Tag: 100-200

《Chiral phosphoric acid-catalyzed enantioselective construction of structurally diverse benzothiazolopyrimidines》 was published in Chemical Science in 2019. These research results belong to Jarrige, Lucie; Glavac, Danijel; Levitre, Guillaume; Retailleau, Pascal; Bernadat, Guillaume; Neuville, Luc; Masson, Geraldine. Recommanded Product: 95-24-9 The article mentions the following:

A highly efficient catalytic enantioselective [4+2] cycloaddition was developed between 2-benzothiazolimines and enecarbamates. A wide range of benzothiazolopyrimidines bearing three contiguous stereogenic centers was obtained in high to excellent yields and with excellent diastereo- and enantioselectivities (d.r. > 98 : 2 and up to >99% ee). Furthermore, this chiral phosphoric acid-catalyzed strategy was scalable and enabled access to a new class of optically pure Lewis base isothiourea derivatives The results came from multiple reactions, including the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Recommanded Product: 95-24-9)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Recommanded Product: 95-24-9Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.

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

Zhang, Zeshuai; Wang, Zhiqiang; Li, Zheng published an article in Organic Letters. The title of the article was 《Three-Component One-Pot Construction of 2-Aryl-4H-benzo[4,5]thiazolo[3,2-a]pyrimidines Using Solid Calcium Carbide as a Surrogate of Gaseous Acetylene》.HPLC of Formula: 95-24-9 The author mentioned the following in the article:

A concise method for the construction of 2-aryl-4H-benzo[4,5]thiazolo[3,2-a]pyrimidines I (R = H, Cl, OMe; R1 = Ph, naphthalen-2-yl, thiophen-2-yl, 2H-1,3-benzodioxol-5-yl, etc.) using solid calcium carbide instead of gaseous acetylene as an alkyne source and 2-aminobenzothiazoles II and aromatic aldehydes R1CHO as substrates through one-pot three-component cascade reactions is described. The salient features for this protocol are the use of an inexpensive and easy-to-handle alkyne source, noble-metal-free condition, wide substrate scope and functional tolerance, satisfactory yield, and simple workup procedure. After reading the article, we found that the author used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9HPLC of Formula: 95-24-9)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.HPLC of Formula: 95-24-9Their 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

In 2019,ChemistrySelect included an article by Jafari, Behzad; Jalil, Saquib; Zaib, Sumera; Safarov, Sayfidin; Khalikova, Muattar; Ospanov, Meirambek; Yelibayeva, Nazym; Abilov, Zharylkasyn A.; Turmukhanova, Mirgul Z.; Kalugin, Sergey N.; Ehlers, Peter; Iqbal, Jamshed; Langer, Peter. Name: 6-Chlorobenzothiazol-2-ylamine. The article was titled 《Synthesis and Inhibitory Activity towards Monoamine Oxidase A and B of 8-Functionalized 3-Fluoro-2-methyl-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-ones》. The information in the text is summarized as follows:

An 8-chloro-3-fluoro-2-methyl-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-one was synthesized and employed in various palladium catalyzed cross-coupling-reactions, including Suzuki-Miyaura, Sonogashira and Buchwald-Hartwig reactions, delivering 8-aryl- I (R = C6H5, 4-FC6H4, 3-CH3C6H4, etc.), 8-alkynyl- I (R = CCC6H5, 4-CH3C6H4CC, 4-(CH3)3CC6H4CC) and 8-amino-3-fluoro-2-methyl-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-ones I (R = morpholin-4-yl, (4-fluorophenyl)aminyl, phenylaminyl, etc.) in good to excellent yields. The synthesized derivatives I were analyzed for their monoamine oxidase (MAO-A and MAO-B) inhibitory potential. Most of the compounds I exhibited moderate to good inhibitory activity towards MAO-A and/or MAO-B. Docking anal. was performed to verify the exptl. results. Hence, 8-substituted-3-fluoro-2-methyl-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-ones I might be potential lead compounds towards novel monoamine oxidase inhibitors. In the experimental materials used by the author, we found 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Name: 6-Chlorobenzothiazol-2-ylamine)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Name: 6-Chlorobenzothiazol-2-ylamineThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

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

Wang, Lu; Wang, Huaiyu; Meng, Weidong; Xu, Xiu-Hua; Huang, Yangen published an article on January 31 ,2021. The article was titled 《Facile syntheses of 3-trifluoromethylthio substituted thioflavones and benzothiophenes via the radical cyclization》, and you may find the article in Chinese Chemical Letters.Recommanded Product: 6-Chlorobenzothiazol-2-ylamine The information in the text is summarized as follows:

The 3-CF3S substituted thioflavones I (R1 = C6H5, 4-ClC6H4, 2-thienyl, etc.; R2 = Br) and benzothiophenes II (R3 = C6H5, 4-FC6H4, 2-thienyl, etc.; R4 = 6-Me, 6-Cl, 4,6-(Cl)2, etc.) were achieved via the reactions of AgSCF3 with methylthiolated alkynones 2-(SMe)-5-BrC6H3C(O)CCR1 and alkynylthioanisoles, R5CCR3 (R5 = 4-chloro-2-(methylsulfanyl)phenyl, 5-methyl-2-(methylsulfanyl)phenyl, 2,4-difluoro-6-(methylsulfanyl)phenyl, etc.) resp., promoted by persulfate. This protocol possesses good functional group tolerance and high yields. Mechanistic studies suggested that a classic two-step radical process involves addition of CF3S radical to triple bond and cyclization with SMe moiety. After reading the article, we found that the author used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Recommanded Product: 6-Chlorobenzothiazol-2-ylamine)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Recommanded Product: 6-Chlorobenzothiazol-2-ylamineTheir 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

The author of 《Design, synthesis and evaluation of benzothiazole urea derivatives as an anticonvulsant agent》 were Kachare, Snehal D.; Baheti, Kamalkishor G.; Yasar, Qazi; Jangam, Sampada S.. And the article was published in Pharma Chemica in 2021. Application of 95-24-9 The author mentioned the following in the article:

A series of 1-((-6-substituted-2-yl)-3-(4H-1,2,4 triazole-3-yl))ureas I (R = H, OMe, Cl, NO2, etc.) and (1-((3-(6-substituted-2-yl)ureido)methyl)cyclohexyl)acetic acids II were designed, synthesized using appropriate synthetic route and screened for CNS depressant and anticonvulsant activities. The synthesized compounds I and II were also analyzed for ADME properties. The results of In-Silico ADME Screening showed that compounds I and II could be exploited as an oral drug candidate. Mol. docking studies were performed for all the synthesized compounds I and II against γ-amino butyric acid amino transferase enzyme (1OHV), and all the compounds I and II exhibited docking score in the range of -7.5 to -8.4, among which compound II (R = Cl) had shown the highest docking scores as compared to the standard drug phenytoin. Animal study for anticonvulsant indicated that compounds I (R = NO2, H) and II (R = Cl) were exhibited significant activity at a dose 200 mg/kg. All these compounds I and II were also evaluated for CNS depressant activity using actophotometer. The results of CNS depressant and anticonvulsant activities and docking study showed that synthesized compounds I and II had potential CNS depressant and anticonvulsant activities and can be further optimized and developed as a lead compound The experimental process involved the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Application of 95-24-9)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Application of 95-24-9The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

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

In 2022,Pharmaceuticals included an article by Moodley, Rashmika; Mashaba, Chakes; Rakodi, Goitsemodimo H.; Ncube, Nomagugu B.; Maphoru, Mabuatsela V.; Balogun, Mohammed O.; Jordan, Audrey; Warner, Digby F.; Khan, Rene; Tukulula, Matshawandile. Safety of 6-Chlorobenzothiazol-2-ylamine. The article was titled 《New Quinoline-Urea-BenzΞothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling》. The information in the text is summarized as follows:

A series of 25 new benzothiazole-urea-quinoline hybrid compounds, I (X = H, Me, F, NO2, etc.) and II (n = 0, 2, 3, 4, and 6) were synthesized successfully via a three-step synthetic sequence involving an amidation coupling reaction as a critical step. In vitro evaluation of these hybrid compounds for their antitubercular inhibitory activity against the Mycobacterium tuberculosis H37Rv pMSp12::GPF bioreporter strain was undertaken. Of the 25 tested compounds, 17 compounds exhibited promising anti-TB activities of less than 62.5μM (MIC90) and 13 compds showed promising activity with MIC90 values in the range of 1-10μM, while compound I(X = CF3), being the most active, exhibited sub-micromolar activity (0.968μM) in the CAS assay. In addition, minimal cytotoxicity against the HepG2 cell line (cell viability above 75%) in 11 of the 17 compounds, at their resp. MIC90 concentrations, was observed, with compound I(X = CF3), exhibiting 100% cell viability. The hybridization of the quinoline, urea, and benzothiazole scaffolds demonstrated a synergistic relationship because the activities of resultant hybrids were vastly improved compared to the individual entities. In silico ADME predictions showed that the majority of these compounds have drug-like properties and are less likely to potentially cause cardiotoxicity (QPlogHERG > -5).6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Safety of 6-Chlorobenzothiazol-2-ylamine) was used in this study.

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Safety of 6-Chlorobenzothiazol-2-ylamineThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

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

Walker, Erin Joanne; Heydet, Deborah; Veldre, Timothy; Ghildyal, Reena published their research in Scientific Reports on December 31 ,2019. The article was titled 《Transcriptomic changes during TGF-β-mediated differentiation of airway fibroblasts to myofibroblasts》.Formula: C7H5ClN2S The article contains the following contents:

In this study, we have used next generation sequencing to delineate changes in transcriptome induced by TGF-β treatment of WI-38 airway fibroblasts in both short term and after differentiation into myofibroblasts. The data obtained from RNAseq anal. was confirmed by quant. PCR and protein expression by western blotting. We found that genes coding for intermediates in TGF-β signalling pathways (SMADs) were differentially expressed after TGF-β treatment, SMAD2 being upregulated and SMAD3 being downregulated. Genes involved in cytoskeletal pathways (FN1, LAMA, ITGB1) were upregulated in myofibroblasts. Genes that were previously shown to be changed in asthmatic lungs (ADAMTS1, DSP, TIMPs, MMPs) were similarly differentially expressed in myofibroblasts, strongly suggesting that TGF-β mediated differentiation of fibroblasts to myofibroblasts may underlie important changes in the asthmatic airway. We also identified new intermediates of signalling pathways (PKB, PTEN) that are changed in myofibroblasts compared to fibroblasts. We have found a significant number of genes that are altered after TGF-β induced transdifferentiation of WI-38 fibroblasts into myofibroblasts, many of which were expected or predicted. We also identified novel genes and pathways that were affected after TGF-β treatment, suggesting addnl. pathways are activated during the transition between fibroblasts and myofibroblasts and may contribute to the asthma phenotype. In the part of experimental materials, we found many familiar compounds, such as 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Formula: C7H5ClN2S)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Formula: C7H5ClN2STheir 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

The author of 《Organocatalytic asymmetric synthesis of benzothiazolopyrimidines via a [4+2] cycloaddition of azlactones with 2-benzothiazolimines》 were Ke, Chaoqi; Liu, Zhenzhong; Ruan, Sai; Feng, Xiaoming; Liu, Xiaohua. And the article was published in Organic Chemistry Frontiers in 2021. Safety of 6-Chlorobenzothiazol-2-ylamine The author mentioned the following in the article:

An easily available L-proline-derived guanidine-amide were found to be efficient at catalyzing a [4+2] cycloaddition of azlactones with 2-benzothiazolimines by affording various benzothiazolopyrimidines bearing adjacent tertiary and quaternary stereogenic centers in excellent yields at 2 mol% loading. The diastereoisomers of the main adducts differed from those in a previous bifunctional organocatalytic system. In the experiment, the researchers used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Safety of 6-Chlorobenzothiazol-2-ylamine)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Safety of 6-Chlorobenzothiazol-2-ylamineTheir 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

In 2021,Heterocyclic Letters included an article by Prajapat, Prakash; Pappula, Venkata Narayana; Vaghani, Hasit; Agarwal, Shikha; Samota, Jayanti; Talesara, Ganpat L.. Name: 6-Chlorobenzothiazol-2-ylamine. The article was titled 《Synthesis of biologically potent alkoxyphthalimido plugged N-(2,4-dioxo-1,4-dihydroquinazolin)-3(2H)-yl)-4-oxo-4H-benzo[4,5]thiazolo[3,2-a]pyrimidine-3-carboxamide via Gould Jacobs reaction》. The information in the text is summarized as follows:

Convenient methods for the synthesis of new alkoxyphthalimidoquinazolinedione and their pyrimidobenzothiazole derivatives I [R1 = H, Cl, O2N; R2 = H, 2-(1,3-dioxoisoindolin-2-yl)oxyethyl] were reported. A series of benzothiazolopyrimidine-3-carboxamides I were prepared starting from substituted 2-aminobenzothiazoles via solvent free multi-component Gould-Jacobs reaction. Structures of newly synthesized compounds were established based on IR, 1H-NMR, mass, anal. studies and fluorescence tests. Some of synthesized mols. I were assayed for their antimalarial activity. IC50 values of antimalarial activity of compounds were also determined The results came from multiple reactions, including the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Name: 6-Chlorobenzothiazol-2-ylamine)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Name: 6-Chlorobenzothiazol-2-ylamineThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

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

Name: 5-Bromothiazol-2-amineIn 2020 ,《Novel small molecule retrograde transport blocker confers post-exposure protection against ricin intoxication》 appeared in Acta Pharmaceutica Sinica B. The author of the article were Zhao, Xu; Li, Haixia; Li, Jia; Liu, Kunlu; Wang, Bo; Wang, Yuxia; Li, Xingzhou; Zhong, Wu. The article conveys some information:

Ricin is a highly toxic type 2 ribosome-inactivating protein (RIP) which is extracted from the seeds of castor beans. Ricin is considered a potential bioterror agent and no effective antidote for ricin exists so far. In this study, by structural modification of a retrograde transport blocker Retro-2cycl, a series of novel compounds were obtained. The primary screen revealed that compound I has an improved antiricin activity compare to pos. control. In vitro pre-exposure evaluation in Madine-Darby Canine Kidney (MDCK) cells demonstrated that compound I is a powerful anti-ricin compound with an EC50 of 41.05 nmol/L against one LC (lethal concentration, 5.56 ng/mL) of ricin. Further studies surprisingly indicated that compound I confers post-exposure activity against ricin intoxication. An in vivo study showed that 1 h post-exposure administration of compound I can improve the survival rate as well as delay the death of ricin-intoxicated mice. A drug combination of compound I with monoclonal antibody mAb4C13 rescued mice from one LD (LD) ricin challenge and the survival rate of tested animals is 100%. These results represent, for the first time, indication that small mol. retrograde transport blocker confers both in vitro and in vivo post-exposure protection against ricin and therefore provides a promising candidate for the development of anti-ricin medicines. In the part of experimental materials, we found many familiar compounds, such as 5-Bromothiazol-2-amine(cas: 3034-22-8Name: 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Name: 5-Bromothiazol-2-amine

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