Day: November 3, 2022

On January 31, 2013, Lacriola, Christopher J.; Falk, Shaun P.; Weisblum, Bernard published an article.Computed Properties of 92-36-4 The title of the article was Screen for agents that induce autolysis in Bacillus subtilis. And the article contained the following:

The growing prevalence of antibiotic-resistant infections underscores the need to discover new antibiotics and to use them with maximum effectiveness. In response to these needs, the authors describe a screening protocol for the discovery of autolysis-inducing agents that uses two Bacillus subtilis reporter strains, SH-536 and BAU-102. To screen chem. libraries, autolysis-inducing agents were first identified with a BAU-102-based screen and then subdivided with SH-536 into two major groups: those that induce autolysis by their direct action on the cell membrane and those that induce autolysis secondary to inhibition of cell wall synthesis. SH-536 distinguishes between the two groups of autolysis-inducing agents by synthesizing and then releasing β-galactosidase (β-Gal) in late stationary phase at a time that cells have nearly stopped growing and are therefore tolerant of cell wall synthesis inhibitors. Four hits, named compound 2, compound 3, compound 5, and compound 24, obtained previously as inducers of autolysis by screening a 10,080-compound discovery library with BAU-102, were probed with SH-536 and found to release β-Gal, indicating that their mode of action was to permeabilize the B. subtilis cell membrane. The four primary hits inhibited growth in Staphylococcus aureus, Enterococcus faecium, Bacillus subtilis, and Bacillus anthracis, with MICs in the 12.5- to 25-μg/mL (20 to 60 μM) range. The four primary hits were further used to probe B. subtilis, and their action was partially characterized with respect to the dependence of induced autolysis on specific autolysins. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Computed Properties of 92-36-4

The Article related to agent autolysis bacillus, Microbial, Algal, and Fungal Biochemistry: Antimicrobial Sensitivity and other aspects.Computed Properties of 92-36-4

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

On December 12, 2017, Liu, Denggui; Yang, Kunyu; Zhou, Wei; Chen, Hao; Zeng, Qingdong published a patent.Application In Synthesis of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate The title of the patent was Method for preparing anticancer drug intermediate. And the patent contained the following:

The title anticancer drug intermediate is a compound shown in formula IIIa or IIIb. The title method comprises the steps of: conducting halogenation on 2-acetyl-4-formate thiazole compound, and reacting with tri-Ph phosphine, tri-Me phosphite, or tri-Et phosphite. The inventive compound can be applied in preparing a compound shown in formula I via conducting Wittig or Wittig-Horner reaction with isobutyraldehyde. The preparing process has the advantages of low raw material costs, mild reaction conditions, little pollution, and easy industrialization. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Application In Synthesis of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

The Article related to thiazole containing phosponate preparation anticancer drug intermediate, Organometallic and Organometalloidal Compounds: Phosphorus Compounds and other aspects.Application In Synthesis of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

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

Koppireddi, Satish; Avula, Sreenivas; Tiwari, Ashok K.; Ali, Amtul Z.; Yadla, Rambabu published an article in 2014, the title of the article was α-glucosidase inhibitory activity of 4-aryl-N-(2,4-thiazolidinedione-5-acetyl)-1,3-thiazol-2-amines.Application of 31699-14-6 And the article contains the following content:

A series of N-(4-aryl-1,3-thiazol-2-yl)-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamides 3a-k and N-(1,3-benzothiazol-2-yl)-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamides 3l-n are synthesized and evaluated for their α-glucosidase inhibitory activity. N-[4-(m-Chlorophenyl)-1,3-thiazol-2yl]-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamide (3g) and N-[4-(o-fluorophenyl)-1,3-thiazol-2-yl]-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamide (3j) have shown very good inhibition. The remaining compounds have exhibited moderate to good activity ranging from 37-63 % of α-glucosidase enzyme inhibition. 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 alpha glucosidase enzyme inhibition acetamide, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Application of 31699-14-6

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

On November 30, 2019, Joshi, Shrinivas D.; Kumar, S. R. Prem; Patil, Sonali; Vijayakumar, M.; Kulkarni, Venkatarao H.; Nadagouda, Mallikarjuna N.; Badiger, Aravind M.; Lherbet, Christian; Aminabhavi, Tejraj M. published an article.COA of Formula: C9H8N2S The title of the article was Chemical synthesis, molecular modeling and pharmacophore mapping of new pyrrole derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth. And the article contained the following:

Abstract: Substituted phenylthiazolyl benzamide and pyrrolyl benzamide derivatives were developed using mol. hybridization technique to create novel lead antimycobacterial mols. used to fight against Mycobacteriumtuberculosis. The newly synthesized mols. have inhibited InhA, the enoyl-ACP reductase enzyme from the mycobacterial type II fatty acid biosynthetic pathway. Of these, compound 3b showed H-bonding interactions with Tyr158 and co-factor NAD+ that binds the active site of InhA. All the mols. were screened for in vitro antitubercular activity against M. tuberculosis H37Rv, as well as some representative mols. as the inhibitors of InhA. Thirteen compounds exhibited good anti-TB activities (MIC = 1.6μg/mL), but only few representative mols. showed the moderate InhA enzyme inhibition activity. [Figure not available: see fulltext.]. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).COA of Formula: C9H8N2S

The Article related to pyrrole inhibitor enoylacp reductase, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.COA of Formula: C9H8N2S

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

On June 15, 2004, Chen, Yen Ting; Seto, Christopher T. published an article.Electric Literature of 92-36-4 The title of the article was Parallel synthesis of a library of bidentate protein tyrosine phosphatase inhibitors based on the α-ketoacid motif. And the article contained the following:

Protein tyrosine phosphatases (PTPases) regulate intracellular signal transduction pathways by controlling the level of tyrosine phosphorylation in cells. These enzymes play an important role in a variety of diseases including type II diabetes and infection by the bacterium Yersinia pestis, which is the causative agent of bubonic plague. This report describes the synthesis, using parallel solution-phase methods, of a library of 104 potential inhibitors of PTPases. The library members are based on the bis(aryl α-ketocarboxylic acid) motif that incorporates a carboxylic acid on the central benzene linker. This carboxylic acid was coupled with a variety of different aromatic amines through an amide linkage. The aromatic component of the resulting amides is designed to make contacts with residues that surround the active site of the PTPase. The library was screened against the Yersinia PTPase and PTP1B. Based upon the screening results, four members of the library were selected for further study. These four compounds were evaluated against the Yersinia PTPase, PTP1B, TCPTP, CD45, and LAR. Compound 14 has an IC50 value of 590 nM against PTP1B and is a reversible competitive inhibitor. This affinity represents a greater than 120-fold increase in potency over compound 2, the parent structure upon which the library was based. A second inhibitor, compound 12, has an IC50 value of 240 nM against the Yersinia PTPase. In general, the selectivity of the inhibitors for PTP1B was good compared to LAR, but modest when compared to TCPTP and CD45. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Electric Literature of 92-36-4

The Article related to combinatorial library protein tyrosine phosphatase inhibitor alpha ketoacid, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Electric Literature of 92-36-4

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

Xing, Shuai; Zhang, Xue; Huang, Xia; Xie, Lin; Jiang, Fengchao; Zhou, Ping published an article in 2019, the title of the article was Modulating the conformation of the TIR domain by a neoteric MyD88 inhibitor leads to the separation of GVHD from GVT.Recommanded Product: 4-Phenylthiazol-2-amine And the article contains the following content:

Graft-vs.-host disease (GVHD) remains the least curable complication after allogeneic bone marrow transplantation (BMT). Myeloid differentiation factor 88 (MyD88) is an adaptor mol. critically involved in the toll-like receptor (TLR) signaling pathway. The Toll/IL-1 receptor (TIR) domains of MyD88 and TLR are interactional modules responsible for sorting and signaling via direct or indirect TIR-TIR interactions, which can contribute to all phases of GVHD progression. Here, we describe the mechanisms of the novel MyD88 inhibitor, TJ-M2010-5, and the discovery of its immunosuppressive properties in the context of GVHD and the graft-vs.-tumor (GVT) effect in a fully MHC-mismatched murine model. TJ-M2010-5 potentially interrupted the conformation of the TIR domain through its predicted DD loops, BB loops, and Poc site, and inhibited the homodimerization of MyD88, the LPS-stimulated activation of dendritic cells, and the priming of donor allogeneic T cell proliferation in a dose-dependent manner. Oral administration of TJ-M2010-5 ameliorated the inflammatory environment, decreased the number of apoptotic cells, increased tissue repair in GVHD target organs, and suppressed lethal GVHD. Further, protection against GVHD by TJ-M2010-5 did not abrogate a GVT effect against SP2/0, a myeloma cell line. Our data define the mechanisms of actions and provide novel insight into the potential clin. uses of TJ-M2010-5 for GVHD prevention. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Recommanded Product: 4-Phenylthiazol-2-amine

The Article related to tir domain neoteric inhibitor separation gvhd gvt modulating conformation, gvhd, gvt, myd88, tj-m2010-5, tlr, innate immunity, Immunochemistry: Other (Immunity, Immune Suppression, Tolerance, etc.) and other aspects.Recommanded Product: 4-Phenylthiazol-2-amine

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

On May 5, 2021, Chen, Jin-Ping; Battini, Narsaiah; Ansari, Mohammad Fawad; Zhou, Cheng-He published an article.Application of 24295-03-2 The title of the article was Membrane active 7-thiazoxime quinolones as novel DNA binding agents to decrease the genes expression and exert potent anti-methicillin-resistant Staphylococcus aureus activity. And the article contained the following:

A novel class of 7-thiazoxime quinolones was developed as potential antimicrobial agents for the sake of bypassing resistance of quinolones. Biol. assays revealed that some constructed 7-thiazoxime quinolones possessed effective antibacterial efficiency. Me acetate oxime derivative I exhibited 32-fold more active than ciprofloxacin against MRSA, which also possessed rapidly bactericidal ability and low toxicity towards mammalian cells. The combination use of 7-thiazoxime quinolone I and ciprofloxacin was able to improve antibacterial potency and effectively alleviate bacterial resistance. The preliminarily mechanism exploration revealed that compound I could destroy the cell membrane and insert into MRSA DNA to bind with DNA gyrase, then decrease the expression of gyrB and femB genes. The above results strongly suggested that Me acetate oxime derivative I held a promise for combating MRSA infection. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Application of 24295-03-2

The Article related to membrane active thiazoxime quinolone preparation mrsa antibacterial dna binding, cell membrane, drug-resistance, gene, mrsa dna, quinolone, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 24295-03-2

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

On July 31, 2007, Ukrainets, I. V.; Mospanova, E. V.; Sidorenko, L. V. published an article.Reference of 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was 4-hydroxy-2-quinolones. 122. 1-hydroxy-3-oxo-5,6-dihydro-3H-pyrrolo[3,2,1-ij]quinoline-2-carboxylic acid hetarylamides as potential antitubercular agents. And the article contained the following:

An improved method is reported for the synthesis of a series of 1-hydroxy-3-oxo-5,6-dihydro-3H-pyrrolo[3,2,1-ij]quinoline-2-carboxylic acid hetarylamides, e.g., I. The antitubercular activity of all of the compounds prepared has been studied. The structure-biol. activity dependence revealed is discussed. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Reference of 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to hydroxyoxodihydropyrroloquinoline carboxylic acid heteroaryl amine amidation, pyrroloquinoline amide hydroxyoxodihydro derivative preparation tuberculostatic activity, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Reference of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On May 26, 1983, Kinast, Guenther published a patent.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Intermediates useful in the preparation of cephalosporins. And the patent contained the following:

Thiazolines I [R = protective group; R1, R2 = (un)substituted alkyl, cycloalkyl, aryl, heterocyclic], useful as intermediates for cephalosporins II [R3 = (un)substituted alkyl, cycloalkyl, aryl, heterocyclic; R4 = appropriate substituent], were prepared Thus Et 2-amino-4-thiazolylacetate was treated with (Me3CO2C)2O to give I (R = Me3CO2C, R1 = CMe3, R2 = Et) which was treated with MeCHO to give III. Saponification of III to the acid, successive reaction with MeSO2Cl and 7-aminocephalosporanic acid, and deblocking gave II (R3 = Me, R4 = CH2OAc). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to aminothiazolylalkenamidocephem, cephem aminothiazolylalkenamido, Biomolecules and Their Synthetic Analogs: Beta-Lactam Fungal Metabolites and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On August 24, 1999, Hirota, Yoshihiro; Matsunaga, Tomonori published a patent.Name: Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of chloroacetylamino thiazoleacetic acid ester derivatives. And the patent contained the following:

The title cephalosporin intermediates of formula I [X = alkyl, aralkyl; Y = H2, O, alkoxyimino, carbalkoxy-alkoxyimino] are prepared Thus, chloroacetyl chloride was added slowly to Et 2-(2-aminothiazol-4-yl)-2(Z)-methoxyiminoacetate and propylene oxide acid capture agent in THF to give II in 84% yield. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Name: Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to thiazoleacetic acid ester chloroacetylamino preparation cephalosporin intermediate, Biomolecules and Their Synthetic Analogs: Beta-Lactam Fungal Metabolites and other aspects.Name: Methyl 2-(2-aminothiazol-4-yl)acetate

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