Reference of 2-Bromo-6-fluorobenzothiazoleOn October 9, 2003 ,《Design and synthesis of pyrrolidine-5,5′-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability》 was published in Journal of Medicinal Chemistry. The article was written by Borthwick, Alan D.; Davies, Dave E.; Ertl, Peter F.; Exall, Anne M.; Haley, Terry M.; Hart, Graham J.; Jackson, Deborah L.; Parry, Nigel R.; Patikis, Angela; Trivedi, Naimisha; Weingarten, Gordon G.; Woolven, James M.. The article contains the following contents:
A series of chiral, (S)-proline-α-methylpyrrolidine-5,5-trans-lactam serine protease inhibitors has been developed as antivirals of human cytomegalovirus (HCMV). The SAR of the functionality on the proline nitrogen has shown that derivatives of para-substituted Ph ureas > para-substituted Ph sulfonamides > para-substituted Ph carboxamide for activity against HCMV δAla protease, producing para-substituted Ph ureas with single figure nM potency (Ki) against the viral enzyme. The SAR of the functionality on the lactam nitrogen has defined the steric and electronic requirements for high human plasma stability while retaining good activity against HCMV protease. The combination of high potency against HCMV δAla protease and high human plasma stability has produced compounds with significant in vitro antiviral activity against human cytomegalovirus with the 6-hydroxymethyl benzothiazole derivative 72 being equivalent in potency to ganciclovir. The parent benzothiazole 56 had good pharmacokinetics in dogs with 29% bioavailability and good brain and ocular penetration in guinea pigs. The experimental part of the paper was very detailed, including the reaction process of 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Reference of 2-Bromo-6-fluorobenzothiazole)
2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Reference of 2-Bromo-6-fluorobenzothiazoleTheir presence in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica