Day: October 13, 2022

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

Zhang, Xiaolin; Yang, Hongxia Ou; Ding, Yonghong published the artcile< The synthesis and characterization of potential novel active compounds, 2-aminothiazole derives Schiff bases>, Safety of 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is aromatic ketone thiourea cyclocondensation; aminothiazole preparation condensation aryl aldehyde; Schiff base preparation.

Some 4-substituted-2-aminothiazoles were prepared starting from aromatic ketones and thiourea in the presence of powered iodine. Then treating 4-substituted-2-aminothiazole with substituted benzaldehyde gave corresponding 2-aminothiazole derivatives Schiff bases in good yield.

Advanced Materials Research (Durnten-Zurich, Switzerland) published new progress about Amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (heteroaryl). 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

Li, Jian-Yuan; Miklossy, Gabriella; Modukuri, Ram K.; Bohren, Kurt M.; Yu, Zhifeng; Palaniappan, Murugesan; Faver, John C.; Riehle, Kevin; Matzuk, Martin M.; Simmons, Nicholas published the artcile< Palladium-Catalyzed Hydroxycarbonylation of (Hetero)aryl Halides for DNA-Encoded Chemical Library Synthesis>, Recommanded Product: Thiazole-5-carboxyaldehyde, the main research area is palladium catalyzed hydroxycarbonylation heteroaryl halide DNA encoded library synthesis.

A strategy for DNA-compatible, palladium-catalyzed hydroxycarbonylation of (hetero)aryl halides on DNA-chem. conjugates has been developed. This method generally provided the corresponding carboxylic acids in moderate to very good conversions for (hetero)aryl iodides and bromides, and in poor to moderate conversions for (hetero)aryl chlorides. These conditions were further validated by application within a DNA-encoded chem. library synthesis and subsequent discovery of enriched features from the library in selection experiments against two protein targets.

Bioconjugate Chemistry published new progress about Carbonylation. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Recommanded Product: Thiazole-5-carboxyaldehyde.

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

Liu, Tracy W.; Gammon, Seth T.; Fuentes, David; Piwnica-Worms, David published the artcile< Multi-modal multi-spectral intravital macroscopic imaging of signaling dynamics in real time during tumor-immune interactions>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is bioluminescence; imaging reporters; immune cell imaging; intravital imaging; molecular imaging; tumor signaling; tumor–immune interactions.

A major obstacle in studying the interplay between cancer cells and the immune system has been the examination of proposed biol. pathways and cell interactions in a dynamic, physiol. relevant system in vivo. Intravital imaging strategies are one of the few mol. imaging techniques that can follow biol. processes at cellular resolution over long periods of time in the same individual. Bioluminescence imaging has become a standard preclin. in vivo optical imaging technique with ever-expanding versatility as a result of the development of new emission bioluminescent reporters, advances in genomic techniques, and tech. improvements in bioluminescence imaging and processing methods. Herein, we describe an advance of technol. with a mol. imaging window chamber platform that combines bioluminescent and fluorescent reporters with intravital macro-imaging techniques and bioluminescence spectral unmixing in real time applied to heterogeneous living systems in vivo for evaluating tumor signaling dynamics and immune cell enzyme activities concurrently.

Cells published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

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