Protective effects of 6-ureido/thioureido-2,4,5-trimethylpyridin-3-ols against 4-hydroxynonenal-induced cell death in adult retinal pigment epithelial-19 cells was written by Bae, Dawon;Gautam, Jaya;Jang, Hyeonjin;Banskota, Suhrid;Lee, Sang Yeul;Jeong, Min-Ji;Kim, A.-Sol;Kim, Hong Chul;Lee, Iyn-Hyang;Nam, Tae-gyu;Kim, Jung-Ae;Jeong, Byeong-Seon. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.Name: Isopropylisothiocyanate The following contents are mentioned in the article:
Dysfunction or progressive degeneration of retinal pigment epithelium (RPE) contributes in the initial pathogenesis of age-related macular degeneration (AMD) causing irreversible vision loss, which makes RPE the prime target of the disease. The present study aimed to identify compounds to protect 4-hydroxynonenal (4-HNE)-induced RPE cell death by inhibiting NADPH oxidase 4 (NOX4) activity, not just as free radical scavengers, using ARPE-19, a human adult retinal pigment epithelial cell line, as a RPE representative. Novel thirty-two 6-ureido/thioureido-2,4,5-trimethylpyridin-3-ol derivatives were synthesized and tested. The authors found that there was a strong correlation between level of protective effect of novel compounds against 4-HNE-induced APRE-19 cell death and that of inhibitory activity against 4-HNE-induced superoxide production, and that most of the novel compounds showed minimal DPPH radical scavenging activity. Compound 17-28 (1-butyl-3-(5-hydroxy-3,4,6-trimethylpyridin-2-yl)thiourea) showed the best protective activity against 4-HNE-induced superoxide production (79.5% inhibition) and cell death (85.1% recovery) at 10 μM concentration, which was better than that of VAS2870, a NOX2/4 inhibitor. In addition, compound 17-28 blocked 4-HNE-induced apoptosis of ARPE-19 cells in a concentration-dependent manner. The results indicate that compound 17-28 may be a lead compound to develop AMD therapeutics. This study involved multiple reactions and reactants, such as Isopropylisothiocyanate (cas: 2253-73-8Name: Isopropylisothiocyanate).
Isopropylisothiocyanate (cas: 2253-73-8) belongs to esters. Esters are also usually derived from carboxylic acids. It may also be obtained by reaction of acid anhydride or acid halides with alcohols or by the reaction of salts of carboxylic acids with alkyl halides. 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.Name: Isopropylisothiocyanate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics