Hill, Matthew D.’s team published research in Bioorganic & Medicinal Chemistry Letters in 27 | CAS: 31784-71-1

Bioorganic & Medicinal Chemistry Letters published new progress about 31784-71-1. 31784-71-1 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorothiazolo[5,4-b]pyridin-2-amine, and the molecular formula is C6H4ClN3S, Category: thiazole.

Hill, Matthew D. published the artcileDevelopment of spiroguanidine-derived α7 neuronal nicotinic receptor partial agonists, Category: thiazole, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(3), 578-581, database is CAplus and MEDLINE.

We describe the synthesis of quinuclidine-containing spiroguanidines and their utility as α7 neuronal nicotinic acetylcholine receptor (nAChR) partial agonists. The convergent synthetic route developed for this study allowed for rapid SAR investigation and provided access to a structurally diverse set of analogs. A potent and selective α7 nAChR partial agonist, N-(6-methyl-1,3-benzoxazol-2-yl)-3′,5′-dihydro-4-azaspiro[bicyclo[2.2.2]octane-2,4′-imidazole]-2′-amine (BMS-910731, I), was identified. This compound induced immediate early genes c-fos and Arc in a preclin. rodent model of α7 nAChR-derived cellular activation and plasticity. Importantly, the ability to incorporate selectivity for the α7 nACh receptor over the 5-HT3A receptor in this series suggested a significant difference in steric requirements between the two receptors.

Bioorganic & Medicinal Chemistry Letters published new progress about 31784-71-1. 31784-71-1 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorothiazolo[5,4-b]pyridin-2-amine, and the molecular formula is C6H4ClN3S, Category: thiazole.

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

Lacriola, Christopher J.’s team published research in Antimicrobial Agents and Chemotherapy in 57 | CAS: 92-36-4

Antimicrobial Agents and Chemotherapy published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole.

Lacriola, Christopher J. published the artcileScreen for agents that induce autolysis in Bacillus subtilis, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole, the publication is Antimicrobial Agents and Chemotherapy (2013), 57(1), 229-234, database is CAplus and MEDLINE.

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.

Antimicrobial Agents and Chemotherapy published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole.

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

Kim, Dae-Shik’s team published research in ChemMedChem in 16 | CAS: 1192027-04-5

ChemMedChem published new progress about 1192027-04-5. 1192027-04-5 belongs to thiazole, auxiliary class Other Aliphatic Heterocyclic,Amine, name is N,N-Dimethyl-N’-(3-thioxo-3H-1,2,4-dithiazol-5-yl)formimidamide, and the molecular formula is C5H7N3S3, Application of N,N-Dimethyl-N’-(3-thioxo-3H-1,2,4-dithiazol-5-yl)formimidamide.

Kim, Dae-Shik published the artcileE7766, a Macrocycle-Bridged Stimulator of Interferon Genes (STING) Agonist with Potent Pan-Genotypic Activity, Application of N,N-Dimethyl-N’-(3-thioxo-3H-1,2,4-dithiazol-5-yl)formimidamide, the publication is ChemMedChem (2021), 16(11), 1740-1743, database is CAplus and MEDLINE.

A strategy for creating potent and pan-genotypic stimulator of interferon genes (STING) agonists is described. Locking a bioactive U-shaped conformation of cyclic dinucleotides by introducing a transannular macrocyclic bridge between the nucleic acid bases leads to a topol. novel macrocycle-bridged STING agonist (MBSA). In addition to substantially enhanced potency, the newly designed MBSAs, exemplified by clin. candidate E7766, exhibit broad pan-genotypic activity in all major human STING variants. E7766 is shown to have potent antitumor activity with long lasting immune memory response in a mouse liver metastatic tumor model. Two complementary stereoselective synthetic routes to E7766 are also described.

ChemMedChem published new progress about 1192027-04-5. 1192027-04-5 belongs to thiazole, auxiliary class Other Aliphatic Heterocyclic,Amine, name is N,N-Dimethyl-N’-(3-thioxo-3H-1,2,4-dithiazol-5-yl)formimidamide, and the molecular formula is C5H7N3S3, Application of N,N-Dimethyl-N’-(3-thioxo-3H-1,2,4-dithiazol-5-yl)formimidamide.

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

Al-Janabi, Ahmed S. M.’s team published research in Journal of Molecular Structure in 1228 | CAS: 95-24-9

Journal of Molecular Structure 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.

Al-Janabi, Ahmed S. M. published the artcileSynthesis, anti-bacterial evaluation, DFT study and molecular docking as a potential 3-chymotrypsin-like protease (3CLpro) of SARS-CoV-2 inhibitors of a novel Schiff bases, Quality Control of 95-24-9, the publication is Journal of Molecular Structure (2021), 129454, database is CAplus and MEDLINE.

New Schiff bases (L1H) I (I), (L2H) II (II), (L3H) III (III) were synthesized by reaction of 2-benzoylpyridine with different amines (2-amino-6-chlorobenzothiazole, isonicotinohydrazide and N1-(naphthalen-1-yl)ethane-1,2-diamine) and characterized by 1H-NMR, 13C-NMR, IR mass spectroscopy and elemental anal. The compounds (I), (II) and (III) were assayed by the disk diffusion method for anti-bacterial against five pathogenic bacteria species (Staphylococcus aureus, Micrococcus luteus, Staphylococcus pyogenes, Bacillus subtilis, and E. coli). All prepared Schiff bases (I), (II) and (III) showed good activity compared to pos. control (streptomycin). Moreover the L3H showed the highest activity against S. aureus, and M. luteus than the other compounds and streptomycin. In addnl. mol. docking studies with 3-chymotrypsin-like protease (3CLpro), the essential enzyme for SARS-CoV-2 proliferation. The rest of compounds have shown promising results as 3CLpro inhibitors interacting with the active sites of the enzymes. Finally, DFT’s estimated electrostatic mol. potential results were used to illustrate the mol. docking findings. The DFT calculations showed that L3H has the highest dipole moment and electrophilicity index. Interestingly, L2H of the largest energy gap ΔE = 2.49 eV, there are several hydrophilic interactions that could facilitate the binding with the receptors. All of these parameters could be shared to significantly affect the protein sites of binding affinity with different extent.

Journal of Molecular Structure 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

Hathoot, A. A.’s team published research in International Journal of Electrochemical Science in 6 | CAS: 92-36-4

International Journal of Electrochemical Science published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Quality Control of 92-36-4.

Hathoot, A. A. published the artcileElectrochemical and electrocatalytic properties of hybrid films composed of conducting polymer and metal hexacyanoferrate, Quality Control of 92-36-4, the publication is International Journal of Electrochemical Science (2011), 6(3), 637-649, database is CAplus.

Hybrid organic/inorganic modified electrode, composed of poly(2-(4-aminophenyl)-6-methylbenzothiazole) (PABT) matrix and Prussian blue (PB) like Ni hexacyanoferrate redox centers (PABT/NiHcF), showed reversible electrochem. behavior in aqueous electrolytes. Pt disk (Pt) was used as a conductive substrate onto which the composite film was electrodeposited by potential cycling. Electrochem. behavior of the modified electrode was well characterized using cyclic voltammetry (CV). The voltammetric characteristics of the composite modified electrodes were also studied in presence of different alkali metal cations (Li+, Na+, K+ ,Ce+ and NH4+). The heterogeneous electron transfer processes involving the composite and their stability were examined by subjecting the system to the long term cyclic voltammetric potential, cycling in 0.2 M NaCl electrolyte. Bilayer composite electrodes exhibit higher ionic conductivity, higher stability in comparison with pure inorganic (MeHcF) films. The inner electro active polymer chains in the film cause enhancement in the elec. conductivity of the composite electrodes. The modified electrode presented a good electrocatalytic activity towards the oxidation of MeOH, and oxalic acid (COOH)2.

International Journal of Electrochemical Science published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Quality Control of 92-36-4.

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

Abdel-Azzem, M.’s team published research in European Polymer Journal in 31 | CAS: 92-36-4

European Polymer Journal published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Product Details of C14H12N2S.

Abdel-Azzem, M. published the artcileElectrochemical copolymerization of 2-(4-aminophenyl)-6-methyl benzothiazole and aniline, Product Details of C14H12N2S, the publication is European Polymer Journal (1995), 31(12), 1207-13, database is CAplus.

Electropolymerization of 2-(4-aminophenyl)-6-Me benzothiazole (ABT) was carried out in acetonitrile. Potential sweep electrolysis of ABT at platinum electrode produced an electroactive polymeric film in acidic solutions Electropolymerization of ABT with different ratios of aniline were performed. The compositions of the copolymers were found by using 1H-NMR spectroscopy. Conductivity measurements were carried out on the copolymer prepared by constant current electrolysis. The films produced vary in their properties depending on the initial ratio of ABT to aniline. Films grown from a solution containing ABT and aniline in the ratio 50:50 exhibited good electroactivity and conductivity

European Polymer Journal published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Product Details of C14H12N2S.

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

Petrou, Anthi’s team published research in Molecules in 24 | CAS: 95-24-9

Molecules 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, Related Products of thiazole.

Petrou, Anthi published the artcileNovel thiazolidin-4-ones as potential non-nucleoside inhibitors of HIV-1 reverse transcriptase, Related Products of thiazole, the publication is Molecules (2019), 24(21), 3821, database is CAplus and MEDLINE.

Background: HIV is the causative agent of Acquired Immunodeficiency Syndrome (AIDS), an infectious disease with increasing incidence worldwide. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) play an important role in the treatment of AIDS. Although, many compounds are already being used as anti-HIV drugs, research for the development of new inhibitors continues as the virus develops resistant strains. Methods: The best features of available NNRTIs were taken into account for the design of novel inhibitors. PASS (Prediction of activity spectra for substances) prediction program and mol. docking studies for the selection of designed compounds were used for the synthesis. Compounds were synthesized using conventional and microwave irradiation methods and HIV RT inhibitory action was evaluated by colorimetric photometric immunoassay. Results: The evaluation of HIV-1 RT inhibitory activity revealed that seven compounds have significantly lower IC50 values than nevirapine (0.3μM). It was observed that the activity of compounds depends not only on the nature of substituent and it position in benzothiazole ring but also on the nature and position of substituents in benzene ring. Conclusion: Twenty four of the tested compounds exhibited inhibitory action lower than 4μM. Seven of them showed better activity than nevirapine, while three of the compounds exhibited IC50 values lower than 5 nM. Two compounds 9 and 10 exhibited very good inhibitory activity with IC50 1 nM.

Molecules 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, Related Products of thiazole.

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

Ofosu, Fred Kwame’s team published research in Antioxidants in 9 | CAS: 30931-67-0

Antioxidants published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C18H24N6O6S4, Application of Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate).

Ofosu, Fred Kwame published the artcilePhenolic profile, antioxidant, and antidiabetic potential exerted by millet grain varieties, Application of Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), the publication is Antioxidants (2020), 9(3), 254, database is CAplus and MEDLINE.

This study evaluated the potential antioxidant and antidiabetic properties in vitro of four millet grain varieties cultivated in South Korea. The free fractions were tested for their total antioxidant capacity using 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS+) and 2,2′-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assays, followed by α-glucosidase, α-amylase, and advanced glycation endproducts (AGEs) formation inhibition assays. The total phenolics, flavonoids, and condensed tannins in the free fractions ranged from 107.8 to 136.4 mg ferulic acid equivalent (FAE)/100 g, 101.3 to 115.8 mg catechin equivalent (CE)/100 g, and 17.65 to 59.54 mg catechin equivalent (CE)/100 g, resp. Finger Italian millet had the highest total phenolic content (136.4 mg FAE/100 g) and flavonoid content (115.8 mg CE/100 g). Barnyard and finger Italian millet showed the highest DPPH (IC50 = 359.6μg/mL and 436.25μg/mL, resp.) and ABTS radical scavenging activity (IC50 = 362.40μg/mL and 381.65μg/mL, resp.). Similarly, finger Italian millet also exhibited significantly lower IC50 values for the percentage inhibition of α-glucosidase (18.07μg/mL) and α-amylase (10.56μg/mL) as compared with acarbose (IC50 = 59.34μg/mL and 27.73μg/mL, resp.) and AGEs formation (33.68μg/mL) as compared with aminoguanidine (AG) (52.30μg/mL). All eight phenolic compounds identified in finger Italian millet were flavonoids, with flavanols being the predominant subclass. Taken together, millet flavonoids play important roles in the prevention and management of type 2 diabetes, and hence finger Italian millet has the potential to be developed as a functional food.

Antioxidants published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C18H24N6O6S4, Application of Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate).

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

Moharram, H. H.’s team published research in Egyptian Journal of Chemistry in 27 | CAS: 92-36-4

Egyptian Journal of Chemistry published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Product Details of C14H12N2S.

Moharram, H. H. published the artcileSynthesis of some benzothiazole derivatives of expected biological activity, Product Details of C14H12N2S, the publication is Egyptian Journal of Chemistry (1985), 27(2), 241-5, database is CAplus.

Benzothiazoles I [R = CONHR1 (R1 = Et, Bu, Ph, cyclohexyl), C(S)NHR2 (R2 = Me, allyl), COCH2NHNH2, COCH2NHN:CHR3 [R3 = 3,4-(MeO)2C6H3, 4-Me2NC6H4]] were prepared, starting from I (R = H), as potential bactericides.

Egyptian Journal of Chemistry published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Product Details of C14H12N2S.

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

Tay, Funda’s team published research in Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry in 53B | CAS: 56503-96-9

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about 56503-96-9. 56503-96-9 belongs to thiazole, auxiliary class Thiazole,Amine,Naphthalene, name is 4-(Naphthalen-1-yl)thiazol-2-amine, and the molecular formula is C11H14O2, Formula: C13H10N2S.

Tay, Funda published the artcileA quantum chemical DFT/HF study on acidity constants of some benzothiazole and thiazole derivatives, Formula: C13H10N2S, the publication is Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2014), 53B(1), 102-110, database is CAplus.

The acid dissociation (Ka) constants of some 4-and/or 6-substituted-2-aminobenzothiazole compounds have been investigated theor. The gas and aqueous phase geometries, thermal and solvation free energies have been calculated with full geometry optimization by using HF (6-31G(d)) and B3LYP (6-31G(d)) methods for 2-aminobenzothiazole, 2-aminothiazole derivatives and their fixed models. From the calculated acidity constants of investigated compounds, it has been detected that the protonation occurs at the the nitrogen atom of the amino group for 2-aminobenzothiazoles and at ring nitrogen atom for 2-aminothiazoles. Acceptable correlations have been observed between theor. (HF and B3LYP) and exptl. pKa values of the mols. with regression coefficients (R2 = 0.98, 0.86) and (R2 = 0.98, 0.85) for the protonation of benzothiazole and thiazole mols., resp. Theor. calculations also show that basicity of the studied compounds increase in the presence of electron donor substituents.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about 56503-96-9. 56503-96-9 belongs to thiazole, auxiliary class Thiazole,Amine,Naphthalene, name is 4-(Naphthalen-1-yl)thiazol-2-amine, and the molecular formula is C11H14O2, Formula: C13H10N2S.

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