Day: November 8, 2022

On January 18, 2012, Capule, Christina C.; Brown, Caitlin; Olsen, Joanna S.; Dewhurst, Stephen; Yang, Jerry published an article.Name: 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Oligovalent Amyloid-Binding Agents Reduce SEVI-Mediated Enhancement of HIV-1 Infection. And the article contained the following:

This paper evaluates the use of oligovalent amyloid-binding mols. as potential agents that can reduce the enhancement of human immunodeficiency virus-1 (HIV-1) infection in cells by semen-derived enhancer of virus infection (SEVI) fibrils. These naturally occurring amyloid fibrils found in semen have been implicated as mediators that can facilitate the attachment and internalization of HIV-1 virions to immune cells. Mols. that are capable of reducing the role of SEVI in HIV-1 infection may, therefore, represent a novel strategy to reduce the rate of sexual transmission of HIV-1 in humans. Here, we evaluated a set of synthetic, oligovalent derivatives of benzothiazole aniline (BTA, a known amyloid-binding mol.) for their capability to bind cooperatively to aggregated amyloid peptides and to neutralize the effects of SEVI in HIV-1 infection. We demonstrate that these BTA derivatives exhibit a general trend of increased binding to aggregated amyloids as a function of increasing valence number of the oligomer. Importantly, we find that oligomers of BTA show improved capability to reduce SEVI-mediated infection of HIV-1 in cells compared to a BTA monomer, with the pentamer exhibiting a 65-fold improvement in efficacy compared to a previously reported monomeric BTA derivative These results, thus, support the use of amyloid-targeting mols. as potential supplements for microbicides to curb the spread of HIV-1 through sexual contact. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Name: 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to benzothiazole aniline oligovalent derivative sevi hiv1 infection, Pharmacology: Structure-Activity and other aspects.Name: 2-(4-Aminophenyl)-6-methylbenzothiazole

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

Bolchi, Cristiano; Pallavicini, Marco; Bernini, Sergio K.; Chiodini, Giuseppe; Corsini, Alberto; Ferri, Nicola; Fumagalli, Laura; Straniero, Valentina; Valoti, Ermanno published an article in 2011, the title of the article was Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase.SDS of cas: 64987-16-2 And the article contains the following content:

Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing internal dipeptide AA with 4-amino-2-phenylbenzoic acid and cysteine (C) with 2-amino-4-thiazolyl-, 2-mercapto-4-thiazolyl-, 2-mercapto-4-imidazolyl- and 2-methylmercapto-4-thiazolyl-acetic or propionic acid. The compound in which C is replaced by 2-amino-4-thiazolylacetic acid inhibited FTase activity in the low nanomolar range and showed antiproliferative effect on rat aortic smooth muscle cells interfering with Ras farnesylation. On the basis of these results, 2-aminothiazole can be considered as an alternative to heterocycles, such as pyridine and imidazole, normally used in FTase inhibitors designed as non-thiol CAAX mimetics. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).SDS of cas: 64987-16-2

The Article related to preparation thiazole imidazole peptidomimetic inhibitor farnesyltransferase, Pharmacology: Structure-Activity and other aspects.SDS of cas: 64987-16-2

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

On January 31, 2004, Muri, E. M. F.; Mishra, H.; Stein, S. M.; Williamson, J. S. published an article.Recommanded Product: 64987-16-2 The title of the article was Molecular modeling, synthesis and biological evaluation of heterocyclic hydroxamic acids designed as Helicobacter pylori urease inhibitors. And the article contained the following:

A computer-generated homol. model of the antimicrobial target Helicobacter pylori urease was derived, using the x-ray crystal structure of Klebsiella aerogenes as a template, in order to design novel urease inhibitors. Based on these computational studies, several heterocyclic hydroxamic acid derivatives have been designed, synthesized, and examined for their ability to inhibit urease activity. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Recommanded Product: 64987-16-2

The Article related to helicobacter urease inhibitor heterocyclic hydroxamate derivative preparation, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 64987-16-2

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

On March 1, 2012, Baraldi, Pier Giovanni; Romagnoli, Romeo; Saponaro, Giulia; Aghazadeh Tabrizi, Mojgan; Baraldi, Stefania; Pedretti, Pamela; Fusi, Camilla; Nassini, Romina; Materazzi, Serena; Geppetti, Pierangelo; Preti, Delia published an article.Application of 31699-14-6 The title of the article was 7-Substituted-pyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as antagonists of the transient receptor potential ankyrin 1 (TRPA1) channel: A promising approach for treating pain and inflammation. And the article contained the following:

The transient receptor potential ankyrin 1 (TRPA1) channel is activated by a series of byproducts of oxidative/nitrative stress, produced under inflammatory conditions or in the case of tissue damage, thus generating inflammatory and neuropathic pain and neurogenic inflammatory responses. These findings have identified TRPA1 as an emerging opportunity for the design and synthesis of selective inhibitors as potential analgesic and antiinflammatory agents. Herein we present the synthesis and functional evaluation of a new series of 7-substituted-1,3-dimethyl-1,5-dihydro-pyrrolo[3,2-d]pyrimidine-2,4-dione derivatives designed as TRPA1 antagonists. A small library of compounds has been built by the introduction of differently substituted N7-phenylacetamide or N7-[4-(substituted-phenyl)-thiazol-2-yl]-acetamide chains. All the synthesized compounds were assayed to evaluate their ability to block acrolein-mediated activation of native human and rat TRPA1 channels employing a fluorometric calcium imaging assay. Our study led us to the identification of compound 3h which showed considerably improved potency (IC50 = 400 nM) against human TRPA1 with regard to some of the most representative antagonists previously reported and integrated in our screening program as reference compounds In addition, 3h proved to maintain its efficacy toward rTRPA1, which designates it as a possible candidate for future evaluation of in vivo efficacy in rodent animal model of inflammatory and neuropathic pain. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).Application of 31699-14-6

The Article related to pyrrolo pyrimidine dione derivative preparation trpa1 channel pain inflammation, Pharmacology: Structure-Activity and other aspects.Application of 31699-14-6

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

On October 14, 2021, Lee, Kun-Hung; Yen, Wan-Ching; Lin, Wen-Hsing; Wang, Pei-Chen; Lai, You-Liang; Su, Yu-Chieh; Chang, Chun-Yu; Wu, Cai-Syuan; Huang, Yu-Chen; Yang, Chen-Ming; Chou, Ling-Hui; Yeh, Teng-Kuang; Chen, Chiung-Tong; Shih, Chuan; Hsieh, Hsing-Pang published an article.Category: thiazole The title of the article was Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model. And the article contained the following:

Colony-stimulating factor-1 receptor (CSF1R) is implicated in tumor-associated macrophage (TAM) repolarization and has emerged as a promising target for cancer immunotherapy. Herein, we describe the discovery of orally active and selective CSF1R inhibitors by property-driven optimization of BPR1K871 (9), our clin. multitargeting kinase inhibitor. Mol. docking revealed an addnl. nonclassical hydrogen-bonding (NCHB) interaction between the unique 7-aminoquinazoline scaffold and the CSF1R hinge region, contributing to CSF1R potency enhancement. Structural studies of CSF1R and Aurora kinase B (AURB) demonstrated the differences in their back pockets, which inspired the use of a chain extension strategy to diminish the AURA/B activities. A lead compound BPR1R024 (12) exhibited potent CSF1R activity (IC50 = 0.53 nM) and specifically inhibited protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth. In vivo, oral administration of 12 mesylate delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Category: thiazole

The Article related to quinazoline derivative preparation oral csf1r inhibitor antitumor immunomodulator, Pharmacology: Structure-Activity and other aspects.Category: thiazole

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

On May 25, 2019, Jalal, Mahir A.; TAlmalki, Ziyad; Radhi, Wisam A. published an article.SDS of cas: 2010-06-2 The title of the article was Quantitative structure-activity relationship studies of amino acids conjugated 2-amnio-arylthiazole as antifungal. And the article contained the following:

Thiazole derivatives as fungi-inhibitors belonging to 16 amino acids conjugated 2- amnio-arylthiazole was subjected computationally to quant. structure-activity relationship (QSAR) anal. by optimization of chem. structures at min. energy using mol. mechanics (MM+) theory and the semi-empirical MO (AM1) method. Correlation of their exptl. inhibitory zones against three types of fungi, namely, Fusarium monoliforme, Aspergillus Flavus, and Aspergillus niger with obtained physiochem. parameters was carried out using multiple linear regression (MLR) anal. As a result, there excellent out of 12 models were correlated with numerous descriptors having correlation coefficient rang (0.967-0.843). discriminant models were selected depending on their correlation coefficients (R2), Fisher ratios (F), and standard errors (S). These QSAR results and the probable pharmacophore features identified in this study offer important structural insight into designing novel amino acids conjugated 2-amnio-arylthiazole. Other 15 thiazole derivatives was proposed and it found that they are in good inhibitory zones. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).SDS of cas: 2010-06-2

The Article related to amino acid arylthiazole antifungal quant structure activity relationship analysis, Pharmacology: Structure-Activity and other aspects.SDS of cas: 2010-06-2

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

Hawas, Samia S.; El-Gohary, Nadia S.; Gabr, Moustafa T.; Shaaban, Mona I.; El-Ashmawy, Mahmoud B. published an article in 2019, the title of the article was Synthesis, molecular docking, antimicrobial, antiquorum-sensing and antiproliferative activities of new series of pyrazolo[3,4-b]pyridine analogs.Name: 4-Phenylthiazol-2-amine And the article contains the following content:

New series of pyrazolo[3,4-b]pyridines were prepared and evaluated for antimicrobial activity toward six selected microorganisms. Compounds and exhibited good activity toward Bacillus cereus. On the other hand, and evinced interesting activity over Candida albicans, whereas and displayed promising activity over Aspergillus fumigatus. Antiquorum-sensing effectiveness of the new members over Chromobacterium violaceum was also assessed, where compounds and exhibited higher activity than that of the reference compound, indole. In vitro antiproliferative assessment toward HepG2, HCT-116 and MCF-7 cancer cells evidenced that has notable effectiveness on all examined cell lines, whereas were active but to a lower extent. In vivo antitumor activity of and against EAC cells was also esteemed, where and showed considerable activity comparable to that of doxorubicin. Cytotoxicity screening over WI38 and WISH normal cells evinced that and are less cytotoxic than doxorubicin. Compounds and were evaluated for DNA-binding affinity and topoisomerase IIβ inhibitory activity. Analogs and illustrated strong DNA-binding affinity, whereas and exhibited interesting topoisomerase IIβ inhibitory activity. Compounds and were docked into topoisomerase IIβ, where showed preferential binding to topoisomerase IIβ. Computational studies articulated that the new members are in compliance with Veber’s standards and Lipinski’s rule. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Name: 4-Phenylthiazol-2-amine

The Article related to pyrazolo pyridine analog preparation antimicrobial antiquorum cancer topoisomerase, Pharmacology: Structure-Activity and other aspects.Name: 4-Phenylthiazol-2-amine

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

On March 20, 2003, Deghati, Paymaneh Y. F.; Borghini, Alice; Van Den Nieuwendijk, Adrianus M. C. H.; Dissen-de Groote, Miriam; IJzerman, Adriaan P. published an article.Recommanded Product: 19989-66-3 The title of the article was Inhibition of nucleoside transport By new analogues of nitrobenzylthioinosine. And the article contained the following:

Nitrobenzylthioinosine (NBTI, 1) was systematically modified by attachment of substituents at positions C6 and N9, and also by substitution of N1 with C. These modifications were chosen to reduce the polarity of the new compounds Incorporation of the nitro functionality into a benzoxadiazole ring system was considered first. These new nucleosides showed high affinity (1.5-10 nM) towards the nucleoside transport protein as present on human erythrocyte ghosts. Next, modification of this benzoxadiazole ring system with C, S and O in different positions produced a number of less polar nucleosides with affinity in the higher nanomolar range. Modification of N9 was achieved with different alkyl and alc. substituents. An Bu substituent proved best, although all variations yielded substantial decreases in affinity. Replacement of N1 by a carbon atom in combination with a 2-Cl substituent also resulted in a relatively potent NBTI derivative (47 nM). The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Recommanded Product: 19989-66-3

The Article related to nitrobenzylthioinosine analog preparation structure activity nucleoside transport protein, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 19989-66-3

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

Payaz, Deniz Uzeroglu; Kucukbay, F. Zehra; Kucukbay, Hasan; Angeli, Andrea; Supuran, Claudiu T. published an article in 2019, the title of the article was Synthesis carbonic anhydrase enzyme inhibition and antioxidant activity of novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine moieties.Formula: C14H12N2S And the article contains the following content:

Thirteen novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine were synthesized by facile acylation reactions through benzotriazole or DCC mediated reactions and their structures were identified by 1H-NMR, 13C-NMR, and FT-IR spectroscopic techniques and elemental anal. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA V, and hCA XIII. Some of the synthesized compounds showed good in vitro carbonic anhydrase inhibitory properties, with inhibition constants in the micromolar level. The new amino acid benzothiazole conjugates found to be more effective against hCA V and hCA II inhibition. In vitro antioxidant activities of the novel compounds were determined by DPPH method. Most of the synthesized compounds showed moderate to low antioxidant activities compared to the control antioxidant compounds (BHA and α-tocopherol). The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Formula: C14H12N2S

The Article related to benzothiazole amino acid synthesis antioxidant carbonic anhydrase, benzothiazole, amino acids, carbonic anhydrase, antioxidant, benzotriazole methodology, Pharmacology: Structure-Activity and other aspects.Formula: C14H12N2S

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

On January 18, 2007, Murray, Anthony; Lau, Jesper; Vedsoe, Per; Jeppesen, Lone; Kristiansen, Marit published a patent.Related Products of 859522-19-3 The title of the patent was Preparation of dicycloalkylcarbamoyl ureas as glucokinase activators. And the patent contained the following:

Title compounds represented by the formula I [wherein R1 = (cycloalkyl)alkyl, cycloalkyl, heterocyclyl, etc.; R2 = cycloalkyl, cycloalkenyl, heterocyclyl, etc.; R3 = H, alkyl, alkenyl, etc.; R4 = H, (cyclo)alkyl, arylalkyl, etc.; and pharmaceutically acceptable salts thereof] were prepared as glucokinase activators. For example, reaction of dicyclohexyl carbamoyl chloride with methylurea in THF gave II. The glucose sensitivity of I are measured at a compound concentration of 10 μM and at glucose concentrations of 5 and 15 mM. I and their pharmaceutical compositions are useful as activators of glucokinase for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Related Products of 859522-19-3

The Article related to dicycloalkylcarbamoyl urea preparation glucokinase activator, Alicyclic Compounds: Cyclohexanes and other aspects.Related Products of 859522-19-3

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