Month: December 2022

Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors was written by Li, Qifei;Li, Jieming;Cai, Yan;Zou, Yuxing;Chen, Bin;Zou, Feng;Mo, Jiaxian;Han, Ting;Guo, Weiwei;Huang, Wenlong;Qiu, Qianqian;Qian, Hai. And the article was included in Bioorganic & Medicinal Chemistry in 2020.Synthetic Route of C4H5NO2S This article mentions the following:

Bromodomain-containing protein 4 (BRD4) is a key epigenetic regulator in cancer; and inhibitors targeting BRD4 exhibit great anticancer activity. By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors I (R = OEt, OH, tert-butylamino, cyclopropylamino, piperidin-1-yl, morpholin-4-yl, etc.) and II were designed and synthesized. Compound I [R = cyclopentylamino] (III) had a hydrophobic acetylcyclopentanyl side chain, showing the most potent BRD4 inhibitory activity in the BRD4-BD1 inhibition assay (IC₅₀ value of 110 nM), and it also significantly suppressed the proliferation of MV-4-11 cells with high BRD4 level (IC₅₀ value of 0.42μM). Furthermore, the potent apoptosis-promoting and G0/G1 cycle-arresting activities of compound III were indicated by flow cytometry. As the downstream-protein of BRD4, c-Myc was in significantly low expression by compound III treatment in a dose-dependent manner. All the findings supported that the novel compound III provided a perspective for developing effective BRD4 inhibitors. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Synthetic Route of C4H5NO2S).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidine derivatives have been found to exhibit very prominent anti-inflammatory and anti-nociceptive activity. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.Synthetic Route of C4H5NO2S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Influence of substituents on the synthesis of thiazolidinones was written by Sahu, M.;Garnaik, B. K.;Behera, Rajani. And the article was included in Indian Journal of Chemistry in 1987.Safety of 3-Methylthiazolidine-2,4-dione This article mentions the following:

Unsym. thioureas R¹NHCSNHR² (R¹ = arylthiazolyl, Ph, pyridyl, allyl, ClC₆H₄, O₂NC₆H₄; R² = allyl, Me, cyclohexyl, Ph, anisyl) were heated with ClCH₂CO₂H in EtOH to give iminothiazolidinones I. The addition reaction of R¹NH₂ with R²NCS gave the thioureas. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Safety of 3-Methylthiazolidine-2,4-dione).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. The thiazolidine ring is a cyclic N,S acetal, and most syntheses of perhydrothiazolo [3,2-a]pyridines construct the five-membered ring by condensation of aldehydes or ketones either as such or masked. In addition, the use of thiazolidines as an inhibitor of tyrosyl-DNA phosphodiesterase Iand influenza neuraminidase, pro-drugs for the treatment of cystinosis, radioprotective against γ-irradiation and as S1P1 receptor agonist has also been reported.Safety of 3-Methylthiazolidine-2,4-dione

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Computational study of molecular electrostatic potential, drug likeness screening and structure-activity/property relationships of thiazolidine-2,4-dione derivatives was written by Medjahed, Sihem;Belaidi, Salah;Djekhaba, Salim;Tchouar, Noureddine;Kerassa, Aicha. And the article was included in Journal of Bionanoscience in 2016.Recommanded Product: 16312-21-3 This article mentions the following:

Mol. geometry, electronic properties, effect of the substitution, and structure phys.-chem. relationship for thiazolidine-2,4-dione derivatives have been studied by d. functional theory (DFT) theory. In the present work, the calculated values, namely, net charges, mol. electrostatic potential (MESP) contours/surfaces have also been drawn to explain the electronic activity of thiazolidine-2,4-dione, bond lengths, dipole moments, heats of formation, Quant. structure- activity relationship (OSAR) properties, Lipinski’s and Veber’s parameters, Ligand efficiency (LE), Lipophilic Efficiency (LipE), etc., are reported and discussed in this paper. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Recommanded Product: 16312-21-3).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. In the thiazolidine nucleus, a large number of substitutions are possible on 2, 4 and 5 positions responsible for enhancing the compound’s pharmaceutical importance. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.Recommanded Product: 16312-21-3

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Synthesis of spirocyclic thiazolidinediones using ring-closing metathesis and one-pot sequential ring-closing/cross metathesis was written by Dhara, Kalyan;Paladhi, Sushovan;Midya, Ganesh Chandra;Dash, Jyotirmayee. And the article was included in Organic & Biomolecular Chemistry in 2011.Application In Synthesis of 3-Methylthiazolidine-2,4-dione This article mentions the following:

A novel synthetic route to spirocyclic thiazolidinediones is reported by utilizing ring-closing metathesis (RCM). A selective cross metathesis (CM) of N-allyl azaspiro derivatives with different olefins has been demonstrated to prepare substituted azaspiro-[4.4]nonenediones. The X-ray crystal structure of a spirocyclic thiazolidinedione dimer is described, which has been prepared in two steps from thiazolidinedione using a one-pot sequential ring-closing and self metathesis. Cross metathesis proceeds smoothly with both electron rich and poor olefins. The sym. bis-thiazolidinedione spirocyclic system can be used as CM coupling partner with olefins. One-pot sequential RCM-CM has been developed for the synthesis of substituted spirocyclic compounds The methodol. allows a quick access to thiaazaspiro[4.4]nonene and -[4.5]decenedione ring systems from readily available starting materials which are not otherwise accessible. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Application In Synthesis of 3-Methylthiazolidine-2,4-dione).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidine is a heterocyclic compound with five-membered saturated ring with a thioether group and an amine group in 1 and 3 positions of the ring. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.Application In Synthesis of 3-Methylthiazolidine-2,4-dione

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Design and synthesis of novel L-tyrosine derivatives containing phenoxyacetyl structural unit and and PPAR agonist activities was written by Zhou, Li-jiang;Yan, Ju-fang;Zhang, Kun;Fan, Li;Chen, Xin;Yang, Da-cheng. And the article was included in Yaoxue Xuebao in 2013.Electric Literature of C4H5NO2S This article mentions the following:

The design, synthesis and bioevaluation of a series of novel L-tyrosine derivatives as peroxisome proliferator-activated receptor(PPAR) agonists are reported. Four intermediates and twenty L-tyrosine derivatives containing phenoxyacetyl structural unit TM1 were synthesized starting from L-tyrosine via four step reactions including esterification of carboxyl group, phenoxyacetylation of α-amino group, bromoalkylation of phenolic hydroxyl group and then nucleophilic substitution reaction with various heterocyclic amines in 21%-75% overall yield. L-tyrosine derivatives TM1 were hydrolyzed to give sixteen corresponding target compounds TM2 in 77%-99% yield. The chem. structures of the thirty-nine new compounds were identified using ¹H NMR, ¹³C NMR techniques and thirty-five compounds were confirmed by HR-MS techniques. Screening results in vitro show that the PPAR relative activation activities of the target mols. are weak overall, while compound TM2i reaches 50.01%, which indicates that the mol. structures of these obtained compounds need to be modified further. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Electric Literature of C4H5NO2S).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidines undergo hydrolysis to aldehyde and amino thiol under acid or basic aqueous conditions. Open-chain compounds are obtained when thiazolidines are treated with tris(trimethylsilyl)silane in a reaction in which the thiazolidine derivatives act as a source of α-aminoalkyl radicals.Electric Literature of C4H5NO2S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Organic reactions in ionic liquids. Ionic liquid-accelerated facile synthesis of 3-alkyl-2,4-thiazolidinediones was written by Yang, De-Hong;Yang, Ben-Yong;Chen, Zhen-Chu;Chen, Song-Ying;Zheng, Qin-Guo. And the article was included in Journal of Chemical Research in 2005.Application In Synthesis of 3-Methylthiazolidine-2,4-dione This article mentions the following:

The room temperature ionic liquid [bmim]PF₆ is a new green solvent for the N-alkylation of 2,4-thiazolidinones. Significant rate enhancement and improved yields were observed In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Application In Synthesis of 3-Methylthiazolidine-2,4-dione).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidine is an important scaffold and has a wide range of promising biological activities. Thiazolidine derivatives have reported anti-inflammatory and anti-nociceptive activity. Open-chain compounds are obtained when thiazolidines are treated with tris(trimethylsilyl)silane in a reaction in which the thiazolidine derivatives act as a source of α-aminoalkyl radicals.Application In Synthesis of 3-Methylthiazolidine-2,4-dione

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Coupling kinetics of 4-sulfobenzenediazonium ion with 2,4-thiazolidinedione, its 3-methyl derivative and 3-methyl-5-isoxazolone was written by Kavalek, Jaromir;Machacek, Vladimir;Sterba, Vojeslav. And the article was included in Collection of Czechoslovak Chemical Communications in 1994.Category: thiazolidine This article mentions the following:

3- And 4-substituted 5-phenylazo derivatives of 2,4-thiazolidinedione were prepared as potential biol. active fungicides. The kinetics of coupling of 4-sulfobenzenediazonium salt with 2,4-thiazolidinedione and 3-methyl-2,4-thiazolidinedione have been studied and the results have been compared with kinetic data of coupling reaction of 3-methyl-5-isoxazolone. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Category: thiazolidine).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidine is a heterocyclic compound with five-membered saturated ring with a thioether group and an amine group in 1 and 3 positions of the ring. Thiazolidine is prepared as it was in its first reported synthesis, by the condensation of cysteamine and formaldehyde. Other thiazolidines may be synthesized by similar condensations. A notable derivative is 4-carboxythiazolidine, derived from formaldehyde and cysteine.Category: thiazolidine

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Functionalization of Meldrum’s acid by Diels-Alder approach was written by Kotha, Sambasivarao;Gaikwad, Vidyasagar. And the article was included in Heterocycles in 2022.Electric Literature of C4H5NO2S This article mentions the following:

Author’s have synthesized several Meldrum’s acid derivatives using Diels-Alder reaction as a key step. Here, the key sultine derivative is prepared by rongalite and the sultine derivative is useful as a latent diene. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Electric Literature of C4H5NO2S).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Derivatives, thiazolidines, are known. For example, the drug pioglitazone contains a thiazolidine ring. Another drug that contains a thiazolidine ring is the antibiotic penicillin. Thiazolidine and its composites are key components of many natural products and drugs , and are also present in many synthetic compounds such as anticancer, anti-inflammatory, antitubercular, antifungal, antiviral, anti-HIV, cytotoxicity, antitrypanosomal, antinociceptive and anti-hypernociceptive compounds.Electric Literature of C4H5NO2S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Discovery, synthesis and SAR analysis of novel selective small molecule S1P₄-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype was written by Urbano, Mariangela;Guerrero, Miguel;Velaparthi, Subash;Crisp, Melissa;Chase, Peter;Hodder, Peter;Schaeffer, Marie-Therese;Brown, Steven;Rosen, Hugh;Roberts, Edward. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.HPLC of Formula: 16312-21-3 This article mentions the following:

High affinity and selective S1P₄ receptor (S1P₄-R) small mol. agonists may be important proof-of-principle tools used to clarify the receptor biol. function and effects to assess the therapeutic potential of the S1P₄-R in diverse disease areas including treatment of viral infections and thrombocytopenia. A high-throughput screening campaign of the Mol. Libraries-Small Mol. Repository was carried out by our laboratories and identified (2Z,5Z)-5-((1-(2-fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)methylene)-3-methyl-2-(methylimino) thiazolidin-4-one I as a promising S1P₄-R agonist hit distinct from literature S1P₄-R modulators. Rational chem. modifications of the hit allowed the identification of a promising lead mol. with low nanomolar S1P₄-R agonist activity and exquisite selectivity over the other S1P_1-3,5-Rs family members. The lead mol. herein disclosed constitutes a valuable pharmacol. tool to explore the effects of the S1P₄-R signaling cascade and elucidate the mol. basis of the receptor function. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3HPLC of Formula: 16312-21-3).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. In the thiazolidine nucleus, a large number of substitutions are possible on 2, 4 and 5 positions responsible for enhancing the compound’s pharmaceutical importance. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.HPLC of Formula: 16312-21-3

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

PEG-600 mediated one-pot synthesis of quinolinylidenethiazolidinediones as potential anti-hyperglycemic agents was written by Riyaz, Sd;Naidu, A.;Dubey, P. K.. And the article was included in Indian Journal of Chemistry in 2012.Related Products of 16312-21-3 This article mentions the following:

Knoevenagel condensation between quinoline-2-carboxaldehyde (I) and active-methylene-containing 2,4-thiazolidinedione in PEG-600 at 100° for 2 h, without the usage of any base, yields 5-quinolin-2-ylidenethiazolidine-2,4-dione, which on alkylation gives N-substituted derivatives (II). Both the reaction steps can be performed under one-pot conditions. Alternatively, II can also be synthesized by condensation of N-substituted thiazolidine-2,4-dione with I in PEG-600 at 100°C. The α,β-unsaturated carbonyl derivatives II are subjected to C:C reduction using Mg turnings in refluxing EtOH to yield 5-(quinolin-2-ylmethyl)thiazolidine-2,4-diones in high yields, which are novel potential anti-hyperglycemic agents (no data). In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Related Products of 16312-21-3).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidine derivatives have been found to exhibit very prominent anti-inflammatory and anti-nociceptive activity. Open-chain compounds are obtained when thiazolidines are treated with tris(trimethylsilyl)silane in a reaction in which the thiazolidine derivatives act as a source of α-aminoalkyl radicals.Related Products of 16312-21-3

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com