Day: November 1, 2022

On June 8, 2006, Jeppesen, Lone; Kristiansen, Marit published a patent.Formula: C7H10N2O2S2 The title of the patent was Preparation of N-heteroaromatic propionamides as glucokinase activators for treating diabetes and other diseases. And the patent contained the following:

The present invention describes 2,3-di-substituted N-heteroaromatic propionamides of Formula I ( wherein the * indicates an asym. atom; R1,R2 = H, halo, NH2, NHOH, C1-6 alkyl, perfluoro-C1-6 alkyl, etc.; R3 = C3-7 cycloalkyl and C2-4 alkyl; ring A = a monosubstituted or a disubstituted 5-6 membered heteroaromatic ring consisting of, in addition to the C=N shown, carbon atoms and 0-2 heteroatoms selected from S(O)p, 0, and N; p= 0-2) pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators for the treatment II diabetes and other disorders(no data given). The preparation of I is exemplified. For example, II was prepared in 2 steps by reacting intermediate 2-amino-5-(4-methylpiperazin-1-yl)thiazole (preparation given) with 3-cyclopentyl-2-(4-methanesulfonylphenyl)propionic acid. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Formula: C7H10N2O2S2

The Article related to heteroaromatic propionamide preparation glucokinase activator diabetes treatment, metabolic disorder treatment heteroaromatic propionamide glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Formula: C7H10N2O2S2

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

McKillop, Alexander; Sayer, Trevor S. B.; Bellinger, Geoffrey C. A. published an article in 1976, the title of the article was Reaction of benzothiazole and substituted benzothiazoles with dimethyl acetylenedicarboxylate. A novel heterocyclic ring transformation.Safety of Benzo[d]thiazol-6-ylmethanol And the article contains the following content:

Addnl. data considered in abstracting and indexing are available from a source cited in the original document. Reaction of benzothiazole with MeO2CCCCO2Me in aqueous methanol gave trans-dimethyl 4-formyl-2,3-dihydro-1,4-benzothiazine-2,3-dicarboxylate (I) in high yield, and a mechanism via intermediates II and III was proposed for this novel transformation. The scope and limitations of the process were defined by examination of the reactions of a wide range of substituted (e.g., 5- and 6-cyano, 5- and 6-Br, 5- and 6-AcNH) benzothiazoles with MeO2CCCCO2Me in aqueous methanol; the results are fully consistent with the postulated mechanism. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Safety of Benzo[d]thiazol-6-ylmethanol

The Article related to ring enlargement benzothiazole, benzothiazinedicarboxylate, acetylenedicarboxylate reaction benzothiazole, thiazole benzo ring enlargement, thiazinedicarboxylate benzo, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Safety of Benzo[d]thiazol-6-ylmethanol

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

Lepe-Balsalobre, Esperanza; Rubio-Sanchez, Ricardo; Ubeda, Cristina; Lepe, Jose Antonio published an article in 2022, the title of the article was Volatile compounds from in vitro metabolism of seven Listeria monocytogenes isolates belonging to different clonal complexes.Reference of 2-Acetylthiazole And the article contains the following content:

Microorganisms produce a wide variety of volatile organic compounds (VOCs) as products of their metabolism and some of them can be specific VOCs linked to the microorganism’s identity, which have proved to be helpful for the diagnosis of infection via odor fingerprinting. The aim of this study was to determine the VOCs produced and consumed to characterize the volatile metabolism of seven isolates of different clonal complexes (CCs) of Listeria monocytogenes. For this purpose, dichloromethane extracts from the thioglycolate broth medium were analyzed by gas chromatog. coupled to mass spectrometry (GC/MS). Also, multivariate analyses were applied to the data obtained. Results showed that all the isolates of L. monocytogenes produced de novo isobutanol, 2-methyl-1-butanol, 3-methyl-1-butanol, 3-(methylthio)-1-propanol, acetic acid, isobutyric acid, butanoic acid, and isovaleric acid. Significant differences were found among isolates for the production amount of these volatiles, which allowed their differentiation. Thus, CC4 (ST-219/CT-3650) and CC87 (ST-87/CT-4557) showed an active volatile compounds metabolism with high consumption nitrogen and sulfur compounds and production of alcs. and acids, and CC8 (ST-8/CT-8813) and CC3 (ST-3/CT-8722) presented a less active volatile metabolism Moreover, within the VOCs determined, huge differences were found in the production of butanol among the seven isolates analyzed, being probably a good biomarker to discriminate among isolates belonging to different CCs. Hence, the anal. of volatile profile generated by the growth of L. monocytogenes in vitro could be a useful tool to differentiate among CCs isolates. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Reference of 2-Acetylthiazole

The Article related to listeria monocytogenes volatile compound metabolism clonal complex, gc-ms, listeria monocytogenes, vocs, biomarkers, volatile compounds, Microbial, Algal, and Fungal Biochemistry: Metabolism and Microbial Nutrition and other aspects.Reference of 2-Acetylthiazole

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

On November 30, 2021, Sanad, Sherif M. H.; Mekky, Ahmed E. M. published an article.Application In Synthesis of 4-Phenylthiazol-2-amine The title of the article was Synthesis and antibacterial evaluation of new pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-one hybrids linked to different heteroarene units. And the article contained the following:

A three-component protocol involving the reaction of 3-aminothieno[2,3-b]pyridine-2-carboxylate, Me2NCH(OMe)2 and heteroaryl (bis)amines in dioxane under microwave irradiation yielded a new series of pyrimidinones. The target hybrids were formed by an initial formamidine formation, followed by cross-imidination and [5+1] heterocyclization. Pyrazole-linked pyrimidinones displayed the best antibacterial activity against all gram-pos. and neg. strains tested. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Application In Synthesis of 4-Phenylthiazol-2-amine

The Article related to pyridothienopyrimidinone preparation microwave antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of 4-Phenylthiazol-2-amine

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

On December 12, 2019, Lo, Wen-Ting; Belabed, Hassane; Haucke, Volker; Nazare, Marc; Kuecuekdisli, Murat published a patent.Application of 64987-16-2 The title of the patent was Preparation of fused pyrimidinones as class II phosphoinositide 3-kinase inhibitors useful in treatment of diseases. And the patent contained the following:

The invention relates to preparation of fused pyrimidinones of formula (I) as class II phosphoinositide 3-kinase inhibitors. Compounds I wherein R1, R2, and R3 each independently is N or C; R4 is H, halo, alkoxy, etc.; R5 can be absent (covalent bond to R6), C1-5 alkyl-cycloalkyl; R6 is H, alkyl, aryl, etc.; R7is S, absent (covalent bond to R8), NR, wherein R is H, etc.; R8 cycloalkyl, C1-5 alkyl, etc.; R9 is amide, amine, urea, etc.; R10 is 5-membered heterocyclyl or heteroaryl (except for pyrazolyl, tetrahydrofurfuryl), preferably a 5-membered aromatic heterocycle comprising one or more of N, O and/or S, etc.; n is 0-5, are claimed. The example compound II was prepared by multistep synthesis starting from Me 3-aminopyrazine-2-carboxylate (procedure given). Compounds I were evaluated for PI3K inhibiting activity (data given). Compounds I can be used as medicaments, in particular for the treatment of a medical condition associated with defective PI3K signalling. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Application of 64987-16-2

The Article related to fused pyrimidinone preparation pi3k inhibitor disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 64987-16-2

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

On March 31, 2020, Borthakur, Susanta Kumar; Kalita, Pabitra Kumar; Borthakur, Sukanya published an article.Category: thiazole The title of the article was Synthesis and antifungal activities of 3,5-diphenyl-7-amino-[1,3]-thiazolo[3,2-a]pyrimidine-6-nitrile derivatives. And the article contained the following:

A series of novel 3,7-diphenyl-7-amino[1,3]thiazolo[3,2-a]pyrimidine-6-nitrile derivatives I [R = H, 4-Me, 4-OMe, etc.] was synthesized by refluxing 2-amino-4-phenyl-1,3-thiazole and arylidinemalononitriles in propanol using NaOH as catalyst. Antifungal activities of the synthesized compounds were done by testing against Rhizoctonia solani and Drechslera orazae, two fungal pathogens causing diseases on rice crops. Among the tested compounds, compounds I [R = 4-Cl, 4-NMe2, 4-OMe, 3-OMe-4-OH] showed good to moderate antifungal activity. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Category: thiazole

The Article related to diphenyl amino thiazolopyrimidine nitrile preparation antifungal, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: thiazole

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

On December 26, 2017, Mai, Xi; Feng, Lihua; Liao, Yijing; Xu, Zhaoxing published a patent.SDS of cas: 64987-16-2 The title of the patent was Purine hydroxamic acid derivative and its preparation method and application in preparing drug for treating histone deacetylases mediated disease. And the patent contained the following:

The title purine hydroxamic acid derivative has structural formula I, wherein R1 is H or Me; R2 is H, halogen, alkyl, alkoxyl, alkylamino, hydroxyl, cyano or nitro. The derivative and its pharmaceutical composition can be used in preparing drug for treating histone deacetylases mediated disease, and has obvious inhibiting effect on histone deacetylases and anti-tumor activity. 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 purine hydroxamic acid preparation histone deacetylase antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 64987-16-2

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

Shaikh, Asif R.; Patel, Navin B.; Rajani, Dhanji published an article in 2014, the title of the article was Antimycobacterial and antimicrobial studies of newly synthesized 3-(4-(6-methylbenzo[d]thiazol-2-yl) phenyl)quinazolin-4(3H)-ones.HPLC of Formula: 92-36-4 And the article contains the following content:

The 7-chloro-2-(substituted)-3-(4-(6-methylbenzo[d]thiazol-2-yl)phenyl) quinazolin-4(3H)-ones e.g., I (R = furan-2-yl) have been prepared from the substituted acids, which were converted to substituted acetyl chlorides and cyclized with 4-chloro anthranilic acid afforded substituted benzoxazines 4(3H)-ones e.g., II and its further reaction with 4-(6-methylbenzo[d]thiazol-2-yl)aniline a gives desired compounds I. In vitro antitubercular activity was carried out against Mycobacterium tuberculosis H37Rv strain using Lowenstein-Jensen medium (conventional method) and antimicrobial activity against various bacteria and fungi using broth microdilution method. The compounds II, I were emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antituberculars. The compounds II, I showed better antitubercular activities compared to rifampicin and isoniazid. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).HPLC of Formula: 92-36-4

The Article related to quinazolinone preparation antibacterial antifungal antitubercular, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 92-36-4

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

On January 16, 2014, Jana, Gourhari; Kurhade, Sanjay Pralhad; Jagdale, Arun Rangnath; Kukreja, Gagan; Sinha, Neelima; Palle, Venkata P.; Kamboj, Rajender Kumar published a patent.Application of 1092942-42-1 The title of the patent was Preparation of tetrahydroquinazolinone derivatives as PARP inhibitors for treating cancer. And the patent contained the following:

Disclosed are compounds of formula I, their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, (wherein M is C, CH, and N, and the dotted bond is either a single or double bond with provisos; R1 is H and (un)substituted alkyl; R2 and R3 together with the carbon atom(s) to which they are attached form a (un)substituted carbocycle; each R4 is halogen, cyano, (un)substituted alkyl, etc.; R5 and R6 are independently H, halogen, (un)substituted alkyl, etc., or R5 and R6 together constitute oxo or form part of an (un)substituted carbocycle; R7a, R8a, R7b R8b, R7c, R8c, R7d, and R8d are independently H, halogen, (un)substituted alkyl, etc., or any two form oxo or form part of an (un)substituted carbocycle or (un)substituted heterocycle, thereby making ring A either a spiro-bicycle or a fused-bicycle or a bridged-bicycle; Ar is (un)substituted aryl or (un)substituted heteroaryl; p = 0-3; and n = 1-4), pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PARP enzyme of a subject. I can also be used to sensitize a patient that has developed a resistance to other chemotherapeutics. Synthetic procedures for preparing I are exemplified. Example compound II, prepared from intermediates Et 6-oxospiro[2.5]octane-5-carboxylate and 4-(4-(4-chlorophenyl)piperazin-1-yl)butanimidamide, had a PARP 1 inhibition IC50 between 1 nM and 500 nM. The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Application of 1092942-42-1

The Article related to tetrahydroquinazolinone derivative parp inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1092942-42-1

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

On December 31, 2020, Nizamuddin, N. D.; Abdul Ahad, Hindustan; Devanna, Nayakanti published an article.Application In Synthesis of 4-Phenylthiazol-2-amine The title of the article was Synthesis and molecular docking studies of some 1,2-dimethyl-3(4-substituted phenyl-1,3-thiazol-2-yl)2,3-dihydroquinazolin-4(1H)-ones as anticancer agents. And the article contained the following:

Synthesis of 1, 2-dimethyl-3(4-substituted phenyl-1,3-thiazol-2-yl)2,3-dihydro quinazolin-4(1H)-ones derivatives I [R = 4-Me, 2-OH, 4-Cl, etc.] was effected by refluxing 1,2-dimethylbenzoxazine-4-one with different 4-substituted phenyl-1,3-thiazol-2-amines. Synthesized compoundsI were characterized through elemental anal., IR, proton NMR, and Carbon-13 NMR. Mol. docking studies were carried out using Schrodinger Glide (version 2020_1) which was docked into selective P38alpha and Activin A Receptor Type 1 (ACVR1) Activin receptor-like kinase-2 (ALK2) kinase with Protein Data Bank (PDB) code 3GC7, 6GI6. Based on the docking score of synthesized quinazolin-4-one derivatives, I co-crystallized ligands interaction was evaluated with 5-fluorouracil (5-FU) as a reference drug. Compounds I [R = H, 4-MeO, 3-NH2, 2,4-OH] with P38alpha, I [R = 2-OH, 3-NH2, 4-Cl, 2,4-OH] with ACVR1 (ALK2) kinase score were -7.265, -7.078, -7.058 and -6.836; -8.929, -8.749, -8.735 and -8.464 Kcal/mol against enzymes responsible for cancer treatment. The results indicated that quinazolin-4-one derivatives I scored better than ligand and 5-FU. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Application In Synthesis of 4-Phenylthiazol-2-amine

The Article related to dimethyl phenyl thiazolyl dihydroquinazolinone preparation mol docking, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of 4-Phenylthiazol-2-amine

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