Category: thiazolidine

Altered KYN/TRP, Gln/Glu, and Met/methionine sulfoxide ratios in the blood plasma of medication-free patients with major depressive disorder was written by Umehara, Hidehiro;Numata, Shusuke;Watanabe, Shin-ya;Hatakeyama, Yutaka;Kinoshita, Makoto;Tomioka, Yukiko;Nakahara, Kiyoshi;Nikawa, Takeshi;Ohmori, Tetsuro. And the article was included in Scientific Reports in 2017.COA of Formula: C4H7NO2S This article mentions the following:

Capillary electrophoresis-time-of-flight mass spectrometry (CE-TOFMS) is a comprehensive, quant., and high throughput tool used to analyze metabolite profiles. In the present study, we used CE-TOFMS to profile metabolites found in the blood plasma of 33 medication-free patients with major depressive disorder (MDD) and 33 non-psychiatric control subjects. We then investigated changes which occurred in the metabolite levels during an 8-wk treatment period. The medication-free MDD patients and control subjects showed significant differences in their mean levels of 33 metabolites, including kynurenine (KYN), glutamate (Glu), glutamine (Gln), methionine sulfoxide, and methionine (Met). In particular, the ratios of KYN to tryptophan (TRP), Gln to Glu, and Met to methionine sulfoxide were all significantly different between the two groups. Among the 33 metabolites with altered levels in MDD patients, the levels of KYN and Gln, as well as the ratio of Gln to Glu, were significantly normalized after treatment. Our findings suggest that imbalances in specific metabolite levels may be involved in the pathogenesis of MDD, and provide insight into the mechanisms by which antidepressant agents work in MDD patients. In the experiment, the researchers used many compounds, for example, Thiazolidine-4-carboxylic acid (cas: 444-27-9COA of Formula: C4H7NO2S).

Thiazolidine-4-carboxylic acid (cas: 444-27-9) 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 have been applied as prodrug derivatives for various steroids containing a 3-carbonyl group to improve their topical anti-inflammatory activity. COA of Formula: C4H7NO2S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Thiaproline and selenaproline transport in E. coli was written by Di Girolamo, Mario;Cini, Chiara;Busiello, Vincenzo;Coccia, Raffaella;De Marco, Carlo. And the article was included in Physiological Chemistry and Physics and Medical NMR in 1984.SDS of cas: 16310-13-7 This article mentions the following:

The proline transport system in Escherichia coli KL16 was studied. Its K_m is 0.5 μM, and this value is not affected by the presence of glucose nor by pH variations in the range 5.5-8. The proline transport is inhibited by β- and γ-thiaproline, and β- and γ-selenaproline, proline isologs with the methylene group in β or in γ position substituted by an S or Se. The inhibition is of the competitive type and pH-dependent. The K_i values show that all isologs have an affinity for the transport system that is much lower than that of proline; selena isologs have lower affinity than thia isologs. In the experiment, the researchers used many compounds, for example, Thiazolidine-2-carboxylic acid (cas: 16310-13-7SDS of cas: 16310-13-7).

Thiazolidine-2-carboxylic acid (cas: 16310-13-7) belongs to thiazolidine derivatives. Thiazolidine motifs are very intriguing heterocyclic five-membered moieties present in diverse natural and bioactive compounds having sulfur at the first position and nitrogen at the third position. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.SDS of cas: 16310-13-7

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Intercluster aurophilicity-driven aggregation lighting circularly polarized luminescence of chiral gold clusters was written by Han, Zhen;Zhao, Xueli;Peng, Peng;Li, Si;Zhang, Chong;Cao, Man;Li, Kai;Wang, Zhao-Yang;Zang, Shuang-Quan. And the article was included in Nano Research in 2020.COA of Formula: C6H11NS2 This article mentions the following:

Herein, we prepared two novel pairs of enantiomeric gold cluster complexes, AU₄PL₄/Au₄PD₄ and (Au₄L₄)n/(Au₄D₄)n with at. precision. In Au₄PL₄/Au₄PD₄, the discrete chiral Au4-based aggregation-induced emission (AIE) luminogens are separated by bulky substitutes. The corresponding aggregates are cyan-emitting with a photoluminescence quantum yield (PLQY) of 14.4%. Upon decreasing the size of the substituents, these chiral Au4 clusters are strung together by inter-cluster Au-Au interactions, which cause a low-energy green emission from the aggregated (Au4L4)n/(Au4D4)n with a much higher PLQY of 41.4% and more intense circularly polarised photoluminescence (CPL) with a dissymmetry factor |gPL| of 7.0 x 10-3. Using (Au4L4)n/(Au4D4)n, circularly polarised organic light-emitting diodes (CP-OLEDs) were for the first time fabricated. These findings signify that inter-cluster metallophilic interactions are a new and important type of driving force for AIE and crystallization-induced emission (CIE), suggesting great potential of CPL-active metal clusters in CP-OLEDs. In the experiment, the researchers used many compounds, for example, (S)-4-Isopropylthiazolidine-2-thione (cas: 76186-04-4COA of Formula: C6H11NS2).

(S)-4-Isopropylthiazolidine-2-thione (cas: 76186-04-4) 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. 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.COA of Formula: C6H11NS2

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Ethyl lactate mediated 1,3-dipolar cycloaddition of azomethine ylides: a design, synthesis and antibacterial activity of novel dispiro heterocycles was written by Sharma, Kanti;Sharma, Lokesh K.;Jain, Meenakshi;Jain, Renuka. And the article was included in Chemistry & Biology Interface in 2018.Related Products of 444-27-9 This article mentions the following:

A facile, greener and efficient one-pot, three-component procedure for the synthesis of novel dispirooxindolopyrrolothiazole derivatives carried out by cycloaddition reaction of 3-methyl-1-phenyl-4-thiophenylidene-5-pyrazolone dipolarophile, azomethine ylides generated in-situ, via decarboxylative condensation of isatin with thiazolidine-4-carboxylic acid was reported using Et lactate as a recyclable solvent in excellent yield without using any catalyst. This green route provided mild reaction conditions, high yields of products in short reaction time, high regio- and stereoselectivity, operational simplicity and environmentally benign synthesis. The synthesized compounds were characterized by anal. and spectral (IR, ¹H-NMR, ¹³C-NMR and FAB mass) data. All synthesized compounds were screened for antibacterial activity against B. subtilis, S. aureus, E. coli and P. aeruginosa bacteria. In the experiment, the researchers used many compounds, for example, Thiazolidine-4-carboxylic acid (cas: 444-27-9Related Products of 444-27-9).

Thiazolidine-4-carboxylic acid (cas: 444-27-9) 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. Thiazolidines have been applied as prodrug derivatives for various steroids containing a 3-carbonyl group to improve their topical anti-inflammatory activity. Related Products of 444-27-9

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Derivatives of 2-thiazolidinecarboxylic acid was written by Pazenko, Z. N.. And the article was included in Ukrains’kii Khemichnii Zhurnal in 1958.Recommanded Product: Thiazolidine-2-carboxylic acid This article mentions the following:

(EtO)₂CHCO₂H (I) and H₂N(CH₂)₂SH, m. 97°, (from (CH₂)₂NH and H₂S) form in EtOH 2-thiazolidinecarboxylic acid (II), decompose 203°. The Et ester of I forms similarly that of II, m. 37°, HCl salt m. 207-9°, and an unidentified compound, 9.36% N, m. 230°. Cl₂CHCO₂Me forms the Me ester of II, b₄ 8.9°, m. 25°. II, (CH₂)₂O, and BF₃ in Et₂O form 3-β-hydroxyethyl-2-thiazolidinecarboxylic acid δ-lactone, m. 87-9°. MeCOCO₂H and MeCOCO₂Et and H₂N(CH₂)₂SH form the 2-Me derivative of II and its Et ester, m. 192-5° and b₄ 72-5°, resp. In the experiment, the researchers used many compounds, for example, Thiazolidine-2-carboxylic acid (cas: 16310-13-7Recommanded Product: Thiazolidine-2-carboxylic acid).

Thiazolidine-2-carboxylic acid (cas: 16310-13-7) belongs to thiazolidine derivatives. Thiazolidine derivatives have been found to exhibit very prominent anti-inflammatory and anti-nociceptive activity. Thiazolidine-2,4-dione (TZD) is an important derivative of thiazolidine with a sulfur and nitrogen atom in positions 1 and 3, and carbonyl in position 4 of the ring. These derivatives have a wide range of medicinal applications such as antiviral, antimicrobial, anticonvulsant, antiinflammatory, and antimalarial activities.Recommanded Product: Thiazolidine-2-carboxylic acid

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Unique anti-myeloma activity by thiazolidine-2,4-dione compounds with Pim inhibiting activity was written by Fujii, Shiro;Nakamura, Shingen;Oda, Asuka;Miki, Hirokazu;Tenshin, Hirofumi;Teramachi, Jumpei;Hiasa, Masahiro;Bat-Erdene, Ariunzaya;Maeda, Yusaku;Oura, Masahiro;Takahashi, Mamiko;Iwasa, Masami;Endo, Itsuro;Yoshida, Sumiko;Aihara, Ken-ichi;Kurahashi, Kiyoe;Harada, Takeshi;Kagawa, Kumiko;Nakao, Michiyasu;Sano, Shigeki;Abe, Masahiro. And the article was included in British Journal of Haematology in 2018.Formula: C13H13NO3S This article mentions the following:

Proviral integrations of Moloney virus 2 (PIM2) is overexpressed in multiple myeloma (MM) cells, and regarded as an important therapeutic target. Here, we aimed to validate the therapeutic efficacy of different types of PIM inhibitors against MM cells for their possible clin. application. Intriguingly, the thiazolidine-2,4-dione-family compounds SMI-16a and SMI-4a reduced PIM2 protein levels and impaired MM cell survival preferentially in acidic conditions, in contrast to other types of PIM inhibitors, including AZD1208, CX-6258, and PIM447. SMI-16a also suppressed the drug efflux function of breast cancer resistance protein, minimized the sizes of side populations and reduced in vitro colony-forming capacity and in vivo tumorigenic activity in MM cells, suggesting impairment of their clonogenic capacity. PIM2 is known to be subject to ubiquitination-independent proteasomal degradation Consistent with this, the proteasome inhibitors bortezomib and carfilzomib increased PIM2 protein levels in MM cells without affecting its mRNA levels. However, SMI-16a mitigated the PIM2 protein increase and cooperatively enhanced anti-MM effects in combination with carfilzomib. Collectively, the thiazolidine-2,4-dione-family compounds SMI-16a and SMI-4a uniquely reduce PIM2 protein in MM cells, which may contribute to their profound efficacy in addition to their immediate kinase inhibition. Their combination with proteasome inhibitors is envisioned. In the experiment, the researchers used many compounds, for example, 5-(4-propoxybenzylidene)thiazolidine-2,4-dione (cas: 587852-28-6Formula: C13H13NO3S).

5-(4-propoxybenzylidene)thiazolidine-2,4-dione (cas: 587852-28-6) 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. Thiazolidines unsubstituted on the nitrogen atom are readily hydrolyzed by boiling aqueous solutions of acids or bases and the dissociation is complete in the presence of a compound reacting with one of the cleavage products.Formula: C13H13NO3S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

A Convenient Synthesis of Thiazolidin-2-ones from Thiazolidine-2-thiones: Antibiotic Activity and Revisiting the Mechanism was written by Deng, Xiao-Bing;Chen, Ning;Wang, Zhi-Xin;Li, Xin-Yao;Hu, Hong-Yan;Xu, Jia-Xi. And the article was included in Phosphorus, Sulfur and Silicon and the Related Elements in 2011.Computed Properties of C6H11NS2 This article mentions the following:

Various substituted thiazolidin-2-ones were synthesized from the corresponding thiazolidine-2-thiones with bromoethanol in ethanol with sodium ethoxide as a base. The optimal reaction conditions and mechanism were reinvestigated in detail. The bioassay indicated that (S)-4-iso-butylthiazolidin-2-one and (S)-4-benzylthiazolidin-2-one show certain inhibitive activities against Candida albicans and Escherichia coli. In the experiment, the researchers used many compounds, for example, (S)-4-Isopropylthiazolidine-2-thione (cas: 76186-04-4Computed Properties of C6H11NS2).

(S)-4-Isopropylthiazolidine-2-thione (cas: 76186-04-4) 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. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.Computed Properties of C6H11NS2

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Stereoselective syntheses of (+)-isoretronecanol and (+)-5-epi-tashiromine via addition of chiral titanium(IV) enolates to cyclic N-acyliminium ions was written by Pereira, Elaine;de Fatima Alves, Conceicao;Bockelmann, Maria Alice;Pilli, Ronaldo A.. And the article was included in Quimica Nova in 2008.Application In Synthesis of (S)-4-Isopropylthiazolidine-2-thione This article mentions the following:

The stereoselective addition of the titanium (IV) enolates derived from (S)-4-isopropyl-N-4-chlorobutyryl-1,3-thiazolidine-2-thione and from (S)-4-isopropyl-N-4-chloropentanoyl-1,3-thiazolidine-2-thione to N-Boc-2-methoxypyrrolidine afforded the addition products (+)-I [R = (CH₂)₂Cl, (CH₂)₃Cl, resp.] in 84% yield in both cases, as 8.6:1 and 10:1 diastereoisomeric mixtures, resp. A three-step sequence allowed to convert these adducts to (+)-isoretronecanol and (+)-5-epi-tashiromine II [X = CH₂, (CH₂)₂, resp.] in 43% and 49% overall yield, resp. In the experiment, the researchers used many compounds, for example, (S)-4-Isopropylthiazolidine-2-thione (cas: 76186-04-4Application In Synthesis of (S)-4-Isopropylthiazolidine-2-thione).

(S)-4-Isopropylthiazolidine-2-thione (cas: 76186-04-4) 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. Thiazolidines have been applied as prodrug derivatives for various steroids containing a 3-carbonyl group to improve their topical anti-inflammatory activity. Application In Synthesis of (S)-4-Isopropylthiazolidine-2-thione

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Ethyl 6′-cyano-7′-phenyl-1′,6′,7′,7a′-tetrahydro-3′H-spiro[indeno[1,2-b]quinoxaline-11,5′-pyrrolo[1,2-c]thiazole-6′-carboxylate was written by Muthuselvi, C.;Athimoolam, S.;Srinivasan, N.;Ravikumar, B.;Pandiarajan, S.;Krishnakumar, R. V.. And the article was included in IUCrData in 2018.Formula: C4H7NO2S This article mentions the following:

In the title compound, C22H22ClN4O2S, the angle between the mean planes of the indene ring and the quinoxaline ring system is 3.93 (11)°. The five-membered indene and thiazole rings both adopt envelope conformations while the pyrrole ring adopts a twisted conformation. The two acceptor O atoms form a chelated three-centered hydrogen bond with a Ph C atom. In the experiment, the researchers used many compounds, for example, Thiazolidine-4-carboxylic acid (cas: 444-27-9Formula: C4H7NO2S).

Thiazolidine-4-carboxylic acid (cas: 444-27-9) 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.Formula: C4H7NO2S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com

Ambruticins: Tetrahydropyran ring formation and total synthesis was written by Bowen, James I.;Wang, Luoyi;Crump, Matthew P.;Willis, Christine L.. And the article was included in Organic & Biomolecular Chemistry in 2021.Application of 76186-04-4 This article mentions the following:

The ambruticins are a family of polyketide natural products which exhibit potent antifungal activity. Gene knockout experiments are in accord with the proposal that the tetrahydropyran ring of the ambruticins is formed via the AmbJ catalyzed epoxidation of the unsaturated 3,5-dihydroxy acid, ambruticin J, followed by regioselective cyclization to ambruticin F. Herein, a convergent approach to the total synthesis of ambruticin J (I) is described as well as model studies involving epoxidation and cyclizations of unsaturated hydroxy esters to give tetrahydropyrans and tetrahydrofurans. The total synthesis involves preparation of three key fragments which were united via a Suzuki-Miyaura cross-coupling and Julia-Kocienski olefination to generate the required carbon framework. Global deprotection to a triol and selective oxidation of the primary alc. gave, after hydrolysis of the lactone, ambruticin J. In the experiment, the researchers used many compounds, for example, (S)-4-Isopropylthiazolidine-2-thione (cas: 76186-04-4Application of 76186-04-4).

(S)-4-Isopropylthiazolidine-2-thione (cas: 76186-04-4) 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.Application of 76186-04-4

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com