac
Synthesis and structure-activity relationships of 2-substituted-6-(dimethylamino)-9-(4-methylbenzyl)-9H-purines with antirhinovirus activity
Kelley,Linn,Selway
, p. 218 - 224 (2007/10/02)
A series of 2-substituted-6-(dimethylamino)-9-(4-methylbenzyl)-9H-purines where the 2-substituent was H, F, Cl, CF3, CH3, CH2CH3, NH2, NHCH3, N(CH3)2, SCH3,
6-(Alkylamino)-9-benzyl-9H-purines. A New Class of Anticonvulsant Agents
Kelley, James L.,Krochmal, Mark P.,Linn, James A.,McLean, Ed W.,Soroko, Francis E.
, p. 606 - 612 (2007/10/02)
Several 9-alkyl-6-substituted-purines were synthesized and tested for anticonvulsant activity against maximal electroshock-induced seizures (MES) in rats.Most compounds were prepared in three steps from 5-amino-4,6-dichloropyrimidine or in two steps via alkylation of 6-chloropurine.Potent anticonvulsant activity against MES resided in compounds that contain a benzyl substituent at the 9-position of 6-(methylamino)- or 6-(dimethylamino)purine.Among commonly used agents for control of seizures, this type of structure represents a new class of potent anticonvulsant agents.
