On July 10, 2008, Kim, Young Ah; Sharon, Ashoke; Chu, Chung K.; Rais, Reem H.; Al Safarjalani, Omar N.; Naguib, Fardos N. M.; El Kouni, Mahmoud H. published an article.Recommanded Product: 72364-46-6 The title of the article was Structure-Activity Relationships of 7-Deaza-6-benzylthioinosine Analogues as Ligands of Toxoplasma gondii Adenosine Kinase. And the article contained the following:
Several 7-deaza-6-benzylthioinosine analogs with varied substituents on aromatic ring were synthesized and evaluated against Toxoplasma gondii adenosine kinase (EC.2.7.1.20). Structure-activity relationships indicated that the nitrogen atom at the 7-position does not appear to be a critical structural requirement. Mol. modeling reveals that the 7-deazapurine motif provided flexibility to the 6-benzylthio group as a result of the absence of H-bonding between N7 and Thr140. This flexibility allowed better fitting of the 6-benzylthio group into the hydrophobic pocket of the enzyme at the 6-position. In general, single substitutions at the para or meta position enhanced binding. On the other hand, single substitutions at the ortho position led to the loss of binding affinity. The most potent compounds, 7-deaza-p-cyano-6-benzylthioinosine I (R = CN) (IC50 = 5.3 μM) and 7-deaza-p-methoxy-6-benzylthioinosine I (R = OCH3) (IC50 = 4.6 μM), were evaluated in cell culture to delineate their selective toxicity. The experimental process involved the reaction of (2-Fluorophenyl)methanethiol(cas: 72364-46-6).Recommanded Product: 72364-46-6
The Article related to deazabenzylthioinosine nucleoside asym preparation, ribose stereoselective glycosylation benzylthiol benzylhalide nucleophilic substitution, toxoplasma gondii adenosine kinase binding affinity structure activity relationship, mol modeling toxoplasmosis antitoxoplasmic antiparasitic human and other aspects.Recommanded Product: 72364-46-6
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