Month: February 2023

2-Trifluoromethylthiazole-5-carboxamides: Analogues of a Stilbene-Based Anti-HIV Agent that Impact HIV mRNA Processing was written by Zamiri, Maryam;Cheung, Peter K.;Brockman, Mark A.;Brumme, Zabrina L.;Chabot, Benoit;Cochrane, Alan;Grierson, David S.. And the article was included in ACS Medicinal Chemistry Letters in 2021.Related Products of 15864-32-1 This article mentions the following:

The observation that stilbene 3 (5350150) blocks HIV replication through its impact on HIV mRNA processing prompted a program to develop non-cytotoxic analogs that maintain its mechanism of action. This initially involved replacement of the central double bond in 3 by an amide function and the quinoline motif by a 2-aminobenzothiazole subunit, as in 12jj (R’ = Cl), 12pp (R = NO₂), and 12vv (R = CF₃). On the basis of the possible CF₃ 鈫?NO₂ bioisostere relationship in 12vv and 12pp, compound 23 was prepared and also found to be active. In the final step, the thiazole compounds 28 (GPS488) (EC₅₀ = 1.66渭M) and 29 (GPS491) (EC₅₀ = 0.47渭M) were prepared and evaluated. Similar activity and cell viability values (therapeutic index (TI = CC₅₀/EC₅₀) values of 50-100) were observed in primary peripheral blood mononuclear cells. Furthermore, they remained active against a panel of HIV mutant strains displaying resistance to individual drugs used in antiretroviral therapy. It was determined that compound 29 suppressed expression of the HIV-1 structural protein Gag and altered HIV-1 RNA accumulation, decreasing the abundance of RNAs encoding the structural proteins while increasing levels of viral RNAs encoding the regulatory proteins, a pattern similar to that seen for compound 3. In the experiment, the researchers used many compounds, for example, 2-Amino-6-bromobenzothiazole (cas: 15864-32-1Related Products of 15864-32-1).

2-Amino-6-bromobenzothiazole (cas: 15864-32-1) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-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.Related Products of 15864-32-1

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

Impact of Anti-GPIIb/IIIa Antibody-Producing B Cells as a Predictor of the Response to Lusutrombopag in Thrombocytopenic Patients with Liver Disease. was written by Wada, Naohisa;Uojima, Haruki;Satoh, Takashi;Okina, Sosei;Iwasaki, Shuichiro;Shao, Xue;Takiguchi, Hayato;Arase, Yoshitaka;Itokawa, Norio;Atsukawa, Masanori;Miyazaki, Koji;Hidaka, Hisashi;Kako, Makoto;Kagawa, Tatehiro;Iwakiri, Katsuhiko;Horie, Ryouichi;Suzuki, Takahiro;Koizumi, Wasaburo. And the article was included in Digestive diseases (Basel, Switzerland) in 2021.Reference of 1110766-97-6 This article mentions the following:

BACKGROUND: To make an accurate estimate of the response to thrombopoietin (TPO) receptor agonists for thrombocytopenia associated with chronic liver disease, we evaluated the influence of antiplatelet autoantibodies on the response to lusutrombopag in thrombocytopenic patients with liver disease. METHODS: A prospective study was conducted at 2 hospitals. Thrombocytopenic patients with liver disease received oral lusutrombopag 3.0 mg once daily for up to 7 days. We analyzed changes in platelet counts from baseline to the maximum platelet count on days 9-14. The definition of clinical response was a platelet count of 鈮? 脳 104/渭L with an increased platelet count of 鈮? 脳 104/渭L from baseline. We assessed the correlation between the response to treatment drug and antiplatelet autoantibodies measured by anti-GPIIb/IIIa antibody-producing B cells. RESULTS: Thirty patients received the trial drug. There were 25 responders and 5 nonresponders. The median change in platelet counts was 3.9 脳 104/渭L (95% CI 2.8-4.6, p < 0.0001). The correlation between change in platelet counts and the frequency of the anti-glycoprotein IIb/IIIa antibody-producing B cells was moderate (r = 0.414, 95% CI 0.064-0.674, p = 0.023). In multivariate analysis of factors affecting the change in platelet counts, the anti-GPIIb/IIIa antibody-producing B cells were identified as an independent factor (regression coefficient [B] = 0.089; CI 0.021-0.157, p = 0.013). CONCLUSION: Anti-GPIIb/IIIa antibody-producing B cells may be a predictor for TPO receptor agonists in patients with chronic liver disease. In the experiment, the researchers used many compounds, for example, (S,E)-3-(2,6-Dichloro-4-((4-(3-(1-(hexyloxy)ethyl)-2-methoxyphenyl)thiazol-2-yl)carbamoyl)phenyl)-2-methylacrylic acid (cas: 1110766-97-6Reference of 1110766-97-6).

(S,E)-3-(2,6-Dichloro-4-((4-(3-(1-(hexyloxy)ethyl)-2-methoxyphenyl)thiazol-2-yl)carbamoyl)phenyl)-2-methylacrylic acid (cas: 1110766-97-6) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). 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.Reference of 1110766-97-6

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

Diastereoselective and Enantioselective Silylation of 2-Arylcyclohexanols was written by Wang, Li;Akhani, Ravish K.;Wiskur, Sheryl L.. And the article was included in Organic Letters in 2015.Synthetic Route of C15H12N2S This article mentions the following:

The silylation-based kinetic resolution of trans 2-arylcyclohexanols was accomplished by employing a triaryl silyl chloride as the derivatizing reagent with a com. available isothiourea catalyst. The methodol. is selective for the trans diastereomer over the cis, which provides an opportunity to selectively derivatize one stereoisomer out of a mixture of four. By employing this technol., a facile, convenient method to form a highly enantiomerically enriched silylated alc. was accomplished through a 1-pot reduction-silylation sequence that started with a 2-aryl-substituted ketone. In the experiment, the researchers used many compounds, for example, (S)-2-Phenyl-2,3-dihydrobenzo[d]imidazo[2,1-b]thiazole (cas: 950194-37-3Synthetic Route of C15H12N2S).

(S)-2-Phenyl-2,3-dihydrobenzo[d]imidazo[2,1-b]thiazole (cas: 950194-37-3) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Synthetic Route of C15H12N2S

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

Vulcanization of butadiene-nitrile rubber in the presence of ammonium thiocyanate was written by Blokh, G. A.;Zorina, V. B.;Duplyakin, V. D.. And the article was included in Khimicheskaya Tekhnologiya (Kiev) in 1983.Safety of 5-Amino-3H-1,2,4-dithiazole-3-thione This article mentions the following:

Regression equations were derived for optimizing the vulcanization of SKN-26 rubber in the presence of NH₄SCN (I)-Altax (II) [120-78-5]-ZnO system or I–xanthane聽hydride (III) [6846-35-1] system at 416 K with respect to 300% modulus, tensile strength, and breaking elongation. The optimum content of I, II, ZnO, and III were determined from solutions of the equations. In the experiment, the researchers used many compounds, for example, 5-Amino-3H-1,2,4-dithiazole-3-thione (cas: 6846-35-1Safety of 5-Amino-3H-1,2,4-dithiazole-3-thione).

5-Amino-3H-1,2,4-dithiazole-3-thione (cas: 6846-35-1) 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.Safety of 5-Amino-3H-1,2,4-dithiazole-3-thione

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

Nitrogen-Doped Graphene-Activated Iron-Oxide-Based Nanocatalysts for Selective Transfer Hydrogenation of Nitroarenes was written by Jagadeesh, Rajenahally V.;Natte, Kishore;Junge, Henrik;Beller, Matthias. And the article was included in ACS Catalysis in 2015.Category: thiazole This article mentions the following:

Nanoscaled iron oxides on carbon were modified with nitrogen-doped graphene (NGr) and found to be excellent catalysts for the chemoselective transfer hydrogenation of nitroarenes to anilines. Under standard reaction conditions, a variety of functionalized and structurally diverse anilines, which serve as key building blocks and central intermediates for fine and bulk chems., were synthesized in good to excellent yields. In the experiment, the researchers used many compounds, for example, 6-Nitrobenzothiazole (cas: 2942-06-5Category: thiazole).

6-Nitrobenzothiazole (cas: 2942-06-5) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 掳C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Category: thiazole

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

Skp2 is associated with paclitaxel resistance in prostate cancer cells was written by Yang, Yeguo;Lu, Yi;Wang, Lihui;Mizokami, Atsushi;Keller, Evan T.;Zhang, Jian;Fu, Jiejun. And the article was included in Oncology Reports in 2016.Formula: C24H24N2O3S This article mentions the following:

Prostate cancer is the most commonly diagnosed tumor in men in the United States. Patients with hormone refractory prostate cancer are often treated with paclitaxel, but most of them eventually develop drug resistance. S-phase kinase associated protein 2 (Skp2) is a component of the SCF (Skp1-Cullin1-F-box) type of E3 ubiquitin ligase complexes. In the present study, we investigated the role of Skp2 in paclitaxel-resistant DU145-TxR or PC-3-TxR cells by Skp2 silencing or using Skp2 inhibitors. We first confirmed that Skp2 expression is upregulated in DU145-TxR or PC-3-TxR cells compared with their parental cells DU145 or PC-3, resp. Knockdown of Skp2 or Skp2 inhibitor treatment in DU145-TxR or PC-3-TxR cells restored paclitaxel sensitivity. E-cadherin was decreased while Vimentin was increased in PC-3-TxR or DU145-TxR cells. In addition, p27 expression was inversely correlated with Skp2 expression in DU145-TxR or PC-3-TxR cells. Moreover, p27 was found to increase in both Skp2 silencing PC-3-TxR and DU145-TxR cells. These results suggest that Skp2 is associated with prostate cancer cell resistance to paclitaxel. Skp2 may be a potential therapeutic target for drug-resistant prostate cancer. In the experiment, the researchers used many compounds, for example, 3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one (cas: 222716-34-9Formula: C24H24N2O3S).

3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one (cas: 222716-34-9) 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 未 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Formula: C24H24N2O3S

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

One-Pot Domino Synthesis of Diarylalkynes/1,4-Diaryl-1,3-diynes by [9,9-Dimethyl-4,5-bis(diphenylphosphino)xanthene] (Xantphos)-Copper(I) Iodide-Palladium(II) Acetate-Catalyzed Double Sonogashira-Type Reaction was written by Qiu, Shaozhong;Zhang, Caiyang;Qiu, Rui;Yin, Guodong;Huang, Jinkun. And the article was included in Advanced Synthesis & Catalysis in 2018.Category: thiazole This article mentions the following:

The low loading combination of the complex [9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene] (Xantphos)copper(I) iodide and simple ligand-free palladium(II) acetate was found to be efficient for the domino synthesis of diarylalkynes by the reaction of aryl halides with trimethylsilylethynylene or bis(trimethylsilyl)acetylene in a single-step procedure. The unsym. diarylalkynes can be obtained through a one-pot two-step approach. The reactions of aryl bromides with 1,4-bis(trimethylsilyl)butadiyne also furnished the corresponding 1,4-diaryl-1,3-diynes in a similar fashion. This route to diarylalkynes and 1,4-diaryl-1,3-diynes is complementary to previously reported synthetic procedures. In the experiment, the researchers used many compounds, for example, 2-Bromothiazole (cas: 3034-53-5Category: thiazole).

2-Bromothiazole (cas: 3034-53-5) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. 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.Category: thiazole

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

Evaluation of the clinical safety and efficacy of fenbendazole and levamisole in the control of Neoechinorhynchus buttnerae in Colossoma macropomum – Acanthocephalosis treatments was written by de Alexandre Sebastiao, Fernanda;Souza Rocha, Maria Juliete;Rodrigues Brandao, Franmir;Braga de Oliveira, Maria Ines;de Melo Souza, Damy Caroline;Carlos do Nascimento Barbosa, Bruna;Castro Monteiro, Patricia;Majolo, Claudia;Crescencio, Roger;Tavares-Dias, Marcos;Campos Chagas, Edsandra. And the article was included in Aquaculture International in 2022.Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole This article mentions the following:

Abstract: Occurrences of parasitic infections caused by Neoechinorhynchus buttnerae in Colossoma macropomum (tambaqui), especially in the northern region of Brazil, have increased in the past two decades and have caused economic losses in tambaqui production The aim of this study was to evaluate the in vivo efficacy and clin. safety of fenbendazole and levamisole in controlling and treating N. buttnerae in tambaqui for 30 days. Juvenile tambaqui naturally infected with N. buttnerae were distributed in 15 tanks (n = 12 per 1,000 L-tank), constituting five treatments, in triplicate. Treatments were administered via diet (mg kg^-1 of live weight): control (0 mg kg^-1), F1 (100 mg kg^-1 of fenbendazole), F2 (200 mg kg^-1 of fenbendazole), L1 (200 mg kg^-1 of levamisole), and L2 (300 mg kg^-1 of levamisole). Fish survival rate was 100during the entire exptl. period. Fenbendazole treatments were not effective against N. buttnerae; however, L1 and L2 showed efficacy of 73.4 and 99.15, resp. Treatments with fenbendazole or levamisole did not affect the growth parameters of tambaqui. F1 and F2 showed significant reduction in the hematocrit values when compared to L1, and Hb values were significantly reduced in F1 when compared to L1, L2, and the control group. There were no significant differences in RBC, MCV, and CHCM. The plasma glucose value was statistically lower in F1 than in the L1 (p = 0.03) and L2 (p = 0.02) treatments. For alanine aminotransferase, there was a significant reduction (p = 0.004) in the F1 and F2 groups compared to the L2 group. No statistical difference was observed for aspartate aminotransferase among the treatments. More studies are warranted to further evaluate other therapeutic strategies using shorter periods for controlling and efficiently treating N. buttnerae. In the experiment, the researchers used many compounds, for example, (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole (cas: 14769-73-4Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole).

(S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole (cas: 14769-73-4) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. 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.Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole

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

2-Arylation/alkylation of benzothiazoles using superparamagnetic graphene oxide-Fe₃O₄ hybrid material as a heterogeneous catalyst with diisopropyl azodicarboxylate (DIAD) as an oxidant was written by Khalili, Dariush;Etemadi-Davan, Elham;Banazadeh, Ali Reza. And the article was included in Applied Organometallic Chemistry in 2018.Recommanded Product: 2-(4-Methylphenyl)benzothiazole This article mentions the following:

In this report, we introduced Graphene oxide-iron oxide (GO-Fe₃O₄) nanocomposites as a heterogeneous catalyst for arylation/alkylation of benzothiazoles with aldehydes and benzylic alcs. in the presence of diisopropyl azodicarboxylate (DIAD) as an oxidant which exclusively produced 2-aryl (alkyl)-1H-benzothizoles in moderate to excellent yields. The absence of precious metals and toxic solvent, easy product isolation, and recyclability of the GO-Fe₃O₄ with no loss of activity are notable advantages of this method. In the experiment, the researchers used many compounds, for example, 2-(4-Methylphenyl)benzothiazole (cas: 16112-21-3Recommanded Product: 2-(4-Methylphenyl)benzothiazole).

2-(4-Methylphenyl)benzothiazole (cas: 16112-21-3) 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 未 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.Recommanded Product: 2-(4-Methylphenyl)benzothiazole

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

N-doped graphitic carbon-improved Co-MoO₃ catalysts on ordered mesoporous SBA-15 for chemoselective reduction of nitroarenes was written by Huang, Haigen;Liang, Xiangcheng;Wang, Xueguang;Sheng, Yao;Chen, Chenju;Zou, Xiujing;Lu, Xionggang. And the article was included in Applied Catalysis, A: General in 2018.Computed Properties of C7H4N2O2S This article mentions the following:

Metallic Co-MoO₃ catalysts supported on ordered mesoporous SBA-15 were first prepared through in situ reaction of SBA-15-supported Co-Mo oxides with 1,10-phenanthroline. The resulting Co-MoO₃/NC@SBA-15 catalysts with N-doped carbon (NC) exhibited high catalytic activity and chemoselectivity for selective reduction of various functionalized nitroarenes to the corresponding arylamines in ethanol with hydrazine hydrate at near room temperature (30掳). For reduction of all tested substrates (28 examples), the catalyst could afford a conversion of >99% and arylamine selectivity of >99%. The excellent catalytic performance of the Co-MoO₃/NC@SBA-15 was attributed to the Co-N_蠂(C)-Mo active sites generated through the interaction between the surface Co-N_蠂(C) and MoO₃ species, promoting the dissociation of hydrazine mol. into the active H* species for the reduction of nitro groups. After the seventh cycle for reduction of 4-methoxylnitrobenzene, the 2%Co-MoO₃/NC@SBA-15 showed little change in catalytic performance, textural properties, size and dispersion of metal species and valence states of elements, indicating high stability and recyclability. In the experiment, the researchers used many compounds, for example, 6-Nitrobenzothiazole (cas: 2942-06-5Computed Properties of C7H4N2O2S).

6-Nitrobenzothiazole (cas: 2942-06-5) 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 未 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. 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.Computed Properties of C7H4N2O2S

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