Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 27231-36-3, is researched, SMILESS is SC1=NC2=CC(C)=CC=C2N1, Molecular C8H8N2SJournal, Article, Toxicology Reports called Inhibitory and inductive effects of 4- or 5-methyl-2-mercaptobenzimidazole, thyrotoxic and hepatotoxic rubber antioxidants, on several forms of cytochrome P450 in primary cultured rat and human hepatocytes, Author is Miyajima, Atsuko; Kuroda, Yukie; Sakemi-Hoshikawa, Kazue; Usami, Makoto; Mitsunaga, Katsuyoshi; Irie, Tomohiko; Ohno, Yasuo; Sunouchi, Momoko, the main research direction is cytochrome P450 4MeMB 5MeMB hepatocyte Primary culture benzimidazole; 3-MC, 3-methylcholanthrene; 4(5)-MeMBI, 4(or 5)-methyl-2-mercaptobenzimidazole; 4-MeMBI, 4-methyl-2-mercaptobenzimidazole; 5-MeMBI, 5-methyl-2-mercaptobenzimidazole; AhR, aryl hydrocarbon receptor; Benzimidazole; CYP, cytochrome P450; Cytochrome P450; DMSO, dimethyl sulfoxide; Drug-metabolizing activity; EROD, 7-ethoxyresorufin O-deethylation; Hepatocyte; MBI, 2-mercaptobenzimidazole; PXR, pregnane X receptor; Primary culture; T6βH, testosterone 6β-hydroxylation.Product Details of 27231-36-3.
Effects of 4-methyl-2-mercaptobenzimidazole (4-MeMBI) and 5-methyl-2- mercaptobenzimidazole (5-MeMBI) on cytochrome P 450 (CYP) activity were examined in primary cultured rat hepatocytes. Hepatocytes from male Wistar rats were cultured in the presence of 4-MeMBI or 5-MeMBI (0-400μM), and the activity of CYPs 3A2/4 (48 and 96 h) and 1A1/2 (48 h) was determined by measuring the activity of testosterone 6β-hydroxylation and 7-ethoxyresorufin O-deethylation, resp. As a result, 4-MeMBI and 5-MeMBI (≥12.5μM) inhibited CYP3A2 activity. On the other hand, 4-MeMBI (≥25μM) and 5-MeMBI (≥100μM) induced CYP1A1/2 activity, being consistent with the previous in vivo results. In a comparative metabolism study using primary cultured human hepatocytes from two Caucasian donors, 4-MeMBI and 5-MeMBI induced the activity of CYPs 3A4 and 1A1/2 with individual variability. It was concluded from these results that 4-MeMBI, 5-MeMBI and MBI caused inhibition of CYP3A2 activity in primary cultured rat hepatocytes, suggesting their potential for metabolic drug-drug interactions. Primary cultured rat and human hepatocytes were considered to be useful for the evaluation of effects of the benzimidazole compounds on their inducibility and inhibitory activities of cytochrome P 450 forms.
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Reference:
Benzoxazole – Wikipedia,
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