112088-75-2

Upstream product

• 122-51-0 orthoformic acid triethyl ester 
• 112088-63-8 6-chloro-N₄-[(4-fluorophenyl)methyl]-4,5-pyrimidinediamine 
• 459-49-4 p-bromobenzyl fluoride 
• 87-42-3 6-chloropurine 
• 459-46-1 4-Fluorobenzyl bromide 
• 140-75-0 para-fluorobenzylamine 
• 352-11-4 1-chloromethyl-4-fluorobenzene 

Downstream Products

• 125486-45-5 9-(4-Fluoro-benzyl)-6-(furan-2-ylmethoxy)-9H-purine 
• 125486-46-6 9-(4-Fluoro-benzyl)-6-(pyridin-3-ylmethoxy)-9H-purine 
• 112089-05-1 N,N-dimethyl-9-(4-fluorobenzyl)adenine 
• 125486-44-4 6-Benzyloxy-9-(4-fluoro-benzyl)-9H-purine 
• 213528-06-4 6-Amino-9-(4-fluorobenzyl)purine 
• 908255-41-4 6-(8-benzyloxyquinoline-7-carboxamido)-9-(4-fluorobenzyl)purine 
• 1145671-82-4 9-(4-fluorobenzyl)-6-[2-(N-isopropylamino)ethyl]amino-9H-purine 
• 1246307-55-0 6,6'-dichloro-9,9'-di[(4-fluorophenyl)methyl]-9H,9'H-[8,8']bipurinyl 

Relevant academic research and scientific papers

Synthesis and anticonvulsant activity of novel purine derivatives

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.

Synthesis and evaluation of anticonvulsant and antidepressant activities of 7-alkyl-7H-tetrazolo[1,5-g]purine derivatives

Seventeen 7-alkyl-7H-tetrazolo[1,5-g]purine derivatives were synthesized, and their anticonvulsant and antidepressant activities were evaluated in a mouse model. The anticonvulsant effect and neurotoxicity of the compounds were evaluated with a maximal electroshock test and a rotated test in mice, respectively. Most of the compounds had anticonvulsant activity; among the compounds studied, 7-(3-chlorobenzyl)-7H-tetrazolo[1,5-g]purine (3h) was found to be the most potent compound with a median effective dose (ED50) value of 28.9 mg/kg and a protective index value of 15.8, possessing better anticonvulsant activity and higher safety than the marketed drug carbamazepine. To explain the possible mechanism of anticonvulsant activity, compound 3h was tested in pentylenetetrazole-induced seizures tests, and the results suggest that compound 3h exerts anticonvulsant activity through a GABA-mediated mechanism. Forced swimming test showed that at a dose of 40 mg/kg, five compounds have significant antidepressant activity, the most active compound was 7-(2-chlorobenzyl)-7H-tetrazolo[1,5-g]purine (3g), which decreased immobility time by 56 %.

Purine compounds

The invention provides an antimycobacterial 6-aryl-9-(m- or p-substituted-benzyl) purine and purine analog compounds.

Synthesis and biological evaluation of purine derivatives incorporating metal chelating ligands as HIV integrase inhibitors

Because of its essential role in HIV replication and lack of human counterpart, HIV integrase is an attractive target for the development of novel anti-AIDS agents. Among the recently developed integrase inhibitors, only the α,γ-diketo acid (DKA) compound

Synthesis, biological activity, and SAR of antimycobacterial 9-aryl-, 9-arylsulfonyl-, and 9-benzyl-6-(2-furyl)purines

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 OF 9-SUBSTITUTED 6-ALKOXYPURINES UNDER CONDITIONS OF PHASE-TRANSFER CATALYSIS

9-Substituted 6-alkoxypurines were synthesized by the nucleophilic substitution of chlorine in 9-substituted 6-chloropurines under the conditions of phase-transfer catalysis in the benzene-50percent aqueous sodium hydroxide system.

6-(Alkylamino)-9-benzyl-9H-purines. A New Class of Anticonvulsant Agents

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.