Category: 95-24-9

Mishra, Chandra Bhushan published the artcileDiscovery of Potent Carbonic Anhydrase Inhibitors as Effective Anticonvulsant Agents: Drug Design, Synthesis, and In Vitro and In Vivo Investigations, HPLC of Formula: 95-24-9, the publication is Journal of Medicinal Chemistry (2021), 64(6), 3100-3114, database is CAplus and MEDLINE.

Two sets of benzenesulfonamide-based effective human carbonic anhydrase (hCA) inhibitors have been developed using the tail approach. The inhibitory action of these novel mols. was examined against four isoforms: hCA I, hCA II, hCA VII, and hCA XII. Most of the mols. disclosed low to medium nanomolar range inhibition against all tested isoforms. Some of the synthesized derivatives selectively inhibited the epilepsy-involved isoforms hCA II and hCA VII, showing low nanomolar affinity. The anticonvulsant activity of selected sulfonamides was assessed using the maximal electroshock seizure (MES) and s.c. pentylenetetrazole (s.c.-PTZ) in vivo models of epilepsy. These potent CA inhibitors effectively inhibited seizures in both epilepsy models. The most effective compounds17(I) and 22(II) showed long duration of action and abolished MES-induced seizures up to 6 h after drug administration. These sulfonamides were found to be orally active anticonvulsants, being nontoxic in neuronal cell lines and in animal models.

Journal of 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, HPLC of Formula: 95-24-9.

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

Liu, Hongtao published the artcileIdentification of N-benzothiazolyl-2-benzenesulfonamides as novel ABCA1 expression upregulators, SDS of cas: 95-24-9, the publication is RSC Medicinal Chemistry (2020), 11(3), 411-418, database is CAplus and MEDLINE.

ATP binding cassette transporter A1 (ABCA1) is a critical transporter that mediates cellular cholesterol efflux from macrophages to apolipoprotein A-I (ApoA-I). Therefore, increasing the expression level of ABCA1 is anti-atherogenic and ABCA1 expression upregulators have become novel choices for atherosclerosis treatment. In this study, a series of N-benzothiazolyl-2-benzenesulfonamides, based on the structure of WY06 discovered in our laboratory, were designed and synthesized as novel ABCA1 expression upregulators. Based on an in vitro ABCA1 upregulatory cell model, ABCA1 upregulation of target compounds was evaluated. Compounds 6c, 6d, and 6i have good upregulated ABCA1 expression activities, with EC₅₀ values of 0.97, 0.37, and 0.41μM, resp. A preliminary structure-activity relationship is summarized. Replacing the methoxy group on the benzothiazole moiety of WY06 with a fluorine or chlorine atom and exchanging the ester group with a cyano group resulted in more potent ABCA1 upregulating activity. Moreover, compound 6i increased ABCA1 mRNA and protein expression and significantly promoted cholesterol efflux in RAW264.7 cells. In conclusion, N-benzothiazolyl-2-benzenesulfonamides were identified as novel ABCA1 expression upregulators.

RSC 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

Pawde, A. V. published the artcileSynthesis and evaluation of antimicrobial, antioxidant activities of pyrido[3,2-d]pyrazolo[3,2-b]-4H-pyrimido[5,6-e]-4H-pyrimido[2,3-b]benzothiazole derivatives, HPLC of Formula: 95-24-9, the publication is Journal of Applicable Chemistry (Lumami, India) (2019), 8(2), 642-646, database is CAplus.

The objective of the present investigation was to synthesize 3-cyano-4-oxo-2-(methylthio)-6-N-Ph pyrido[3,2-d]pyrazolo[3,2-b]pyrimidine by condensation of 1-phenyl-1H-pyrazolo[3,4-b]pyridine-3-amine with Et cyano bis(methylthio)acrylate which on further condensation with various 2-amino 1/2/3/4-substituted benzothiazoles gives 15-imino-14-oxo-12-N-Ph pyrido[3,2-d]pyrazolo[3,2-b]-4H-pyrimido[5,6-e]-4H-pyrimido[2,3-b]benzothiazole and their 1/3 substituted derivatives I (R¹ = H, CH₃, OCH₃, Cl, NO₂; R² = H, CH₃). These newly synthesized compounds were further screened for antimicrobial and antioxidant properties.

Journal of Applicable Chemistry (Lumami, India) 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, HPLC of Formula: 95-24-9.

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

Pawde, A. V. published the artcileSynthesis and biological evaluation of some newly synthesized thiazolo-pyrimido-pyrimidobenzothiazoles, Synthetic Route of 95-24-9, the publication is European Journal of Biomedical and Pharmaceutical Sciences (2021), 8(4), 256-258, database is CAplus.

Condensation of 2-amino-5-methylthiazole with bis(methylthio)methylene malononitrile give 6-cyano-5-imino-2-methyl-7-(methylthio)-5H-thiazolo[3,2-a]pyrimidine. Which on further condensation with various 2-amino-substituted benzothiazoles yield 12, 13-diimino-9-methyl- thiazolo[2,3-a]-4H-pyrimido[4,5-d]-4H-pyrimido[2,1-b]benzothiazoles I (R¹ = H, Cl; R² = H, Me, OMe, F, Cl, NO₂; R³ = H, Me). Some of the newly synthesized compounds have been screened for their antimicrobial and antioxidant activity.

European Journal of Biomedical 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, Synthetic Route of 95-24-9.

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

Altug-Tasa, Burcugul published the artcileDesign, Synthesis and Biological Evaluation of a Novel Series of Thiadiazole- Based Anticancer Agents as Potent Angiogenesis Inhibitors, Category: thiazole, the publication is Anti-Cancer Agents in Medicinal Chemistry (2021), 21(15), 2041-2049, database is CAplus and MEDLINE.

Thiadiazole has attracted a great deal of interest as a versatile heterocycle for the discovery and development of potent anticancer agents. Thiadiazole derivatives exert potent antitumor activity against a variety of human cancer cell lines through various mechanisms. The goal of this work was to design and synthesize thiadiazole-based anticancer agents with anti-angiogenic activity. N-aryl-2-[(5-(aryl)amino-1,3,4-thiadiazol-2-yl)thio]acetamides (4a-r) were synthesized via the reaction of 5-(aryl)amino-1,3,4-thiadiazole-2(3H)-thiones with N-(aryl)-2-chloroacetamides in the presence of potassium carbonate. The compounds were investigated for their cytotoxic effects on three cancer (A549, HepG2, SH-SY5Y), two normal (HUVEC and 3T3-L1) cell lines using MTT and WST-1 assays. In order to examine whether the compounds have anti-angiogenic effects or not, HUVECs were cultured on matrigel matrix to create a vascular-like tube formation. Compounds 4d, 4m and 4n were more effective on A549 human lung adenocarcinoma cells than cisplatin. The IC₅₀ values of compounds 4d, 4m and 4n for A549 cell line were found to be 7.82 ± 0.4, 12.5 ± 0.22, 10.1 ± 0.52 μM, resp. when compared with cisplatin (IC₅₀= 20 ± 0.51 μM), while their IC₅₀ values for HUVEC cell line were determined as 138.7 ± 0.84, 78 ± 0.44, 177.6 ± 0.2 μM, resp. after 48 h of the treatment. The concentrations (10-20-50 μM) of compounds 4d, 4e, 4l, 4m, 4n, 4q and 4r were found to inhibit vascular like tube formation. According to their anticancer and anti-angiogenic effects, compounds 4d, 4m and 4n may be potential anticancer agents for further in vivo studies.

Anti-Cancer Agents in 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, Category: thiazole.

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

Maliyappa, M. R. published the artcileSix-substituted benzothiazole based dispersed azo dyes having antipyrine moiety: synthesis, characterization, DFT, antimicrobial, anticancer and molecular docking studies, Safety of 6-Chlorobenzothiazol-2-ylamine, the publication is Journal of the Iranian Chemical Society (2022), 19(9), 3815-3835, database is CAplus.

A series of benzothiazole based dispersed azo compounds I [R = H, Cl, Me, etc.] were synthesized by diazotization of benzothiazole derivatives coupling with antipyrine through traditional electrophilic substitution reaction in the temperature range of 0-5°C. The chem. structure of the prepared mols. I was characterized by various anal. and spectroscopic techniques. Further, the theor. vibrational and structural optimization studies of the mols. I were investigated by using DFT/B3LYP method. All the synthesized azo dyes I were evaluated for their in vitro antimicrobial activities against various bacterial and fungal strains, and the obtained results were exhibited to be potent antimicrobial activities compared with the reference compound Further, the mol. docking studies was performed and results showed the possible interaction between the synthesized chem. compound and the receptor. In addition, the in vitro anticancer activity of all the synthesized azo dyes was performed against different human cancer cell lines such as A549, K562 and MDA-MB-231 by using MTT assay.

Journal of the Iranian Chemical Society 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, Safety of 6-Chlorobenzothiazol-2-ylamine.

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

Maliyappa, M. R. published the artcile6-Substituted benzothiazole based dispersed azo dyes having pyrazole moiety: Synthesis, characterization, electrochemical and DFT studies, Name: 6-Chlorobenzothiazol-2-ylamine, the publication is Journal of Molecular Structure (2020), 126959, database is CAplus.

In the present work discusses synthesis, structural characterization and electrochem. investigation on some azo dyes derived from substituted benzothiazoles. The conventional diazo-coupling method was adopted to afford the heterocyclic azo dyes of benzothiazoles having pyrazole moiety. The obtained azo dyes were characterized by FT-IR, UV-visible, fluorescence, 1HNMR and, mass spectrometric techniques. The quantum chem. studies (DFT) was also used to interpret the structural properties of the compounds by using B3LYP program at 6-311++ (d, p) basis set. Further, the cyclic voltammetry was used to study the electrochem. behavior of the synthesized azo dyes in 0.1 M H₂SO₄ solution on a glassy carbon electrode at different scan rates.

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, Name: 6-Chlorobenzothiazol-2-ylamine.

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

Harisha, S. published the artcileSynthesis, characterization, pharmacological evaluation and molecular docking studies of benzothiazole azo derivatives, Safety of 6-Chlorobenzothiazol-2-ylamine, the publication is Journal of Molecular Structure (2020), 128477, database is CAplus.

A series of novel benzothiazole based azo dyes were synthesized and fully characterized by using different anal. techniques. The antioxidant activity of synthesized azo dyes was studied with the DPPH, hydrogen peroxide, metal chelating and nitric oxide radical methods and compared with the known antioxidant ascorbic acid. Further, the anticancer properties of synthesized azo dyes were carried out against breast cancer (MCF-7) cell lines by MTT assay and results revealed that the synthesized compounds exhibited good anticancer property in micro-molar range. Addnl., the anti-inflammatory activities of target compounds were also investigated by protein denaturation method and were found to have effective anti-inflammatory property. In order to predict the binding modes and binding affinity of synthesized compounds, they were docked into the active sites of protein B-cell lymphoma-extra-large (Bcl-xL) to predict their anticancer property. The synthesized compounds were found to have good affinity for B-cell lymphoma-extra-large (Bcl-xL). A good correlation was found between in-silico docking anal. and in biol. screening of all synthesized azo dyes with less binding energies and higher inhibition constants value against the target protein.

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, Safety of 6-Chlorobenzothiazol-2-ylamine.

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

Mor, Satbir published the artcileRegioselective synthesis of benzo[b]indeno[1,2-e][1,4]thiazin-11(10aH)-ones and antimicrobial evaluation thereof, HPLC of Formula: 95-24-9, the publication is Synthetic Communications (2022), 52(13-14), 1526-1536, database is CAplus.

Benzo[b]indeno[1,2-e][1,4]thiazin-11(10aH)-ones I [R = 2-F, 3-F, 4-Cl; R¹ = H, Cl, Br, Me, MeO] were synthesized regioselectively via cyclocondensation of 2,5-dibromo-2-(substitutedphenyl)-1H-indene-1,3(2H)-diones and 2-aminobenzenethiols using freshly dried EtOH as solvent with 42-60% yields. The synthesized derivatives I were well-characterized by employing different spectral techniques (FTIR, ¹H and ¹³C NMR, and HRMS) and X-ray crystallog. anal. All the derivatives I were examined for their preliminary in vitro antimicrobial activity against two Gram-pos. bacterial strains, i.e., B. subtilis, and S. aureus, two Gram-neg. bacterial strains, i.e., P. aeruginosa and E. coli, and two fungal strains, i.e., C. albicans and R. oryzae employing serial dilution method taking Ciprofloxacin and Fluconazole as standard reference drugs for antibacterial and antifungal activities, resp. Among all the tested derivatives I, derivative I [R = 4-Cl; R¹ = Br] was found to exhibit significant inhibition against all the microbial strains under study.

Synthetic Communications 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, HPLC of Formula: 95-24-9.

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

Walker, Erin Joanne published the artcileTranscriptomic changes during TGF-β-mediated differentiation of airway fibroblasts to myofibroblasts, Computed Properties of 95-24-9, the publication is Scientific Reports (2019), 9(1), 20377, database is CAplus and MEDLINE.

In this study, we have used next generation sequencing to delineate changes in transcriptome induced by TGF-β treatment of WI-38 airway fibroblasts in both short term and after differentiation into myofibroblasts. The data obtained from RNAseq anal. was confirmed by quant. PCR and protein expression by western blotting. We found that genes coding for intermediates in TGF-β signalling pathways (SMADs) were differentially expressed after TGF-β treatment, SMAD2 being upregulated and SMAD3 being downregulated. Genes involved in cytoskeletal pathways (FN1, LAMA, ITGB1) were upregulated in myofibroblasts. Genes that were previously shown to be changed in asthmatic lungs (ADAMTS1, DSP, TIMPs, MMPs) were similarly differentially expressed in myofibroblasts, strongly suggesting that TGF-β mediated differentiation of fibroblasts to myofibroblasts may underlie important changes in the asthmatic airway. We also identified new intermediates of signalling pathways (PKB, PTEN) that are changed in myofibroblasts compared to fibroblasts. We have found a significant number of genes that are altered after TGF-β induced transdifferentiation of WI-38 fibroblasts into myofibroblasts, many of which were expected or predicted. We also identified novel genes and pathways that were affected after TGF-β treatment, suggesting addnl. pathways are activated during the transition between fibroblasts and myofibroblasts and may contribute to the asthma phenotype.

Scientific Reports 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 C8H11NO, Computed Properties of 95-24-9.

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