Tag: M.W=150-200

Margathe, Jean-Francois’s team published research in Journal of Medicinal Chemistry in 57 | CAS: 64987-16-2

Journal of Medicinal Chemistry published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Quality Control of 64987-16-2.

Margathe, Jean-Francois published the artcileStructure-Activity Relationship Studies toward the Discovery of Selective Apelin Receptor Agonists, Quality Control of 64987-16-2, the publication is Journal of Medicinal Chemistry (2014), 57(7), 2908-2919, database is CAplus and MEDLINE.

Apelin is the endogenous ligand for the previously orphaned G protein-coupled receptor APJ. Apelin and its receptor are widely distributed in the brain, heart, and vasculature, and are emerging as an important regulator of body fluid homeostasis and cardiovascular functions. To further progress in the pharmacol. and the physiol. role of the apelin receptor, the development of small, bioavailable agonists and antagonists of the apelin receptor, is crucial. In this context, E339-3D6 was described as the first nonpeptidic apelin receptor agonist. The authors show here that 1 is actually a mixture of polymethylated species, and they describe an alternative and versatile solid-phase approach that allows access to highly pure 27, the major component of 1. This approach was also applied to prepare a series of derivatives in order to identify the crucial structural determinants required for the ligand to maintain its affinity for the apelin receptor as well as its capacity to promote apelin receptor signaling and internalization. The study of the structure-activity relationships led to the identification of ligands 19, 21, and 38, which display an increased affinity compared to that of 27. The latter and 19 behave as full agonists with regard to cAMP production and apelin receptor internalization, whereas 21 is a biased agonist toward cAMP production Interestingly, the three ligands display a much higher stability in mouse plasma (T1/2 > 10 h) than the endogenous apelin-17 peptide 2 (T1/2 < 4 min).

Journal of Medicinal Chemistry published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Quality Control of 64987-16-2.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Jafari, Behzad’s team published research in ChemistrySelect in 4 | CAS: 95-24-9

ChemistrySelect published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Application of 6-Chlorobenzothiazol-2-ylamine.

Jafari, Behzad published the artcileSynthesis and Inhibitory Activity towards Monoamine Oxidase A and B of 8-Functionalized 3-Fluoro-2-methyl-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-ones, Application of 6-Chlorobenzothiazol-2-ylamine, the publication is ChemistrySelect (2019), 4(24), 7284-7291, database is CAplus.

An 8-chloro-3-fluoro-2-methyl-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-one was synthesized and employed in various palladium catalyzed cross-coupling-reactions, including Suzuki-Miyaura, Sonogashira and Buchwald-Hartwig reactions, delivering 8-aryl- I (R = C6H5, 4-FC6H4, 3-CH3C6H4, etc.), 8-alkynyl- I (R = CCC6H5, 4-CH3C6H4CC, 4-(CH3)3CC6H4CC) and 8-amino-3-fluoro-2-methyl-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-ones I (R = morpholin-4-yl, (4-fluorophenyl)aminyl, phenylaminyl, etc.) in good to excellent yields. The synthesized derivatives I were analyzed for their monoamine oxidase (MAO-A and MAO-B) inhibitory potential. Most of the compounds I exhibited moderate to good inhibitory activity towards MAO-A and/or MAO-B. Docking anal. was performed to verify the exptl. results. Hence, 8-substituted-3-fluoro-2-methyl-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-ones I might be potential lead compounds towards novel monoamine oxidase inhibitors.

ChemistrySelect published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Application of 6-Chlorobenzothiazol-2-ylamine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Acharya, Prachi T.’s team published research in Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry in 59B | CAS: 95-24-9

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, SDS of cas: 95-24-9.

Acharya, Prachi T. published the artcileSynthesis, docking study and biological evaluation of novel N-(1,3-benzothiazol-2-yl)-2-(pyridin-3-ylformohydrazido)acetamide derivatives, SDS of cas: 95-24-9, the publication is Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2020), 59B(11), 1721-1737, database is CAplus.

A series of N-(1,3-benzothiazol-2-yl)-2-(pyridin-3-ylformohydrazido)acetamide derivatives I (R = H, OMe, OEt, OH, Cl, F; X = H, N) have been synthesized by facile and efficient conventional method. Mol. docking revealed that synthesized derivatives and target proteins are actively involved in the binding pattern and had a significant correlation with biol. activity. Mol. dynamics studies have also been performed and ADME parameters for the synthesized compounds determined Biol. evaluation of all synthesized compounds have been carried out in vitro for their antibacterial, antituberculosis and antifungal efficacy against various bacterial and fungal strains and H37Rv. The different studies indicate that newly synthesized compounds possess moderate to good biol. activities.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, SDS of cas: 95-24-9.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Wu, Yue’s team published research in Chemical Communications (Cambridge, United Kingdom) in 57 | CAS: 95-24-9

Chemical Communications (Cambridge, United Kingdom) published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C10H10O2, Computed Properties of 95-24-9.

Wu, Yue published the artcileIron-catalyzed tandem oxidative coupling and acetal hydrolysis reaction to prepare formylated benzothiazoles and isoquinolines, Computed Properties of 95-24-9, the publication is Chemical Communications (Cambridge, United Kingdom) (2021), 57(26), 3271-3274, database is CAplus and MEDLINE.

The direct formylation of benzothiazoles and isoquinolines was reported. The reaction features a novel iron-catalyzed Minisci-type oxidative coupling process using com. available 1,3-dioxolane as a formylated reagent followed by acetal hydrolysis without a separation process. The reaction was performed under exceedingly mild reaction conditions and exhibited broad functional group tolerance.

Chemical Communications (Cambridge, United Kingdom) published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C10H10O2, Computed Properties of 95-24-9.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Kmari, Sangeeta’s team published research in World Journal of Pharmacy and Pharmaceutical Sciences in 10 | CAS: 95-24-9

World Journal of Pharmacy and Pharmaceutical Sciences published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Recommanded Product: 6-Chlorobenzothiazol-2-ylamine.

Kmari, Sangeeta published the artcileSynthesis, characterization & pharmacological activity of 1,2,4-triazole derivatives (Z)-1(benzo[d]thiazole-2-yl)(1-subsituted phenylidene) hydrazine containing benzothiazole, Recommanded Product: 6-Chlorobenzothiazol-2-ylamine, the publication is World Journal of Pharmacy and Pharmaceutical Sciences (2021), 10(11), 1204-1214, database is CAplus.

The present study shows effort to synthesize new triazole products I (R = 3-nitrol, 2,5-dihydroxy, 2-bromo-4-chloro, etc.) and measure them for anti-convulsion action through Maximal electrode shock attack method. First step, aniline and potassium thiocynate were synthesized and reacted through using bromine solution and glacial acetic acid formaylation and gave complex 6-chlorobenzo[d] thiazole-2-amine. The above compound 6-chlorobenzo[d] thiazole-2-amine was once responded by way of 6-chlorobenzo[d] thiazole-2-amine in the occurrence of ethylene glycol, and hydrazine hydrate to present 1-(6-chlorobenzo[d] thiazole-2yl) hydrazine (II). Complex II used to be allowable to reply with numerous substituted potassium thiocynate offers conforming triazole products. Triazole products II had been replied through acetophenone and giacial acetic acid and ethanol at reflux for 5h to afford complexes I. Last triazole (Z)-1-(benzo[d] thiazole-2-yl)-2-(1-subsituted phenylthylidene) hydrazine I, was synthesized from substituted acetophenone through the response with ethanol. Pharmacol. screening through an ear electrode prompted cutting-edge 51mA for 0.3 2d in electro-convulsiometer for anti-conversant activity. The synthesized compound Is used to be I. The complicated I (R = 4-methoxy, 4-hydroxy) was once set up to be maximum powerful complicated with associate to general medications phenytoin sodium.

World Journal of Pharmacy and Pharmaceutical Sciences published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Recommanded Product: 6-Chlorobenzothiazol-2-ylamine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Kamel, M.’s team published research in Kolorisztikai Ertesito in 18 | CAS: 1753-29-3

Kolorisztikai Ertesito published new progress about 1753-29-3. 1753-29-3 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Amine, name is Benzo[d][1,2,3]thiadiazol-5-amine, and the molecular formula is C6H5N3S, HPLC of Formula: 1753-29-3.

Kamel, M. published the artcileHeterocyclic azo dyes. V. Further studies on azo dyes containing a benzothiadiazole ring, HPLC of Formula: 1753-29-3, the publication is Kolorisztikai Ertesito (1976), 18(5-6), 155-61, database is CAplus.

Disperse and acid dyes were prepared by coupling 5-hydroxy-1,2,3-benzothiadiazole (I) [7686-40-0] with various aromatic amines, and their dyeing and fastness properties on nylon 66 or wool were determined The disperse dyes showed poor affinity for nylon (except at high temperature) in contrast to corresponding dyes from 5-amino-1,2,3-benzothiadiazole which have good affinity; the latter dyes also show better light- and washfastness. All the acid dyes, prepared by coupling I with diazotized naphthylamine sulfonic acids, showed good affinity for wool and good leveling properties; light- and washfastness were 2-3 and 3-4, resp.

Kolorisztikai Ertesito published new progress about 1753-29-3. 1753-29-3 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Amine, name is Benzo[d][1,2,3]thiadiazol-5-amine, and the molecular formula is C6H5N3S, HPLC of Formula: 1753-29-3.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Ward, E. R.’s team published research in Journal of the Chemical Society in | CAS: 1753-29-3

Journal of the Chemical Society published new progress about 1753-29-3. 1753-29-3 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Amine, name is Benzo[d][1,2,3]thiadiazol-5-amine, and the molecular formula is C11H14O4, Application of Benzo[d][1,2,3]thiadiazol-5-amine.

Ward, E. R. published the artcile1,2,3-Benzothiadiazole. III. Electrophilic substitution in 5- and 7-amino-1,2,3-benzothiadiazoles and the preparation of some substituted 1,2,3-benzothiadiazoles, Application of Benzo[d][1,2,3]thiadiazol-5-amine, the publication is Journal of the Chemical Society (1965), 1023-8, database is CAplus.

cf. CA 59:12787f. Bromination, iodination, nitration, and diazo-coupling of 5- and 7-amino-1,2,3-benzothiadiazoles, and some N-acyl derivatives, have been studied. The results largely confirm the interpretation of electrophilic substitution in the 1,2,3-benzothiadiazole system previously advanced. Some bromination reactions probably proceed by mechanisms other than simple electrophilic substitution. Spectroscopic anal. of the mixture of 5- and 7-nitro-1,2,3-benzothiadiazoles, obtained by nitration of the parent compound, shows that the 7-nitro isomer predominates. Preparation of nitro-, amino-, and hydroxy-1,2,3-benzothiadiazoles has been further investigated, particular attention being given to methods involving ring opening of appropriate benzothiazoles. The synthesis of 4-hydroxy-1,2,3-benzothiadiazole, an analog of 8-hydroxyquinoline, is described.

Journal of the Chemical Society published new progress about 1753-29-3. 1753-29-3 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Amine, name is Benzo[d][1,2,3]thiadiazol-5-amine, and the molecular formula is C11H14O4, Application of Benzo[d][1,2,3]thiadiazol-5-amine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Hoveyda, Hamid R.’s team published research in ACS Medicinal Chemistry Letters in 6 | CAS: 1375066-73-1

ACS Medicinal Chemistry Letters published new progress about 1375066-73-1. 1375066-73-1 belongs to thiazole, auxiliary class Thiadiazole,Hydrazine,Amine,Hydrazide,Amide, name is 3-Methyl-1,2,4-thiadiazole-5-carbohydrazide, and the molecular formula is C4H6N4OS, Name: 3-Methyl-1,2,4-thiadiazole-5-carbohydrazide.

Hoveyda, Hamid R. published the artcileOptimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II), Name: 3-Methyl-1,2,4-thiadiazole-5-carbohydrazide, the publication is ACS Medicinal Chemistry Letters (2015), 6(7), 736-740, database is CAplus and MEDLINE.

Further lead optimization on N-acyl-triazolopiperazine antagonists to the neurokinin-3 receptor (NK3R) based on the concurrent improvement in bioactivity and ligand lipophilic efficiency (LLE) is reported. Overall, compound I (LLE > 6) emerged as the most efficacious in castrated rat and monkey to lower plasma LH, and it displayed the best off-target safety profile that led to its clin. candidate nomination for the treatment of sex-hormone disorders.

ACS Medicinal Chemistry Letters published new progress about 1375066-73-1. 1375066-73-1 belongs to thiazole, auxiliary class Thiadiazole,Hydrazine,Amine,Hydrazide,Amide, name is 3-Methyl-1,2,4-thiadiazole-5-carbohydrazide, and the molecular formula is C4H6N4OS, Name: 3-Methyl-1,2,4-thiadiazole-5-carbohydrazide.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Li, Yudong’s team published research in iScience in 23 | CAS: 30536-19-7

iScience published new progress about 30536-19-7. 30536-19-7 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine, and the molecular formula is C6H4ClN3S, Application of 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine.

Li, Yudong published the artcileProton Transfer Can Govern Regioselectivity Assisted by Iron Catalysis, Application of 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine, the publication is iScience (2020), 23(6), 101214, database is CAplus and MEDLINE.

Ortho-selective aromatic C-H functionalization is frequently used in organic synthesis and chem./pharmaceutical industries. However, this reaction relies heavily on the use of directing groups suffering from limited substrate scope and extra steps to put on and remove the directing/protecting groups. Herein authors present the previously neglected concept that enables good to nearly complete selective ortho position. Proton transfer was utilized to tune the electron d. on the aryl ring and determine the positional selectivity of electrophilic substitution. Consistently with deuteration experiments and DFT studies, this work demonstrates that acid-promoted proton transfer directs accelerated ortho-selective halogenation of NH/OH contained aromatic amines/phenols with excellent selectivity (>40 examples; up to 98:2 ortho/para selectivity). The application potential of this Fe-catalyzed method is demonstrated by the convenient synthesis of three alkaloids and tizanidine. This report raises the possibility that proton transfer could serve as the basis of developing new selective C-H functionalization reactions.

iScience published new progress about 30536-19-7. 30536-19-7 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine, and the molecular formula is C6H4ClN3S, Application of 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

He, Wei-Bao’s team published research in Chinese Chemical Letters in 31 | CAS: 95-24-9

Chinese Chemical Letters published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Quality Control of 95-24-9.

He, Wei-Bao published the artcileVisible-light-initiated malic acid-promoted cascade coupling/cyclization of aromatic amines and KSCN to 2-aminobenzothiazoles without photocatalyst, Quality Control of 95-24-9, the publication is Chinese Chemical Letters (2020), 31(7), 1895-1898, database is CAplus.

By using ambient air as the oxidant and malic acid as the promoter, a practical method for the preparation of 2-aminobenzothiazoles through visible-light-initiated cascade reaction of aromatic amines and KSCN in eco-friendly bis(methoxypropy)ether under metal-, hazardous additive-, photocatalyst-free conditions was established.

Chinese Chemical Letters published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Quality Control of 95-24-9.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica