Category: 10574-69-3

Zaveri, Mehul; Kawathekar, Neha published the artcile< Synthesis, characterization and antimalarial activity of some new 3-benzyl-2-thioxothiazolidin-4-one derivatives>, Category: thiazole, the main research area is benzyl thioxothiazolidinone preparation antimalarial.

In present investigation, a series of new 3-benzyl-2-thioxothiazolidin-4-one I (Ar = Ph, 2-pyrrolyl, 4-pyridyl, etc.) derivatives, have been synthesized using conventional and microwave-assisted technique. These compounds were evaluated for in-vitro antimalarial activity by microdilution technique against resistance strains of Plasmodium falciparum. The result of antimalarial activity revealed that six compounds I (Ar = Ph, 2-furanyl, 2-pyridyl, 4-pyridyl, 4-Me2NC6H4, 2-HOC6H4) exhibited IC50 values ranging from 0.8-1.2 μg/mL, four compounds I (Ar = 4-ClC6H4, 4-FC6H4, 2-indolyl, 3-O2NC6H4) displayed antimalarial activity IC50 values in the range of 0.7-0.8 μg/mL. Compound I (Ar = 2-pyrrolyl) showed most significant result with maximum IC50 value of 0.7 μg/mL, thus it could be identified as structural lead for further development of new antimalarial agents.

International Journal of Pharmacy and Pharmaceutical Research published new progress about Antimalarials. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Category: thiazole.

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

Takeda, Norihiko; Taguchi, Tomoyo; Nakajima, Takeshi; Azuma, Mitsuyoshi published the artcile< Design, synthesis and biological activity evaluation of thiazolidinones containing alkynyl and alkenyl furans for disrupting protein-protein interactions between HIF-1α and p300>, Reference of 10574-69-3, the main research area is thiazolidinone furanylidene preparation HIF1alpha p300 interaction inhibitor.

Based on the structure of the potent hypoxia-inducible factor (HIF) inhibitor, a novel series of furanylidene thiazolidinones I (R1 = trimethylsilylethynyl, triethylsilylethynyl, cyclopropylethynyl, etc.; R2 = C6H5,CH2NMe2, CH2C6H5, etc.) were designed and synthesized using Sonogashira or Suzuki-Miyaura cross-couplings, and subsequent Knoevenagel condensation. In particular, derivatives I (R1 = trimethylsilylethynyl, t-butylethynyl, cyclopropylethynyl, t-butylethenyl, cyclopropylethenyl; R2 = C6H5,CH2(4-methylpiperazin-1-yl)) bearing an alkynyl or alkenyl group on the furan ring, exhibited four- to five-fold higher activities than II. These potent compounds will serve as leads for the development of novel small mols. for targeting the HIF-1α/p300 complex.

Heterocycles published new progress about Alkynes, α- Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Reference of 10574-69-3.

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

Nitsche, Christoph; Schreier, Verena N.; Behnam, Mira A. M.; Kumar, Anil; Bartenschlager, Ralf; Klein, Christian D. published the artcile< Thiazolidinone-Peptide Hybrids as Dengue Virus Protease Inhibitors with Antiviral Activity in Cell Culture>, Application of C10H9NOS2, the main research area is thiazolidindione rhodanine peptide preparation antiviral dengue virus protease inhibitor.

The protease of dengue virus is a promising target for antiviral drug discovery. We here report a new generation of peptide-hybrid inhibitors of dengue protease that incorporate N-substituted 5-arylidenethiazolidinone heterocycles (rhodanines and thiazolidinediones) as N-terminal capping groups of the peptide moiety. The compounds were extensively characterized with respect to inhibition of various proteases, inhibition mechanisms, membrane permeability, antiviral activity, and cytotoxicity in cell culture. A sulfur/oxygen exchange in position 2 of the capping heterocycle (thiazolidinedione-capped vs rhodanine-capped peptide hybrids) has a significant effect on these properties and activities. The most promising in vitro affinities were observed for thiazolidinedione-based peptide hybrids containing hydrophobic groups with Ki values between 1.5 and 1.8 μM and competitive inhibition mechanisms. Rhodanine-capped peptide hybrids with hydrophobic substituents have, in correlation with their membrane permeability, a more pronounced antiviral activity in cell culture than the thiazolidinediones.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Application of C10H9NOS2.

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

Condon, F. E.; Shapiro, D.; Sulewski, P.; Vasi, I.; Waldman, R. published the artcile< Facile and uniform procedure for the large-scale preparation of some N-alkylrhodanines>, Synthetic Route of 10574-69-3, the main research area is rhodanine alkyl; chloroacetic acid thiocarbamate cyclization.

3-Methyl-, ethyl-, allyl-, and benzylrhodanine were prepared by treating the appropriate primary amine with CS2 in the presence of NH3 and the resulting ammonium alkyldithiocarbamate with ClCH2CO2H.

Organic Preparations and Procedures International published new progress about 10574-69-3. 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

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>, Quality Control of 10574-69-3, the main research area is rhodanine thiazolidinedione preparation green chem; amine primary carbon disulfide bromoacetate methyl three component reaction.

A synthesis of 3-substituted rhodanine and thiazolidine-2,4-dione derivatives I [X = S, O; R = CH2:CHCH2, CH3CH(CH3)CH2, 3,4-Cl2C6H3, etc.] starting from primary amines RNH2, carbon disulfide, and Me 2-bromoacetate, were described. The reaction proceeds successfully both in water and under solvent-free conditions, but 2-thioxothiazolidin-4-one (rhodanine) derivatives I (X = S) were obtained under solvent-free conditions, and thiazolidine-2,4-dions I (X = O) were formed when water was used as the solvent.

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, Quality Control of 10574-69-3.

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

Khiat, Manel; Zradni, Fatima-Zohra; Kasmi-Mir, Souad; Baeza, Alejandro published the artcile< Study of the electrochemical behavior of merocyanine and merocarbocyanine salts and their transformation into π-electron donor molecules, namely tetrathiatetraazafulvalenes>, Computed Properties of 10574-69-3, the main research area is tetrathiatetraazafulvalene electrochem preparation cyclic voltammetry voltammogram.

An electrochem. study using cyclic voltammetry method was carried out on some previously prepared merocyanines salts, namely thiazolideniumsulfonate salts and thiazolidenium chloride salts I [R = Ph, Bn; R1 = H, SMe; X = Cl, 4-methylbenzenesulfonate] and merocarbocyanines salts, namely alkylidenthiazolidenium sulfonate salt and alkylidenthiazolidenium chloride salt II [R = n-Pr]. These salts were transformed by dimerization in situ in a voltammetric cell into tetrathiatetraazafulvalenes (TTTAFs) such as III supposed to be π-electron donor mols. due to existing conjugation in their structure. The structure of all new chem. synthesized mols. was confirmed by IR, 1H-NMR, 13C-NMR, and MS. The transformation of salts into TTTAF was confirmed by a reversible voltammogram curve and variation of observed potentials.

Indonesian Journal of Chemistry published new progress about Charge transfer complexes Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Computed Properties of 10574-69-3.

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

Vydzhak, R. N.; Brovarets, V. S.; Pil’o, S. G.; Drach, B. S. published the artcile< Synthesis and Transformations of Two Types of 4-Phosphorylated Aldehydes of the Oxazole Series>, Name: 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is formylpiperidinyloxazolyl phosphonate preparation; formyloxazolyl phosphonate preparation; piperidinyl formyloxazolyl phosphonate preparation; morpholinyl formyloxazolyl phosphonate preparation; phosphonium oxothiazolylideneoxazolyl preparation; thiazolylhydrazonooxazolyl phosphonate preparation.

The reaction of 2,2-dichloro-N-(1,2,2,2-tetrachloroethyl)acetamide with trialkyl phosphites and triphenylphosphine gave [2,2-dichloro-1-[(dichloroacetyl)amino]ethenyl]triphenylphosphonium chloride and [2,2,2-trichloro-1-(dichloroacetyl)amino]phosphonic acid di-Me ester and [2,2,2-trichloro-1-(dichloroacetyl)amino]phosphonic acid di-Et ester. Cyclocondensation of the latter in the presence of amines gave [2-formyl-5-(1-piperidinyl)-4-oxazolyl]phosphonic acid di-Me ester (I), [2-formyl-5-(1-piperidinyl)-4-oxazolyl]phosphonic acid di-Et ester (II) and [2-formyl-5-(4-morpholinyl)-4-oxazolyl]phosphonic acid di-Me ester (III) and [2-formyl-5-(4-morpholinyl)-4-oxazolyl]phosphonic acid di-Et ester (IV). Their structure of products was determined by spectroscopy and also by chem. transformations into phenylhydrazones, thiosemicarbazones, aminals, and other functional derivatives of I-IV.

Russian Journal of General Chemistry (Translation of Zhurnal Obshchei Khimii) published new progress about Condensation reaction. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Name: 3-Benzyl-2-thioxothiazolidin-4-one.

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

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