Category: 152937-04-7

The author of 《1-Phenyl-N-(benzothiazol-2-yl)methanimine derivatives as Middle East respiratory syndrome coronavirus inhibitors》 were Hu, Min-Qi; Li, Heng; Lin, Ying; Zhang, Ying; Tang, Jie; Zuo, Jian-Ping; Yu, Li-Fang; Tong, Xian-Kun; Tang, Wei; Yang, Fan. And the article was published in RSC Advances in 2020. Synthetic Route of C7H3BrFNS The author mentioned the following in the article:

Middle East respiratory syndrome coronavirus (MERS-CoV) poses a serious threat to human health, and currently there are no effective or specific therapies available to treat it. Herein a series of 1-phenyl-N-(benzothiazol-2-yl)methanimine derivatives with inhibitory activity against MERS-CoV are described. The compound 4f with a 50% inhibition concentration value of 0.09 μM is a promising inhibitor that warrants further evaluation, towards the development of potential anti-MERS-CoV drugs. After reading the article, we found that the author used 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Synthetic Route of C7H3BrFNS)

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.Synthetic Route of C7H3BrFNSTheir 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

Recommanded Product: 2-Bromo-6-fluorobenzothiazoleOn March 9, 2011, Bonin, Helene; Leuma-Yona, Rodrigue; Marchiori, Bruno; Demonchaux, Patrice; Gras, Emmanuel published an article in Tetrahedron Letters. The article was 《Highly practical boronic acid surrogates for the Suzuki-Miyaura cross-coupling》. The article mentions the following:

Boronic acids and esters are well known substrates for the Suzuki-Miyaura cross-coupling, yet their isolation can sometimes be tedious. We report here that the use of aryl dioxazaborocanes afford a simple isolation procedure while keeping a high efficiency in the cross-coupling process. In the experiment, the researchers used 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Recommanded Product: 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.Recommanded Product: 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

Recommanded Product: 2-Bromo-6-fluorobenzothiazoleOn March 9, 2011, Bonin, Helene; Leuma-Yona, Rodrigue; Marchiori, Bruno; Demonchaux, Patrice; Gras, Emmanuel published an article in Tetrahedron Letters. The article was 《Highly practical boronic acid surrogates for the Suzuki-Miyaura cross-coupling》. The article mentions the following:

Boronic acids and esters are well known substrates for the Suzuki-Miyaura cross-coupling, yet their isolation can sometimes be tedious. We report here that the use of aryl dioxazaborocanes afford a simple isolation procedure while keeping a high efficiency in the cross-coupling process. In the experiment, the researchers used 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Recommanded Product: 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.Recommanded Product: 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

Luci, Diane K.; Jameson, J. Brian II; Yasgar, Adam; Diaz, Giovanni; Joshi, Netra; Kantz, Auric; Markham, Kate; Perry, Steve; Kuhn, Norine; Yeung, Jennifer; Kerns, Edward H.; Schultz, Lena; Holinstat, Michael; Nadler, Jerry L.; Taylor-Fishwick, David A.; Jadhav, Ajit; Simeonov, Anton; Holman, Theodore R.; Maloney, David J. published an article on January 23 ,2014. The article was titled 《Synthesis and Structure-Activity Relationship Studies of 4-((2-Hydroxy-3-methoxybenzyl)amino)benzenesulfonamide Derivatives as Potent and Selective Inhibitors of 12-Lipoxygenase》, and you may find the article in Journal of Medicinal Chemistry.Synthetic Route of C7H3BrFNS The information in the text is summarized as follows:

Human lipoxygenases (LOXs) are a family of iron-containing enzymes which catalyze the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling mols. are involved in a number of physiol. responses such as platelet aggregation, inflammation, and cell proliferation. Our group has taken a particular interest in platelet-type 12-(S)-LOX (12-LOX) because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Herein, we report the identification and medicinal chem. optimization of a 4-((2-hydroxy-3-methoxybenzyl)-amino)-benzenesulfonamide-based scaffold. Top compounds, exemplified by I [R = 2-benzothiazole, 2-benzoxazole], display nM potency against 12-LOX, excellent selectivity over related lipoxygenases and cyclooxygenases, and possess favorable ADME properties. In addition, compounds I [R = 2-benzothiazole, 2-benzoxazole] inhibit PAR-4 induced aggregation and calcium mobilization in human platelets and reduce 12-HETE in β-cells.2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Synthetic Route of C7H3BrFNS) was used in this study.

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.Synthetic Route of C7H3BrFNSTheir 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

Setoguchi, Masaki; Iimura, Shin; Sugimoto, Yuuichi; Yoneda, Yoshiyuki; Chiba, Jun; Watanabe, Toshiyuki; Muro, Fumihito; Iigo, Yutaka; Takayama, Gensuke; Yokoyama, Mika; Taira, Tomoe; Aonuma, Misato; Takashi, Tohru; Nakayama, Atsushi; Machinaga, Nobuo published an article on February 1 ,2012. The article was titled 《Identification of trans-4-[1-[[7-fluoro-2-(1-methyl-3-indolyl)-6-benzoxazolyl]acetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid as a potent, orally active VLA-4 antagonist》, and you may find the article in Bioorganic & Medicinal Chemistry.Computed Properties of C7H3BrFNS The information in the text is summarized as follows:

For the purpose of obtaining orally potent VLA-4 inhibitors, we have carried out structural modification of the (N’-phenylureido)phenyl group in compound 1, where the group was found to be attributed to poor pharmacokinetic profile in our previous research. Through modification, we have identified several compounds with both potent in vitro activity and improved oral exposure. In particular, compound 7e with 7-fluoro-2-(1-methyl-1H-indol-3-yl)-1,3-benzoxazolyl group as a novel replacement of the (N’-phenylureido)phenyl group significantly inhibited eosinophil infiltration into bronchoalveolar lavage fluid at 15 mg/kg in an Ascaris-antigen-induced murine bronchial inflammatory model, and its efficacy was comparable to that of the anti-mouse α4 antibody (R1-2). In addition to this study using 2-Bromo-6-fluorobenzothiazole, there are many other studies that have used 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Computed Properties of C7H3BrFNS) was used in this study.

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.Computed Properties of C7H3BrFNSTheir 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

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

Related Products of 152937-04-7On September 15, 2012 ,《Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Malmstroem, Jonas; Viklund, Jenny; Slivo, Can; Costa, Ana; Maudet, Mickael; Sandelin, Catrin; Hiller, Goesta; Olsson, Lise-Lotte; Aagaard, Anna; Geschwindner, Stefan; Xue, Yafeng; Vasaenge, Mervi. The article contains the following contents:

4-(1,3-Benzothiazol-2-yl)thiophene-2-sulfonamide (I) was found to be a moderately potent inhibitor of cyclin-dependent kinase 5 (cdk5) from a HTS screen. The synthesis and SAR around this hit is described. The X-ray coordinates of ligand I with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water mol. The results came from multiple reactions, including the reaction of 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Related Products of 152937-04-7)

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.Related Products of 152937-04-7Their 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

Related Products of 152937-04-7On September 15, 2012 ,《Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Malmstroem, Jonas; Viklund, Jenny; Slivo, Can; Costa, Ana; Maudet, Mickael; Sandelin, Catrin; Hiller, Goesta; Olsson, Lise-Lotte; Aagaard, Anna; Geschwindner, Stefan; Xue, Yafeng; Vasaenge, Mervi. The article contains the following contents:

4-(1,3-Benzothiazol-2-yl)thiophene-2-sulfonamide (I) was found to be a moderately potent inhibitor of cyclin-dependent kinase 5 (cdk5) from a HTS screen. The synthesis and SAR around this hit is described. The X-ray coordinates of ligand I with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water mol. The results came from multiple reactions, including the reaction of 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Related Products of 152937-04-7)

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.Related Products of 152937-04-7Their 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