Tag: 200-300

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

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 November 20, 2008, Richter, Wolfgang published a patent.COA of Formula: C12H15NO3S The title of the patent was Preparation of tubulysine derivatives for treatment of cancer. And the patent contained the following:

The invention relates to novel cytotoxic peptides R1R2NCR3R4CONHCR5R6CONR7CR8R9-X-CHR10-A-CONHR11 [A is an optionally-substituted 5- or 6-membered heteroaryl ring; X is O, S, NR12, CR13R14, or CH2CR13R14; R1-R6, R8-R10, R12-R14 are independently H, optionally substituted alk(en)(yn)yl, aryl, heteroaryl, cycloalkyl, etc.; or two R groups form (hetero)cycloalkyl; R7 is alkyl, oxaalkyl, alkanoyl, CH2OCOPh, alkylaminoalkyl, hydroxyalkyl, etc.; R11 is -CH(CH2R15)(CH2)0-3CHR16R17, where R15 is optionally substituted aryl, heteroaryl, heterocycloalkyl,heteroalkylcycloalkyl, or heteroaralkyl;R16 is H, optionally alkyl, aryl, or heteroaryl;R17 is CO2H or ester, CONHNH2, OH, NH2, SH, or optionally substituted alkyl, cycloalkyl, heteroalkyl, orheterocycloalkyl] and their use for the treatment of cancer and other diseases. Thus, peptide I was prepared by a multistep procedure involving peptide coupling in solution Compounds of the invention show an activity against several cancer cell lines between 0.03 to 60 nM. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).COA of Formula: C12H15NO3S

The Article related to peptide tubulysine derivative preparation treatment cancer, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.COA of Formula: C12H15NO3S

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

On May 8, 2013, Hazra, Dipak K.; Mukherjee, Monika; Mukherjee, Alok K. published an article.Reference of 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Ab initio powder structure analysis and theoretical study of two thiazole derivatives. And the article contained the following:

Crystal structures of 2-amino-5-methylthiazole (1) and 4-(6-methyl-2-benzothiazolyl) aniline (2) have been determined from laboratory X-ray powder diffraction data along with an anal. of the Hirshfeld surfaces and 2D-fingerprint plots, facilitating a comparison of intermol. interactions. The DFT optimized mol. geometries in (1) and (2) agree closely with those obtained from the crystallog. studies. An interplay of NH···N/S hydrogen bonds and C/NH···π interactions connects the mols. of (1) and (2) into two-dimensional framework. Hirshfeld surface anal. of (1) indicates that the H···H and H···π contacts can account for 56.9% of the Hirshfeld surface area, whereas the corresponding fraction in (2) is 80.5%. 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 ab initio powder structure analysis theory thiazole, Physical Organic Chemistry: Other Reactions, Processes, and Spectra and other aspects.Reference of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On May 31, 2007, Sani, Monica; Fossati, Giacomo; Huguenot, Florent; Zanda, Matteo published an article.Reference of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate The title of the article was Total synthesis of tubulysins U and V. And the article contained the following:

A reliable and modular reaction sequence has been developed for the synthesis of the challenging tubulysin U and V (I, R = OAc, OH). This route allowed preparation of hundreds of milligrams of the stereochem. pure tetra-peptides, which are produced in small amounts by two different species of myxobacteria. This strategy made the full biol. evaluation of the tubulysins and their analogs possible. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Reference of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

The Article related to tubulysin asym preparation, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Reference of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

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

On September 1, 2009, Murray, Anthony; Lau, Jesper; Vedso, Per; Kristiansen, Marit; Jeppesen, Lone published a patent.SDS of cas: 859522-19-3 The title of the patent was Preparation of dicycloalkyl thiazolyl ureas as glucokinase activators. And the patent contained the following:

Title compounds represented by the formula R1R2NCONHA [wherein R1 = (un)substituted cyclohexyl; R2 = cyclohexyl; A = (un)substituted thiazolyl; and pharmaceutically acceptable salts, optical isomers or tautomers thereof] were prepared as glucokinase activators. For example, reaction of 2-aminothiazole with dicyclopentylamine and carbonyldiimidazole gave I. The glucose sensitivity of the title compounds are measured at a compound concentration of 10 μM and at glucose concentrations of 5 and 15 mM. The title compounds are useful as activators of glucokinase for the treatment of various diseases such as diabetes (no data). The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).SDS of cas: 859522-19-3

The Article related to dicycloalkyl thiazolyl urea preparation glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.SDS of cas: 859522-19-3

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

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

Title compounds represented by the formula R1R2NCONHA [wherein R1 = (un)substituted cyclohexyl; R2 = cyclohexyl; A = (un)substituted thiazolyl; and pharmaceutically acceptable salts, optical isomers or tautomers thereof] were prepared as glucokinase activators. For example, reaction of 2-aminothiazole with dicyclopentylamine and carbonyldiimidazole gave I. The glucose sensitivity of the title compounds are measured at a compound concentration of 10 μM and at glucose concentrations of 5 and 15 mM. The title compounds are useful as activators of glucokinase for the treatment of diabetes (no data). 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 dicycloalkyl thiazolyl urea preparation glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Related Products of 859522-19-3

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

On January 18, 2007, Lau, Jesper; Murray, Anthony; Vedsoe, Per; Kristiansen, Marit; Jeppesen, Lone published a patent.Category: thiazole The title of the patent was Preparation of cyclohexyl thiazolyl ureas as glucokinase activators. And the patent contained the following:

Title compounds represented by the formula R1R2NCONHA [wherein R1 = (cycloalkyl)alkyl, cycloalkyl, heterocyclyl, etc.; R2 = (cyclo)alkyl, cycloalkenyl, heterocyclyl, etc.; A = (un)substituted heteroaryl; and pharmaceutically acceptable salts, optical isomers or tautomers thereof] were prepared as glucokinase activators. For example, reductive condensation of phenethylamine with cyclohexanone, followed by coupling reaction with Et (2-aminothiazol-5-ylsulfanyl)acetate in the presence of 1,1′-carbonyldiimidazole and hydrolysis, gave I. The glucose sensitivity of the title compounds are measured at a compound concentration of 10 μM and at glucose concentrations of 5 and 15 mM. The title compounds are useful as activators of glucokinase for the treatment of various diseases, e.g. for the treatment of type 2 diabetes (no data). The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Category: thiazole

The Article related to cyclohexyl thiazolyl urea preparation glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Category: thiazole

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

On November 8, 2007, Murray, Anthony; Lau, Jesper; Jeppesen, Lone; Vedsoe, Per published a patent.Related Products of 859522-19-3 The title of the patent was Preparation of thiazolyl benzamides as glucokinase activators. And the patent contained the following:

Title compounds [I; m = 0-2; n = 0-4; R1 = OH, hydroxyalkyl, fluoroalkyl, Cll, F, Br, iodo, alkyl, alkenyl, alkynyl, amino, cyano, Ph, (substituted) heterocyclyl, etc.; R2 = YX; X = OZ, OZOZ, CO2Z, SZ, SOZ, SO2Z, etc.; Z, Z1 = bond, alkenylene, etc.; Y = (substituted) QZ1, etc.; Q = aryl, heterocyclyl, cycloalkyl; B = substituted 5-10 membered heterocyclyl], were prepared as glucokinase activators (no data). Thus, title compound Me [2-(3-isopropoxy-5-phenoxybenzoylamino)thiaol-5-ylsulfanyl]acetate was prepared in 4 steps from Me 3-isopropoxy-5-hydroxybenzoate, phenylboronic acid, 5-bromo-2-aminothiazole, 3-isopropoxy-5-phenoxybenzoic acid, and Me mercaptoacetate. 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 thiazolyl benzamide preparation glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Related Products of 859522-19-3

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

On July 21, 2005, Murray, Anthony; Lau, Jesper; Jeppesen, Lone; Vedso, Per; Ankersen, Michael; Lundbeck, Jane Marie; Kristiansen, Marit; Valcarce-Lopez, Maria Carmen; Polisetti, Dharma Rao; Subramanian, Govindan; Andrews, Robert Carl; Christen, Daniel P.; Cooper, Jeremy T.; Santhosh, Kalpathy Chidambareswaran published a patent.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate The title of the patent was Preparation of heteroaryl ureas and their use as glucokinase activators. And the patent contained the following:

Title compounds I [wherein R1, R2 = (un)substituted cycloalk(en)yl, heterocyclyl or heterocycloalkenyl; A = (un)substituted heteroaryl, or pharmaceutically acceptable salts, stereoisomers and tautomers thereof] were prepared For example, treatment of 2-aminothiazole with carbonyldiimidazole followed by condensation with dicyclohexylamine gave urea II. The invented compounds are activators of glucokinase, and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial (no data). The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

The Article related to urea heteroaryl preparation glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

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