Author: tianli

Zhao, Xin; Li, Runfeng; Zhou, Yang; Xiao, Mengjie; Ma, Chunlong; Yang, Zhongjin; Zeng, Shaogao; Du, Qiuling; Yang, Chunguang; Jiang, Haiming; Hu, Yanmei; Wang, Kefeng; Mok, Chris Ka Pun; Sun, Ping; Dong, Jianghong; Cui, Wei; Wang, Jun; Tu, Yaoquan; Yang, Zifeng; Hu, Wenhui published the artcile< Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses>, Electric Literature of 1003-32-3, the main research area is preparation antiviral pinanamine derivative resistant influenza A virus.

Influenza pandemic is a constant major threat to public health caused by influenza A viruses (IAVs). IAVs are subcategorized by the surface proteins hemagglutinin (HA) and neuraminidase (NA), in which they are both essential targets for drug discovery. While it is of great concern that NA inhibitor oseltamivir resistant strains are frequently identified from human or avian influenza virus, structural and functional characterization of influenza HA has raised hopes for new antiviral therapies. In this study, we explored a structure-activity relationship (SAR) of pinanamine-based antivirals and discovered a potent inhibitor M090 against amantadine-resistant viruses, including the 2009 H1N1 pandemic strains, and oseltamivir-resistant viruses. Mechanism of action studies, particularly hemolysis inhibition, indicated that M090 targets influenza HA and it occupied a highly conserved pocket of the HA2 domain and inhibited virus-mediated membrane fusion by “”locking”” the bending state of HA2 during the conformational rearrangement process. This work provides new binding sites within the HA protein and indicates that this pocket may be a promising target for broad-spectrum anti-influenza A drug design and development.

Journal of Medicinal Chemistrypublished new progress about Antiviral agent resistance. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Electric Literature of 1003-32-3.

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

Valente, Sergio; Mellini, Paolo; Spallotta, Francesco; Carafa, Vincenzo; Nebbioso, Angela; Polletta, Lucia; Carnevale, Ilaria; Saladini, Serena; Trisciuoglio, Daniela; Gabellini, Chiara; Tardugno, Maria; Zwergel, Clemens; Cencioni, Chiara; Atlante, Sandra; Moniot, Sebastien; Steegborn, Clemens; Budriesi, Roberta; Tafani, Marco; Del Bufalo, Donatella; Altucci, Lucia; Gaetano, Carlo; Mai, Antonello published the artcile< 1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells>, Safety of Thiazole-5-carboxyaldehyde, the main research area is preparation dihydropyridine sirtuin AMPK antitumor neoplasm.

Modulators of sirtuins are considered promising therapeutic targets for the treatment of cancer, cardiovascular, metabolic, inflammatory, and neurodegenerative diseases. Here we prepared new 1,4-dihydropyridines (DHPs) bearing changes at the C2/C6, C3/C5, C4, or N1 position. Tested with the SIRTainty procedure, some of them displayed increased SIRT1 activation with respect to the prototype 3a, high NO release in HaCat cells, and ameliorated skin repair in a mouse model of wound healing. In C2C12 myoblasts, two of them improved mitochondrial d. and functions. All the effects were reverted by coadministration of compound C (9), an AMPK inhibitor, or of EX-527 (10), a SIRT1 inhibitor, highlighting the involvement of the SIRT1/AMPK pathway in the action of DHPs. Finally, tested in a panel of cancer cells, the water-soluble form of 3a, compound 8, displayed antiproliferative effects in the range of 8-35 μM and increased H4K16 deacetylation, suggesting a possible role for SIRT1 activators in cancer therapy.

Journal of Medicinal Chemistrypublished new progress about Antitumor agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Safety of Thiazole-5-carboxyaldehyde.

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

Lu, Cuifen; Nie, Junqi; Yang, Guichun; Chen, Zuxing published the artcile< An improved synthesis of sitophilure>, SDS of cas: 171877-39-7, the main research area is asym synthesis sitophilure aldol reaction chiral auxiliary.

The asym. synthesis of sitophilure (I) was carried out in 8 steps, with 42% overall yield and 97% enantiomeric excess from propionaldehyde. The synthesis relied on an approach employing an asym. acyl-thiazolidinethione propionate aldol reaction to establish two stereogenic centers.

Canadian Journal of Chemistrypublished new progress about Aldol condensation, stereoselective. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, SDS of cas: 171877-39-7.

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

Pena, S.; Fagundez, C.; Medeiros, A.; Comini, M.; Scarone, L.; Sellanes, D.; Manta, E.; Tulla-Puche, J.; Albericio, F.; Stewart, L.; Yardley, V.; Serra, G. published the artcile< Synthesis of cyclohexapeptides as antimalarial and anti-trypanosomal agents>, Formula: C12H18N2O4S, the main research area is cyclohexa peptide synthesis antimalarial antitrypanosomal agent structure activity; solid phase peptide synthesis macrocyclization.

Cyclohexapeptide analogs of natural products were obtained in very good yields by a combination of solid-phase peptide synthesis, for the linear peptide, and solution cyclization. The activities against Plasmodium falciparum K1, Trypanosoma brucei brucei and murine macrophages (cell line J774) of these novel compounds and azolic macrocycles, previously reported by us, were evaluated. Seven macrocycles showed submicromolar activities against Plasmodium falciparum K1 and a high selectivity (SI > 125) for the parasite. In addition, two compounds displayed one digit micromolar EC50 against T. brucei brucei and satisfactory selectivity (SI 82 and 95). Preliminary structure-activity relationships are presented.

MedChemCommpublished new progress about Antimalarials. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Formula: C12H18N2O4S.

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

Liu, Gui-Chun; Dong, Zhi-Wei; Hou, Qing-Bai; He, Jin-Wu; Zhao, Ruo-Ping; Wang, Wen; Li, Xue-Yan published the artcile< Second Rhagophthalmid Luciferase Cloned from Chinese Glow-worm Menghuoius giganteus (Rhagophthalmidae: Elateroidea)>, Quality Control of 2591-17-5, the main research area is sequence luciferase mol cloning Rhagophthalmus Menghuoius.

The pH-insensitive beetle luciferases cloned from Rhagophthalmidae, Phengodidae, and Elateridae exhibit great potential application as reporter assays for monitoring gene expression. At present, however, only one luciferase has been reported from the enigmatic and predominantly Asian distributed luminous family Rhagophthalmidae. Here, we cloned the second rhagophthalmid luciferase from the Chinese glow-worm Menghuoius giganteus (Rhagophthalmidae: Elateroidea) by combining reverse transcription polymerase chain reaction (RT-PCR) with rapid amplification of complementary DNA ends (RACE). The luciferase consisted of 546 amino acids and showed high identity to that of Rhagophthalmus ohbai (90.4%). The recombinant M. giganteus luciferase was produced in vitro and exhibited significant bioluminescent activity under neutral conditions (pH 7.8), with low KM for D-luciferin (2.2μM) and ATP (53μM). Activity was highest at 10°C and inactivation occurred at 45°C. This luciferase showed pH-insensitivity and maximum emission spectrum at 560 nm. Phylogenetic analyses based on the deduced amino acids indicated a close relationship between the M. giganteus luciferase and that of R. ohbai. These results increase our understanding of rhagophthalmid luciferases and provide a new resource for the application of luciferases.

Photochemistry and Photobiologypublished new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Quality Control of 2591-17-5.

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

Pan, Qingqing; Deng, Xin; Gao, Wenxia; Chang, Jing; Pu, Yuji; He, Bin published the artcile< ROS triggered cleavage of thioketal moiety to dissociate prodrug nanoparticles for chemotherapy>, Application In Synthesis of 96-53-7, the main research area is cancer doxorubicin PEG nanoparticle delivery ROS; Cancer therapy; Dissociation; Prodrug nanoparticle; ROS-responsive; Thioketal.

With the utilization of high concentration reactive oxygen species (ROS) in tumor microenvironment, PEG-doxorubicin (PEG-DOX) prodrug was synthesized via a thioketal moiety as the linker, which was ROS cleavable to trigger DOX release from the self-assembled prodrug nanoparticles. The in vitro ROS sensitivity of prodrug nanoparticles (NPs) was investigated in Fenton agent and H2O2, and the disassembly of NPs was more sensitive to Fenton reagent. After internalized in HepG2 cells via endocytosis, the cellular ROS consuming test revealed intracellular DOX release. The pharmacokinetics and biodistribution study demonstrated that the in vivo elimination of NPs was significantly improved and the NPs were passively targeted to tumor tissues via EPR effect. The ROS-responsive prodrug NPs exhibited excellent antitumor activity in HepG2 tumor-bearing nude mice, remarkably induced tumor cells apoptosis and reduced the systemic toxicity of DOX. Our study revealed the ROS responsive prodrug nanoparticle is an effective strategy to fabricate nanomedicine for cancer chemotherapy.

Colloids and Surfaces, B: Biointerfacespublished new progress about Aggregation. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Application In Synthesis of 96-53-7.

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

Chen, Ning; Jia, Weiyi; Xu, Jiaxi published the artcile< A Versatile Synthesis of Various Substituted Taurines from Vicinal Amino Alcohols and Aziridines>, Reference of 171877-39-7, the main research area is taurine substituted preparation amino alc aziridine carbon disulfide; oxidation thiazolidinethione.

Taurine and structurally diverse substituted taurines have been synthesized by peroxyformic acid oxidation of the thiazolidine-2-thione intermediates generated from vicinal amino alcs. or aziridines and carbon disulfide. The stereochem. and mechanisms of the reactions are discussed. The method is a salt-free and versatile route, convenient in terms of purification, and can be used to synthesize optically active substituted taurines. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009).

European Journal of Organic Chemistrypublished 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, Reference of 171877-39-7.

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

Crimmins, Michael T.; Christie, Hamish S.; Hughes, Colin O. published the artcile< Synthesis and diastereoselective aldol reactions of a thiazolidinethione chiral auxiliary>, Name: (S)-4-Benzylthiazolidine-2-thione, the main research area is thiazolidinethione chiral auxiliary; propanoyl thiazolidinethione syn aldol.

Thiazolidinethione chiral auxiliary I (R = H) is prepared from (S)-phenylalaninol and carbon disulfide. Propanoylated I [R = C(O)CH2CH3] can be used for either Evans syn aldol reactions or non-Evans syn aldol reactions with a variety of aldehydes, in good yield with good stereoselectivity.

Organic Synthesespublished new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Name: (S)-4-Benzylthiazolidine-2-thione.

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