Category: 95-24-9

In 2021,RSC Medicinal Chemistry included an article by Gao, Kai; Shaabani, Shabnam; Xu, Ruixue; Zarganes-Tzitzikas, Tryfon; Gao, Li; Ahmadianmoghaddam, Maryam; Groves, Matthew R.; Doemling, Alexander. Category: thiazole. The article was titled 《Nanoscale, automated, high throughput synthesis and screening for the accelerated discovery of protein modifiers》. The information in the text is summarized as follows:

Hit finding in early drug discovery is often based on high throughput screening (HTS) of existing and historical compound libraries, which can limit chem. diversity, is time-consuming, very costly, and environmentally not sustainable. On-the-fly compound synthesis and in situ screening in a highly miniaturized and automated format has the potential to greatly reduce the medicinal chem. environmental footprint. Here, acoustic dispensing technol. has been used to synthesize a library in a 1536 well format based on the Groebke-Blackburn-Bienayme’ reaction (GBB-3CR) on a nanomole scale. The unpurified library was screened by differential scanning fluorimetry (DSF) and cross-validated using microscale thermophoresis (MST) against the oncogenic protein-protein interaction menin-MLL. Several GBB reaction products were found as μM menin binder, and the structural basis of the interactions with menin was elucidated by co-crystal structure anal. Miniaturization and automation of the organic synthesis and screening process can lead to an acceleration in the early drug discovery process, which is an alternative to classical HTS and a step towards the paradigm of continuous manufacturing6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Category: thiazole) 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.Category: thiazoleThe 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

Application In Synthesis of 6-Chlorobenzothiazol-2-ylamineOn October 26, 2021 ,《An efficient one-pot synthesis of 2-aminobenzothiazoles from substituted anilines using benzyltrimethylammonium dichloroiodate and ammonium thiocyanate in DMSO:H2O》 was published in Tetrahedron Letters. The article was written by Dass, Reuben; Peterson, Matt A.. The article contains the following contents:

Treatment of anilines with benzyltrimethylammonium dichloroiodate and ammonium thiocyanate in DMSO:H2O at 70°C gave the 2-aminobenzothiazoles I [R = 6-F, 6-Me, 4-F, etc.] in excellent isolated yields (75-97% and ave. yield for all substrates is 90%). The reaction worked well for 2(4)mono-2,4-di- or 3,4,5-tri-substituted anilines and a wide range of both electron donating groups (MeO, HO, CF3O, Me) and electron withdrawing groups (NO2, CN, CO2Et, CO2H, Cl, F) were well tolerated. This method provided a useful alternative to other methods that are either less efficient (requiring 3-7 fold equivalent of reagents) or utilize highly toxic and corrosive liquid Br2 as the oxidizing agent. The experimental part of the paper was very detailed, including the reaction process of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Application In Synthesis 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.Application In Synthesis of 6-Chlorobenzothiazol-2-ylamineThiazoles 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

Lan, Xiaohao; Zhang, Yueli; Jia, Xiaoying; Dong, Siqi; Liu, Yang; Zhang, Mengmeng; Guo, Jiao; Cao, Junyuan; Guo, Yu; Xiao, Gengfu; Wang, Wei published an article on January 31 ,2022. The article was titled 《Screening and identification of Lassa virus endonuclease-targeting inhibitors from a fragment-based drug discovery library》, and you may find the article in Antiviral Research.Synthetic Route of C7H5ClN2S The information in the text is summarized as follows:

Lassa virus (LASV) belongs to the Old World genus Mammarenavirus, family Arenaviridae, and order Bunyavirales. Arenavirus contains a segmented neg.-sense RNA genome, which is in line with the bunyavirus and orthomyxoviruses. The segmented neg.-sense RNA viruses utilize a cap-snatching strategy to provide primers cleavaged from the host capped mRNA for viral mRNA transcription. As a similar strategy and the conformational conservation shared with these viruses, the endonuclease (EN) would serve as an attractive target for developing broad-spectrum inhibitors. Using the LASV minigenome (MG) system, we screened a fragment-based drug discovery library and found that two hits, F1204 and F1781, inhibited LASV MG activity. Both hits also inhibited the prototype arenavirus Lymphocytic choriomeningitis virus (LCMV) MG activity. Furthermore, both hits effectively inhibited authentic LCMV and severe fever with thrombocytopenia syndrome virus (SFTSV) infections. Similarly, both hits could inhibit the activity of LASV, LCMV, and SFTSV EN. The combination of either compound with an arenavirus entry inhibitor had significant synergistic antiviral effects. Moreover, both hits were found to be capable of binding to LASV EN with a binding affinity at the micromolar level. These findings provide a basis for developing the hits as potential candidates for the treatment of segmented neg.-sense RNA virus infections. After reading the article, we found that the author used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Synthetic Route of 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.Synthetic Route of C7H5ClN2SThe 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

《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