Synthesis and evaluation of new pyridyl/pyrazinyl thiourea derivatives: Neuroprotection against amyloid-尾-induced toxicity was written by Park, Jung-eun;Elkamhawy, Ahmed;Hassan, Ahmed H. E.;Pae, Ae Nim;Lee, Jiyoun;Paik, Sora;Park, Beoung-Geon;Roh, Eun Joo. And the article was included in European Journal of Medicinal Chemistry in 2017.Formula: C4H7NS The following contents are mentioned in the article:
Herein, synthesis and evaluation of twenty six new pyridyl/pyrazinyl thiourea derivatives I (X = CH, N; R1 = H, 3-F, 2-Cl, 3-Cl; R2 = Et, i-Pr, Bn, etc.) against 尾 amyloid (A尾)-induced opening of mitochondrial permeability transition pore (mPTP) using JC-1 assay which measures the change of mitochondrial membrane potential (螖唯m) were reported. The neuroprotective effect of seventeen compounds against A尾-induced mPTP opening was superior to that of the standard Cyclosporin A (CsA). Fifteen derivatives eliciting increased green to red fluorescence percentage less than 40.0% were evaluated for their impact on ATP production, cell viability and neuroprotection against A尾-induced neuronal cell death. Among evaluated compounds, derivatives I (X = N; R1 = 3-F; R2 = 4-MeC6H4), I (X = CH; R1 = 3-Cl; R2 = 3-ClC6H4), I (X = CH; R1 = 3-F; R2 = 1-naphthyl), had safe profile regarding ATP production and cell viability. In addition, they exhibited significant neuroprotection (69.3, 51.8 and 48.2% resp.). Mol. modeling study using CDocker algorithm predicted plausible binding modes explaining the elicited mPTP blocking activity. Hence, this study suggests compounds I (X = N; R1 = 3-F; R2 = 4-MeC6H4), I (X = CH; R1 = 3-Cl; R2 = 3-ClC6H4) and I (X = CH; R1 = 3-F; R2 = 1-naphthyl) as leads for further development of novel therapy to Alzheimer’s disease. This study involved multiple reactions and reactants, such as Isopropylisothiocyanate (cas: 2253-73-8Formula: C4H7NS).
Isopropylisothiocyanate (cas: 2253-73-8) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.Formula: C4H7NS
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics