Category: 10574-69-3

Robertson, Mark J.; Hadzic, Gordana; Ambrus, Joseph; Pome, D. Yuri; Hyde, Emily; Whiting, Ainslie; Mariana, Anna; von Kleist, Lisa; Chau, Ngoc; Haucke, Volker; Robinson, Phillip J.; McCluskey, Adam published the artcile< The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity>, Related Products of 10574-69-3, the main research area is dynamin GTPase inhibitor rhodanine analog preparation SAR; Knoevengal condensation; dynamin inhibition; rhodanine.

Six focused rhodanine-based libraries, 60 compounds in total, were synthesized and evaluated as potential dynamin I GTPase inhibitors. Twenty-six were more potent than the lead compound with 13 returning IC50 values ≤10 μM, making the Rhodadyn series among the most active dynamin inhibitors reported. Two analogs were highly effective at blocking receptor-mediated endocytosis: C10 and D10 (I) with IC50(RME) = 7.0 ± 2.2 and 5.9 ± 1.0 μM, resp. These compounds are equipotent with the best reported in-cell dynamin inhibitors.

ACS Medicinal Chemistry Letters published new progress about Drug targets (endocytosis). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Related Products of 10574-69-3.

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

Powers, Jay P.; Piper, Derek E.; Li, Yang; Mayorga, Veronica; Anzola, John; Chen, James M.; Jaen, Juan C.; Lee, Gary; Liu, Jinqian; Peterson, M. Greg; Tonn, George R.; Ye, Qiuping; Walker, Nigel P. C.; Wang, Zhulun published the artcile< SAR and Mode of Action of Novel Non-Nucleoside Inhibitors of Hepatitis C NS5b RNA Polymerase>, Related Products of 10574-69-3, the main research area is nonnucleoside inhibitor thioxothiazolidine aryl derivative hepatitis C NS5b polymerase.

Novel non-nucleoside inhibitors of the HCV RNA polymerase (NS5b) with sub-micromolar biochem. potency have been identified which are selective for the inhibition of HCV NS5b over other polymerases. The structures of the complexes formed between several of these inhibitors and HCV NS5b were determined by x-ray crystallog., and the inhibitors were found to bind in an allosteric binding site sep. from the active site. Structure-activity relationships and structural studies have identified the mechanism of action for compounds in this series, several of which possess drug-like properties, as unique, reversible, covalent inhibitors of HCV NS5b.

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

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

He, Xiao-Yang; Zou, Peng; Qiu, Jiayin; Hou, Ling; Jiang, Shibo; Liu, Shuwen; Xie, Lan published the artcile< Design, synthesis and biological evaluation of 3-substituted 2,5-dimethyl-N-(3-(1H-tetrazol-5-yl)phenyl)pyrroles as novel potential HIV-1 gp41 inhibitors>, SDS of cas: 10574-69-3, the main research area is gp41 inhibitor HIV 1 antiviral tetrazolylphenylpyrrole preparation; pyrrole tetrazolylphenyl preparation gp41 inhibitor HIV 1 antiviral.

Based on the structure of HIV-1 gp41 binding site for small-mol. inhibitors, optimization of a lead compound resulted in the discovery of a new series of 2,5-dimethyl-3-(5-(N-phenylrhodaninyl)methylene)-N-(3-(1H-tetrazol-5-yl)phenyl)pyrrole compounds with improved anti-HIV-1 activity. The two most active compounds exhibited significant potency against gp41 6-HB formation with IC50 values of 4.4 and 4.6 μM and against HIV-1 replication in the MT-2 cells with EC50 values of 3.2 and 2.2 μM, resp., thus providing a new starting point to develop highly potent small-mol. HIV fusion inhibitors targeting gp41.

Bioorganic & Medicinal Chemistry published new progress about AIDS (disease). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, SDS of cas: 10574-69-3.

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

Robertson, Mark J.; Hadzic, Gordana; Ambrus, Joseph; Pome, D. Yuri; Hyde, Emily; Whiting, Ainslie; Mariana, Anna; von Kleist, Lisa; Chau, Ngoc; Haucke, Volker; Robinson, Phillip J.; McCluskey, Adam published the artcile< The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity>, SDS of cas: 10574-69-3, the main research area is dynamin GTPase inhibitor rhodanine analog preparation SAR; Knoevengal condensation; dynamin inhibition; rhodanine.

Six focused rhodanine-based libraries, 60 compounds in total, were synthesized and evaluated as potential dynamin I GTPase inhibitors. Twenty-six were more potent than the lead compound with 13 returning IC50 values ≤10 μM, making the Rhodadyn series among the most active dynamin inhibitors reported. Two analogs were highly effective at blocking receptor-mediated endocytosis: C10 and D10 (I) with IC50(RME) = 7.0 ± 2.2 and 5.9 ± 1.0 μM, resp. These compounds are equipotent with the best reported in-cell dynamin inhibitors.

ACS Medicinal Chemistry Letters published new progress about Drug targets (endocytosis). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, SDS of cas: 10574-69-3.

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

Powers, Jay P.; Piper, Derek E.; Li, Yang; Mayorga, Veronica; Anzola, John; Chen, James M.; Jaen, Juan C.; Lee, Gary; Liu, Jinqian; Peterson, M. Greg; Tonn, George R.; Ye, Qiuping; Walker, Nigel P. C.; Wang, Zhulun published the artcile< SAR and Mode of Action of Novel Non-Nucleoside Inhibitors of Hepatitis C NS5b RNA Polymerase>, COA of Formula: C10H9NOS2, the main research area is nonnucleoside inhibitor thioxothiazolidine aryl derivative hepatitis C NS5b polymerase.

Novel non-nucleoside inhibitors of the HCV RNA polymerase (NS5b) with sub-micromolar biochem. potency have been identified which are selective for the inhibition of HCV NS5b over other polymerases. The structures of the complexes formed between several of these inhibitors and HCV NS5b were determined by x-ray crystallog., and the inhibitors were found to bind in an allosteric binding site sep. from the active site. Structure-activity relationships and structural studies have identified the mechanism of action for compounds in this series, several of which possess drug-like properties, as unique, reversible, covalent inhibitors of HCV NS5b.

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

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

He, Xiao-Yang; Zou, Peng; Qiu, Jiayin; Hou, Ling; Jiang, Shibo; Liu, Shuwen; Xie, Lan published the artcile< Design, synthesis and biological evaluation of 3-substituted 2,5-dimethyl-N-(3-(1H-tetrazol-5-yl)phenyl)pyrroles as novel potential HIV-1 gp41 inhibitors>, Product Details of C10H9NOS2, the main research area is gp41 inhibitor HIV 1 antiviral tetrazolylphenylpyrrole preparation; pyrrole tetrazolylphenyl preparation gp41 inhibitor HIV 1 antiviral.

Based on the structure of HIV-1 gp41 binding site for small-mol. inhibitors, optimization of a lead compound resulted in the discovery of a new series of 2,5-dimethyl-3-(5-(N-phenylrhodaninyl)methylene)-N-(3-(1H-tetrazol-5-yl)phenyl)pyrrole compounds with improved anti-HIV-1 activity. The two most active compounds exhibited significant potency against gp41 6-HB formation with IC50 values of 4.4 and 4.6 μM and against HIV-1 replication in the MT-2 cells with EC50 values of 3.2 and 2.2 μM, resp., thus providing a new starting point to develop highly potent small-mol. HIV fusion inhibitors targeting gp41.

Bioorganic & Medicinal Chemistry published new progress about AIDS (disease). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Product Details of C10H9NOS2.

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; 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 Engineeringpublished 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

Singh, Sarangthem Joychandra; Devi, Nepram Sushuma published the artcile< Diacetoxyiodobenzene mediated oxidative dethionation of N-substituted 5-arylmethylidene rhodanines: an efficient synthesis of N-substituted 5-arylmethylidene thiazolidine-2,4-diones>, Recommanded Product: 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is arylmethylidene thiazolidine dione preparation; rhodanine arylmethylidene oxidative dethionation.

A simple and efficient synthesis of N-substituted-5-arylmethylidene thiazolidine-2,4-diones I (R1 = Ph, 2-fluorophenyl, 4-methoxyphenyl, 2-furyl, etc.; R2 = CH3, C6H5CH2, CH2=CHCH2; X = S) has been developed via oxidative dethionation of N-substituted-5-arylmethylidene rhodanines I (R1 = Ph, 2-fluorophenyl, 4-methoxyphenyl, 2-furyl, etc.; R2 = CH3, C6H5CH2, CH2=CHCH2; X = O) using diacetoxyiodobenzene (DIB) in ethanol at room temperature This protocol is simple, mild and column free, and obviates the need of acids and bases, and offers a broad substrate scope.

ARKIVOC (Gainesville, FL, United States)published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Recommanded Product: 3-Benzyl-2-thioxothiazolidin-4-one.

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

Moghimi, S.; Heravi, M. M.; Oskooie, H. A.; Beheshtiha, Y. S. published the artcile< A novel un-catalyzed and solvent-free method for the synthesis of 2-thioxothiazolidin-4-ones>, Application of C10H9NOS2, the main research area is rhodanine preparation catalyst solvent free; primary amine carbon disulfide chloroacetyl chloride multicomponent re??action.

An easy and highly efficient one-pot, three-component synthesis of rhodanines was reported. The reaction of primary amines, carbon disulfide and chloroacetyl chloride proceeded in the absence of solvent and catalyst affording 2-thioxothiazolidin-4-ones in good to excellent yields.

Scientia Iranica, Transaction C: Chemistry, Chemical Engineeringpublished new progress about Primary amines Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Application of C10H9NOS2.

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>, HPLC of Formula: 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 Chemistrypublished 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, HPLC of Formula: 10574-69-3.

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