Month: October 2022

Vafina, G. F.; Guryanova, T. S. published the artcile< Synthesis of S-Containing Maleopimaric Acid Derivatives>, Related Products of 96-53-7, the main research area is maleopimaric acid thio analog preparation.

New S-containing maleopimaric acid derivatives were synthesized. The structures of all synthesized compounds were elucidated using NMR spectroscopy and elemental analyses.

Chemistry of Natural Compounds published new progress about Diterpenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Related Products of 96-53-7.

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

Marwaha, Tejinder Kaur; Madgulkar, Ashwini; Bhalekar, Mangesh; Asgaonkar, Kalyani published the artcile< Molecular docking, synthesis, and characterization of chitosan-graft-2-mercaptobenzoic acid derivative as potential drug carrier>, COA of Formula: C3H5NS2, the main research area is docking chitosan mercaptobenzoic acid derivative drug carrier.

Chitosan is a hydrophilic polymer with prominent mucoadhesive properties. However, it forms weak hydrogen bonds with mucin thus limiting its mucoadhesion and exhibit reduced bioavailability due to its short retention time in the body. The aim of the present study was to synthesize and characterize novel thiolated chitosan with improved functional property. A unique approach of using mol. docking to select ligand to chem. modify chitosan has been employed in the present research. A set of ligands were screened virtually using docking anal. and 2-mercapto benzoic acid showed the lowest glide score of -4.31 Kcal/Mol thus displayed better binding interaction with chitosan. Based on the docking results, the best-fit ligand was selected for wet laboratory synthesis. 2-Mercapto benzoic acid was covalently attached to chitosan via formation of an amide bond and the reaction was mediated by carbodiimide and N-hydroxysuccinimide. The synthesized polymer was in turn evaluated for zeta potential, Fourier transformed IR, differential scanning calorimetry, mol. weight that confirmed conjugation of chitosan with the thiol ligand. The prepared thiomer was further subjected to mucoadhesion studies and displayed better mucoadhesion properties as compared to unmodified chitosan. Thus, the potential of the novel thiomer can be further explored as an excipient for drug delivery system with an emphasis on mucoadhesion.

Journal of Applied Polymer Science published new progress about Differential scanning calorimetry. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, COA of Formula: C3H5NS2.

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

Kamble, Sonali S.; Hese, Shrikant V.; Dawane, Bhaskar S.; Gacche, Rajesh N. published the artcile< Anti-breast cancer and antiangiogenic potential of substituted thiazolo[2,3-b] quinazoline derivatives: synthesis, in vitro and in vivo analysis>, Safety of 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is thiazolo quinazoline derivative antibreast cancer antiangiogenic potential.

Herein, a series of novel substituted thiazolo[2,3-b]quinazoline derivatives has been synthesized. The capability of the synthesized compounds 3a-i to hinder the viability of human breast cancer cell line (MCF-7) was assessed. The compounds were evaluated as possible inhibitors of angiogenesis by using in vivo chorioallantoic membrane (CAM) model. Amongst the compounds 3a-i screened, 3d and 3f exhibited excellent cytotoxicity with IC50 values 6.0±0.03μM & 5.0±0.36μM resp. Compounds were further tested to evaluate potential to inhibit the pro-angiogenic cytokines associated with tumor development. Both the compounds were found to be potent antiangiogenic agents against VEGF, TNFa, IL6, TGFb, and EGF. The outcome of the present study reveals that, compound 3d and 3f showed the promising inhibitory activity on the viability of MCF-7 cells. In the in vivo CAM model, treatment with all the compounds resulted in the significant decrease in blood vessels d. The findings of the study suggest that, compounds 3d & 3f may act as potential anti-breast cancer and antiangiogenic agents.

Chemistry & Biology Interface published new progress about Angiogenesis. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Safety of 2-Amino-4-(3-nitrophenyl)thiazole.

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

Rinaldi, Marta; Tintori, Cristina; Franchi, Luigi; Vignaroli, Giulia; Innitzer, Anna; Massa, Silvio; Este, Jose A.; Gonzalo, Encarna; Christ, Frauke; Debyser, Zeger; Botta, Maurizio published the artcile< A Versatile and Practical Synthesis toward the Development of Novel HIV-1 Integrase Inhibitors>, Safety of 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is preparation antiviral HIV1 integrase inhibitor.

As a continuation of our previous work, which resulted in the identification of a new hit compound as an HIV-1 integrase inhibitor, three novel series of salicylic acid derivatives were synthesized using three versatile and practical synthetic strategies and were assayed for their capacity to inhibit the catalytic activity of HIV-1 integrase. Biol. evaluations revealed that some of the synthesized compounds possess good inhibitory potency in enzymic assays and are able to inhibit viral replication in MT-4 cells at low micromolar concentrations Finally, docking studies were conducted to analyze the binding mode of the synthesized compounds within the DNA binding site of integrase in order to refine their structure-activity relationships.

ChemMedChem published new progress about Antiviral agents. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Safety of 3-Benzyl-2-thioxothiazolidin-4-one.

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

Chen, Ning; Du, Hongguang; Liu, Weidong; Wang, Shanshan; Li, Xinyao; Xu, Jiaxi published the artcile< Synthesis and Fungicidal Activity of Simple Structural 1,3-Thiazolidine-2-Thione Derivatives>, Category: thiazole, the main research area is vicinal aminoalc carbon disulfide cyclization coupling; thiazolidinethione preparation SAR antifungal activity.

A series of simple structural 1,3-thiazolidine-2-thione derivatives I and II [R1 = H, (s)-Me, (s)-Ph, etc; R2 = H, Me, (s)-Ph] with various substituents on the S-, N-, 4-, and 5-positions was synthesized with high yields from various vicinal amino alcs. via two steps and screened for their antifungal activity. Bioassay results reveal that some thiazolidine-2-thione derivatives show strong antifungal activities against P. capsici, G. zeae, S. sclerotiorum, A. alternata, B. cinerea, or R. solani. The SAR anal. indicates that N-acyl substituted and 4-alkyl substituents can enhance the antifungal activity. Notably, I [R1 = (s)-iPr, R2 = H] shows excellent activity against B. cinerea and G. zeae with IC50 values at 3.7 μg/mL and 6.5 μg/mL, resp., and I [ R1 = (s)-iBu, R2 = H] shows remarkable fungicidal activity against R. solani, S. sclerotiorum, and G. zeae with IC50 values at 1.0 μg/mL, 12.1 μg/mL, and 11.0 μg/mL, resp.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Category: thiazole.

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

Aryanasab, F.; Shokri, A.; Saidi, M. R. published the artcile< A simple approach to the synthesis of 3-substituted rhodanines and thiazolidine-2,4-diones>, Synthetic Route of 10574-69-3, the main research area is rhodanine thiazolidinedione preparation green chem; primary amine carbon disulfide bromoacetate three component reaction.

The green synthesis of 3-substituted rhodanine and thiazolidine-2,4-dione derivs . I [R = C6H5CH2, (CH2)3CH3, C6H5, 4-ClC6H4, etc.; X = S, O] via one-pot three-component reaction of primary amines RNH2, carbon disulfide and methyl-2-bromoacetate in water or under solvent-free conditions is described.

Scientia Iranica, Transaction C: Chemistry, Chemical Engineering published new progress about Green chemistry. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Synthetic Route of 10574-69-3.

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

Bursavich, Matthew G.; Gilbert, Adam M.; Lombardi, Sabrina; Georgiadis, Katy E.; Reifenberg, Erica; Flannery, Carl R.; Morris, Elisabeth A. published the artcile< Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)>, Synthetic Route of 10574-69-3, the main research area is thioxothiazolidinone preparation aggrecanase inhibitor SAR.

5-Benzylidene-2-thioxo-thiazolidin-4-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via com. available starting materials. The identified compounds show micromolar ADAMTS-5 potency and demonstrate SAR trends for both the aryl group and thioxothiazolidinone zinc chelator. This series of compounds represents steps toward a metalloprotease inhibitor as a disease-modifying osteoarthritis drug.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiarthritics. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Synthetic Route of 10574-69-3.

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

Hiremath, Shivayogi P.; Thakar, Shreeram B.; Purohit, Muralidhar G. published the artcile< Synthesis and condensation of 1-chloro-3,4-dihydro-4-oxopyridazino(4,5-b)indoles with 2-aminothiazoles and hydrazine>, Synthetic Route of 72054-60-5, the main research area is chlorodihydrooxopyridazinoindole condensation aminothiazole; pyridazinoindole bactericide preparation.

Condensation of the title compounds I (R = H, Br; R1 = Cl), prepared from II, with aminothiazoles III [R2 = Ph, Me, Et; R3 = H, Me, CO2Et; R2R3 = (CH2)4] and N2H4 gave IV and I (R1 = NHNH2) resp. IV (R = R3 = H, R2 = Ph) showed bactericidal activity.

Journal of the Indian Chemical Society published new progress about 72054-60-5. 72054-60-5 belongs to class thiazole, and the molecular formula is C7H10N2O2S, Synthetic Route of 72054-60-5.

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

Sami, Yuichi; Morita, Masataka; Kubota, Hirokazu; Hirabayashi, Ryoji; Seo, Ryushi; Nakagawa, Nobuaki published the artcile< Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit>, SDS of cas: 324579-90-0, the main research area is oral TRPV4 inhibitor preparation analgesic osteoarthritis.

Novel oral TRPV4 inhibitors were prepared and their potential for pain management in osteoarthritis discussed.

Bioorganic & Medicinal Chemistry published new progress about Analgesics. 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, SDS of cas: 324579-90-0.

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

Gundala, Trivikram Reddy; Godugu, Kumar; Nallagondu, Chinna Gangi Reddy published the artcile< Citric Acid-catalyzed Synthesis of 2,4-Disubstituted Thiazoles from Ketones via C-Br, C-S, and C-N Bond Formations in One Pot: A Green Approach>, Name: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is citric acid thiazole ketone chromatog one pot synthesis.

An improved and greener protocol has been developed for the synthesis of 2,4-disubstituted thiazoles via C-Br, C-S, and, C-N bond formations in a single step from readily available ketones, N-bromosuccinimide (NBS), and thiourea catalyzed by citric acid in a mixture of ethanol and water (3:1) under reflux conditions. This method has the advantages of freedom from the isolation of lachrymatory α-bromoketones, ease of carrying out, cleaner reaction profile, broad substrate scope, freedom from chromatog. purification, and suitability for large-scale synthesis.

Journal of the Chinese Chemical Society (Weinheim, Germany) published new progress about Chromatography. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Name: 2-Amino-4-(3-nitrophenyl)thiazole.

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