Serdons, Kim et al. published their research in Journal of Medicinal Chemistry in 2009 | CAS: 2942-06-5

6-Nitrobenzothiazole (cas: 2942-06-5) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Synthetic Route of C7H4N2O2S

Synthesis and Evaluation of Three 18F-Labeled Aminophenylbenzothiazoles as Amyloid Imaging Agents was written by Serdons, Kim;Van Laere, Koen;Janssen, Peter;Kung, Hank F.;Bormans, Guy;Verbruggen, Alfons. And the article was included in Journal of Medicinal Chemistry in 2009.Synthetic Route of C7H4N2O2S This article mentions the following:

Three 18F-labeled fluorophenylbenzothiazoleamines I (R = H2N, MeNH, Me2N; R1 = 18F) are prepared which display high in vitro binding affinity for human amyloid β plaques (Ki ≤ 10 nM). I (R1 = 18F) are prepared by aromatic nucleophilic substitution of I [R = BocNH, BocN(Me), Me2N; R1 = O2N; Boc = tert-butoxycarbonyl] with 18F-fluoride, followed by deprotection of the Boc group if required; preparation by other methods, for example cyclocondensation of diaminobenzenethiols with benzoic acids, is unsuccessful. Determination of the octanol/water partition coefficient, biodistribution studies in mice, and in vivo μPET studies in rats and a rhesus monkey show that initial brain uptake is high and brain washout is fast in normal animals. Radiometabolites are quantified in plasma and brain of mice and in monkey plasma using HPLC. Of the tested compounds, I (R = H2N; R1 = 18F) shows the most favorable brain kinetics in mice, rats, and a monkey; its polar plasma radiometabolites do not cross the blood-brain barrier. Preliminary results strongly suggest that I (R = H2N; R1 = 18F) is a promising candidate as a PET brain amyloid imaging agent. In the experiment, the researchers used many compounds, for example, 6-Nitrobenzothiazole (cas: 2942-06-5Synthetic Route of C7H4N2O2S).

6-Nitrobenzothiazole (cas: 2942-06-5) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Synthetic Route of C7H4N2O2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica