Author: tianli

Effect of various factors on the reaction of 2-aminobenzothiazoles with propylene oxide was written by Ambartsumova, R. F.;Kosmacheva, L. P.. And the article was included in Chemistry of Heterocyclic Compounds (New York, NY, United States)(Translation of Khimiya Geterotsiklicheskikh Soedinenii) in 2002.Name: N-Phenylbenzo[d]thiazol-2-amine This article mentions the following:

The authors have shown that when 2-substituted 2-aminobenzothiazoles react with propylene oxide in proton-donor solvents, products of hydroxyalkylation of both the heterocycle and o-aminothiophenol formed as a result of its cleavage are synthesized. The authors have traced the effect of the nature of the solvent, various additives, the reaction temperature, and the heating time on this process. In the experiment, the researchers used many compounds, for example, N-Phenylbenzo[d]thiazol-2-amine (cas: 1843-21-6Name: N-Phenylbenzo[d]thiazol-2-amine).

N-Phenylbenzo[d]thiazol-2-amine (cas: 1843-21-6) 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. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Name: N-Phenylbenzo[d]thiazol-2-amine

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

Virtual Screening Approach to Identifying a Novel and Tractable Series of Pseudomonas aeruginosa Elastase Inhibitors was written by Leiris, Simon;Davies, David T.;Sprynski, Nicolas;Castandet, Jerome;Beyria, Lilha;Bodnarchuk, Michael S.;Sutton, Jonathan M.;Mullins, Toby M. G.;Jones, Mark W.;Forrest, Andrew K.;Pallin, T. David;Karunakar, Paduri;Martha, Sathish Kumar;Parusharamulu, Battu;Ramula, Ramesh;Kotha, Venkatesh;Pottabathini, Narender;Pothukanuri, Srinivasu;Lemonnier, Marc;Everett, Martin. And the article was included in ACS Medicinal Chemistry Letters in 2021.Application of 55661-33-1 This article mentions the following:

Novel therapies are required to treat chronic bacterial infections in cystic fibrosis (CF) sufferers. The most common pathogen responsible for these infections is Pseudomonas aeruginosa, which persists within the lungs of CF sufferers despite intensive antibiotic treatment. P. aeruginosa elastase (also known as LasB or pseudolysin) is a key virulence determinant that contributes to the pathogenesis and persistence of P. aeruginosa infections in CF patients. The crucial role of LasB in pseudomonal virulence makes it a good target for the development of an adjuvant drug for CF treatment. Herein we discuss the discovery of a new series of LasB inhibitors by virtual screening and computer assisted drug design (CADD) and their optimization leading to compounds 29 and 39 (K_i = 0.16μM and 0.12μM, resp.). In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Application of 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Application of 55661-33-1

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

Modular click chemistry libraries for functional screens using a diazotizing reagent was written by Meng, Genyi;Guo, Taijie;Ma, Tiancheng;Zhang, Jiong;Shen, Yucheng;Sharpless, Karl Barry;Dong, Jiajia. And the article was included in Nature (London, United Kingdom) in 2019.Computed Properties of C4H6N2S This article mentions the following:

Alkyl and aryl azides were prepared from the corresponding primary alkyl and aryl amines by reaction with fluorosulfonyl azide generated in situ from a fluorosulfonylimidazolium triflate and sodium azide, expanding access to azides and both to the 1,2,3-triazoles derived from them and to functional screens employing them. The method allowed the preparation of a library of >1000 azides from the corresponding amines; the azide library underwent copper-catalyzed azide-alkyne cycloaddition reactions to yield a library of >1000 1,2,3-triazoles. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Computed Properties of C4H6N2S).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Computed Properties of C4H6N2S

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

Plumbophosphates as oxidizing agents in the preparation of benzimidazoles, benzothiazoles, and benzoxazoles was written by El-Meligy, Mahmoud S. A.;Mohamed, Saoud A.. And the article was included in Journal fuer Praktische Chemie (Leipzig) in 1974.COA of Formula: C13H10N2S This article mentions the following:

H2[Pb(H2PO4)2(HPO4)2] or its mixture with Pb-(H2PO4)2 were used as oxidizing agents in the cyclization of the Schiff bases I [Rn = e.g. H, 5-Cl, 5,4-Cl(O2N), or 3,5-(O2N)2; R1 = e.g. Me, Ph, NHPh, or C6H4NO2-4] or 2-H2NC6H4N:C-HPh or of R2C6H4NHCSR3 (R2 = H, 2- or 4-Br, 2-Me, 2-or 4-O2N, or 4-Cl; R3 = NH2, C1-6 alkylamino, NHPh, NHC6H4-Cl-2, NMe2, or Ph) to give benzoxazoles (II), 2-phenylbenzimid-azole (III), or benzothiazoles (IV), resp. In the experiment, the researchers used many compounds, for example, N-Phenylbenzo[d]thiazol-2-amine (cas: 1843-21-6COA of Formula: C13H10N2S).

N-Phenylbenzo[d]thiazol-2-amine (cas: 1843-21-6) 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.COA of Formula: C13H10N2S

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

Design, synthesis and biological evaluation of 2-amino-N-(2-aminophenyl)thiazole-5-carboxamide derivatives as novel Bcr-Abl and histone deacetylase dual inhibitors was written by Chen, Xin;Zhao, Shuang;Wu, Yichao;Chen, Yadong;Lu, Tao;Zhu, Yong. And the article was included in RSC Advances in 2016.Recommanded Product: 55661-33-1 This article mentions the following:

In recent studies, combinations of histone deacetylase (HDAC) inhibitors with kinase inhibitor showed additive and synergistic effects. Herein we present a novel design approach for cancer drug development by combination of breakpoint cluster Abl (Bcr-Abl) and HDAC inhibitory activity, two independent pharmacol. activities, in one mol. The designed compounds were synthesized and tested, showing inhibitory activity against Bcr-Abl and HDAC1. The representative dual Bcr-Abl/HDAC inhibitors, compounds 6a and 6m, showed potent antiproliferative activities against human leukemia cell line K562 and prostate cancer cell line DU145 in cellular assays. This work may lay the foundation for developing dual Bcr-Abl/HDAC inhibitors as potential anticancer therapeutics. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Recommanded Product: 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Recommanded Product: 55661-33-1

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

Proline-Based Allosteric Inhibitors of Zika and Dengue Virus NS2B/NS3 Proteases was written by Millies, Benedikt;von Hammerstein, Franziska;Gellert, Andrea;Hammerschmidt, Stefan;Barthels, Fabian;Goeppel, Ulrike;Immerheiser, Melissa;Elgner, Fabian;Jung, Nathalie;Basic, Michael;Kersten, Christian;Kiefer, Werner;Bodem, Jochen;Hildt, Eberhard;Windbergs, Maike;Hellmich, Ute A.;Schirmeister, Tanja. And the article was included in Journal of Medicinal Chemistry in 2019.Related Products of 6294-52-6 This article mentions the following:

The NS2B/NS3 serine proteases of the Zika and Dengue flaviviruses are attractive targets for the development of antiviral drugs. We report the synthesis and evaluation of a new, proline-based compound class that displays allosteric inhibition of both proteases. The structural features relevant for protease binding and inhibition were determined to establish them as new lead compounds for flaviviral inhibitors. Based on our structure-activity relationship studies, the mols. were further optimized, leading to inhibitors with submicromolar IC₅₀ values and improved lipophilic ligand efficiency. The allosteric binding site in the proteases was probed using mutagenesis and covalent modification of the obtained cysteine mutants with maleimides, followed by computational elucidation of the possible binding modes. In infected cells, antiviral activity against Dengue virus serotype 2 using prodrugs of the inhibitors was observed In summary, a novel inhibitor scaffold targeting an allosteric site shared between flaviviral NS2B/NS3 proteases is presented whose efficacy is demonstrated in vitro and in cellulo. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxybenzo[d]thiazol-2-amine (cas: 6294-52-6Related Products of 6294-52-6).

5,6-Dimethoxybenzo[d]thiazol-2-amine (cas: 6294-52-6) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Related Products of 6294-52-6

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

Structure-Guided Rescaffolding of Selective Antagonists of BCL-X_L was written by Koehler, Michael F. T.;Bergeron, Philippe;Choo, Edna F.;Lau, Kevin;Ndubaku, Chudi;Dudley, Danette;Gibbons, Paul;Sleebs, Brad E.;Rye, Carl S.;Nikolakopoulos, George;Bui, Chinh;Kulasegaram, Sanji;Kersten, Wilhelmus J. A.;Smith, Brian J.;Czabotar, Peter E.;Colman, Peter M.;Huang, David C. S.;Baell, Jonathan B.;Watson, Keith G.;Hasvold, Lisa;Tao, Zhi-Fu;Wang, Le;Souers, Andrew J.;Elmore, Steven W.;Flygare, John A.;Fairbrother, Wayne J.;Lessene, Guillaume. And the article was included in ACS Medicinal Chemistry Letters in 2014.Computed Properties of C5H4ClNO2S This article mentions the following:

Because of the promise of BCL-2 antagonists in combating chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL), interest in addnl. selective antagonists of antiapoptotic proteins has grown. Beginning with a series of selective, potent BCL-X_L antagonists containing an undesirable hydrazone functionality, in silico design and X-ray crystallog. were utilized to develop alternative scaffolds that retained the selectivity and potency of the starting compounds In the experiment, the researchers used many compounds, for example, Methyl2-chloro-4-thiazolecarboxylate (cas: 850429-61-7Computed Properties of C5H4ClNO2S).

Methyl2-chloro-4-thiazolecarboxylate (cas: 850429-61-7) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. 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.Computed Properties of C5H4ClNO2S

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

Unexpected formation of benzothiazoles in the synthesis of new heterocycles: benzo-1,2,4-dithiazines was written by Fajkusova, Dagmar;Pazdera, Pavel. And the article was included in Synthesis in 2008.Application In Synthesis of N-Phenylbenzo[d]thiazol-2-amine This article mentions the following:

The synthesis of benzo-1,2,4-dithiazines was investigated presuming a reversible sulfur-sulfur bond formation. 2-Aminothiophenol, when allowed to react with isothiocyanates, provided benzothiazoles. 2,2′-Diaminodiphenyl disulfide underwent cyclizations very readily without any reducing agent to give, according to the reaction conditions, benzothiazoles (I; R = Bz, Ph, Ac, COOMe, Me) or benzo-1,2,4-dithiazines such as II. The developed procedure offers a simple and convenient way to prepare the title compounds in very good to excellent yields. Until now, benzo-1,2,4-dithiazines as well as 2,2′-diaminodiphenyl disulfides bearing aminocarbonothioyl groups were unknown. In the experiment, the researchers used many compounds, for example, N-Phenylbenzo[d]thiazol-2-amine (cas: 1843-21-6Application In Synthesis of N-Phenylbenzo[d]thiazol-2-amine).

N-Phenylbenzo[d]thiazol-2-amine (cas: 1843-21-6) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Application In Synthesis of N-Phenylbenzo[d]thiazol-2-amine

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

Synthesis and biological evaluation of novel trichodermin derivatives as antifungal agents was written by Zheng, Min;Yao, Ting-Ting;Xu, Xiao-Jun;Cheng, Jing-Li;Zhao, Jin-Hao;Zhu, Guo-Nian. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Safety of 2-Methylthiazol-5-amine This article mentions the following:

To discover more potential antifungal agents, 17 novel trichodermin derivatives were designed and synthesized. The structures of all the synthesized compounds were confirmed by ¹H NMR, ESI-MS and HRMS. Their antifungal activities against Ustilaginoidea oryzae and Pyricularia oryzae were evaluated. Most of the target compounds showed potent inhibitory activity, in which I showed superior inhibitory effects than the parent compound and com. fungicide prochloraz. Addnl., compound II was found to be active against all tested fungal strains, with EC₅₀ values of 0.47 and 3.71 mg L^-1, resp. In the experiment, the researchers used many compounds, for example, 2-Methylthiazol-5-amine (cas: 89281-44-7Safety of 2-Methylthiazol-5-amine).

2-Methylthiazol-5-amine (cas: 89281-44-7) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. 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.Safety of 2-Methylthiazol-5-amine

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

Photoinduced Heterogeneous C-H Arylation by a Reusable Hybrid Copper Catalyst was written by Choi, Isaac;Mueller, Valentin;Lole, Gaurav;Koehler, Robert;Karius, Volker;Vioel, Wolfgang;Jooss, Christian;Ackermann, Lutz. And the article was included in Chemistry – A European Journal in 2020.Recommanded Product: 5-Phenylthiazole This article mentions the following:

Heterogeneous copper catalysis enabled photoinduced C-H arylations of heteroarenes with aryl halides under exceedingly mild conditions at room temperature to afford aryl heteroarenes such as I [R = H, 6-OMe, 5-Cl, etc.; Ar = Ph, 4-MeC₆H₄, 2-MeOC₆H₄, etc.; X = O, S, NMe]. The hybrid copper catalyst could be reused without significant loss of catalytic efficacy. Detailed studies in terms of TEM, HRTEM and XPS anal. of the hybrid copper catalyst, among others, supported its outstanding stability and reusability. In the experiment, the researchers used many compounds, for example, 5-Phenylthiazole (cas: 1826-13-7Recommanded Product: 5-Phenylthiazole).

5-Phenylthiazole (cas: 1826-13-7) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Recommanded Product: 5-Phenylthiazole

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