Day: October 13, 2022

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

Bold, Guido; Faessler, Alexander; Capraro, Hans-Georg; Cozens, Robert; Klimkait, Thomas; Lazdins, Janis; Mestan, Juergen; Poncioni, Bernard; Roesel, Johannes; Stover, David; Tintelnot-Blomley, Marina; Acemoglu, Figan; Beck, Werner; Boss, Eugen; Eschbach, Martin; Huerlimann, Thomas; Masso, Elvira; Roussel, Serge; Ucci-Stoll, Katharina; Wyss, Dominique; Lang, Marc published the artcile< New Aza-Dipeptide Analogs as Potent and Orally Absorbed HIV-1 Protease Inhibitors: Candidates for Clinical Development>, Formula: C10H7NOS, the main research area is human immunodeficiency virus protease inhibitor azapeptide; azadipeptide analog preparation HIV protease inhibitor; azapeptide analog preparation antiviral.

On the basis of previously described X-ray studies of an enzyme/aza-dipeptide complex, aza-dipeptide analogs, e.g. I (R1 = Ph, pyrid-2-yl, thiazol-2-yl, thiazol-5-yl, diethylamino, 2-methyl-2H-tetrazol-5-yl, 2-tert-butyl-2H-tetrazole-5-yl; R2, R3 = iso-Pr, sec-Bu, tert-Bu; R4 = MeO, EtO) carrying N-(bis-aryl-methyl) substituents on the (hydroxyethyl)hydrazine moiety have been designed and synthesized as HIV-1 protease inhibitors. By using either equally or orthogonally protected dipeptide isosteres, sym. and asym. acylated aza-dipeptides can be synthesized. This approach led to the discovery of very potent inhibitors with antiviral activities (ED50) in the subnanomolar range. Acylation of the (hydroxyethyl)hydrazine dipeptide isostere with N-(methoxycarbonyl)-L-tert-leucine increased the oral bioavailability significantly when compared to the corresponding L-valine or L-isoleucine derivatives The bis(L-tert-leucine) derivatives I (R1 = Ph (CGP 75355), pyrid-2-yl (CGP 73547), thiazol-2-yl (CGP 75136), 2-methyl-2H-tetrazol-5-yl (CGP 75176); R2 = R3 = tert-butyl; R4 = OMe) combine excellent antiviral activity with high blood concentration after oral administration. Furthermore, they show no cross-resistance with saquinavir-resistant strains and maintain activity against indinavir-resistant ones. Consequently they qualify for further profiling as potential clin. candidates.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 198904-53-9 belongs to class thiazole, and the molecular formula is C10H7NOS, Formula: C10H7NOS.

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

Andrade, Carlos Kleber Z.; Rocha, Rafael O.; Vercillo, Otilie E.; Silva, Wender A.; Matos, Ricardo Alexandre F. published the artcile< DCC/DMAP-mediated coupling of carboxylic acids with oxazolidinones and thiazolidinethiones>, Computed Properties of 171877-39-7, the main research area is DCC DMAP mediated coupling carboxylic acid oxazolidinone thiazolidinethione; acylation oxazolidinone thiazolidinethione DMAP catalyst dicyclohexylcarbodiimide reagent.

Dicyclohexylcarbodiimide and catalytic dimethylaminopyridine were successfully used in the coupling of carboxylic acids with oxazolidinones and thiazolidinethiones. The acylated products were obtained in good yields.

Synlett published new progress about Acylation. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Computed Properties of 171877-39-7.

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

Calabretta, Maria Maddalena; Alvarez-Diduk, Ruslan; Michelini, Elisa; Roda, Aldo; Merkoci, Arben published the artcile< Nano-lantern on paper for smartphone-based ATP detection>, Quality Control of 2591-17-5, the main research area is adenosine triphosphate biosensor smartphone paper urinary tract infection; ATP biosensor; Bioluminescence; Luciferase; Paper-based biosensor; Smartphone.

ATP-driven bioluminescence relying on the D-luciferin-luciferase reaction is widely employed for several biosensing applications where bacterial ATP detection allows to verify microbial contamination for hygiene monitoring in hospitals, food processing and in general for cell viability studies. Several ATP kit assays are already com. available but an user-friendly ATP biosensor characterized by low-cost, portability, and adequate sensitivity would be highly valuable for rapid and facile on site screening. Thanks to an innovative freeze-drying procedure, we developed a user-friendly, ready-to-use and stable ATP sensing paper biosensor that can be combined with smartphone detection. The ATP sensing paper includes a lyophilized “”nano-lantern”” with reaction components being rapidly reconstituted by 10μL sample addition, enabling detection of 10-14 mol of ATP within 10 min. We analyzed urinary microbial ATP as a biomarker of urinary tract infection (UTI), confirming the capability of the ATP sensing paper to detect the threshold for positivity corresponding to 105 colony-forming units of bacteria per mL of urine.

Biosensors & Bioelectronics published new progress about Bioluminescence. 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

Tapadar, Subhasish; He, Rong; Luchini, Doris N.; Billadeau, Daniel D.; Kozikowski, Alan P. published the artcile< Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: Effects on HDAC biology and antiproliferative activity>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is histone deacetylase inhibitor preparation isoxazole moiety linker antitumor.

A series of hydroxamic acid based histone deacetylase inhibitors 6-15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in the HDAC isoform inhibitory assay and exhibited micromolar inhibitory activity against five pancreatic cancer cell lines.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole.

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

Van Zyl, Winschau F.; Deane, Shelly M.; Dicks, Leon M. T. published the artcile< In vivo bioluminescence imaging of the spatial and temporal colonization of lactobacillus plantarum 423 and enterococcus mundtii ST4SA in the intestinal tract of mice>, Formula: C11H7KN2O3S2, the main research area is intestinal tract Lactobacillus Enterococcus spatial temporal colonization bioluminescence imaging; Colonization; Enterococcus mundtii ST4SA; Gastrointestinal tract; In vivo bioluminescence imaging; Intestinal persistence; Lactic acid bacteria; Lactobacillus plantarum 423; Luciferase.

Background: Lactic acid bacteria (LAB) are major inhabitants and part of the normal microflora of the gastrointestinal tract (GIT) of humans and animals. Despite substantial evidence supporting the beneficial properties of LAB, only a few studies have addressed the migration and colonization of probiotic bacteria in the GIT. The reason for this is mostly due to the limitations, or lack of, efficient reporter systems. Here we describe the development and application of a non-invasive in vivo bioluminescence reporter system to study, in real-time, the spatial and temporal persistence of Lactobacillus plantarum 423 and Enterococcus mundtii ST4SA in the intestinal tract of mice. Results: This study reports on the application of the firefly luciferase gene (ffluc) from Photinus pyralis to develop luciferase-expressing L. plantarum 423 and E. mundtii ST4SA, using a Lactococcus lactis NICE system on a high copy number plasmid (pNZ8048) and strong constitutive lactate dehydrogenase gene promoters (Pldh and STldh). The reporter system was used for in vivo and ex vivo monitoring of both probiotic LAB strains in the GIT of mice after single and multiple oral administrations. Enterococcus mundtii ST4SA reached the large intestine 45 min after gavage, while L. plantarum 423 reached the cecum/colon after 90 min. Both strains predominantly colonized the cecum and colon after five consecutive daily administrations. Enterococcus mundtii ST4SA persisted in feces at higher numbers and for more days compared to L. plantarum 423. Conclusions: Our findings demonstrate the efficiency of a high-copy number vector, constitutive promoters and bioluminescence imaging to study the colonization and persistence of L. plantarum 423 and E. mundtii ST4SA in the murine GIT. The system allowed us to differentiate between intestinal transit times of the two strains in the digestive tract. This is the first report of bioluminescence imaging of a luciferase-expressing E. mundtii strain to study colonization dynamics in the murine model. The bioluminescence system developed in this study may be used to study the in vivo colonization dynamics of other probiotic LAB.

BMC Microbiology published new progress about Bioluminescent imaging. 115144-35-9 belongs to class thiazole, and the molecular formula is C11H7KN2O3S2, Formula: C11H7KN2O3S2.

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

Wang, Rui; Xu, Hongyan; Zhang, Ying; Hu, Yuntao; Wei, Yingsu; Du, Xiao; Zhao, Huaiqing published the artcile< Ag-Cu copromoted direct C2-H bond thiolation of azoles with Bunte salts as sulfur sources>, Quality Control of 1003-32-3, the main research area is thiazole benzothiazole benzoxazole benzimidazole arylthio alkylthio preparation; azole Bunte salt silver copper catalyst thiolation.

A direct C2-H thiolation of azoles with Bunte salts was achieved under the combined action of copper and silver salts. This protocol could furnish various substituted 2-arylthio- or 2-alkylthio-substituted azoles in moderate to good yields. This method has a broad substrate scope and shows good functional group tolerance.

Organic & Biomolecular Chemistry published new progress about Benzimidazoles Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Quality Control of 1003-32-3.

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

Reshi, Noor U. Din; Kathuria, Lakshay; Samuelson, Ashoka G. published the artcile< Chemoselective Reduction of Imines Catalyzed by Ruthenium(II) Half-Sandwich Complexes: A Mechanistic Study>, Product Details of C10H11NS2, the main research area is reduction imine hydrosilane ruthenium catalyst mechanism preparation amine; ruthenium cymene half sandwich catalyst hydrosilane reduction imine; potential energy surface reduction imine hydrosilane ruthenium catalyst.

Ruthenium half-sandwich complexes ligated to chiral 2-oxazolidinethiones or 2-thiazolidinethiones have been examined in the reduction of N-benzylideneaniline using silyl hydrides as reductants. The chemoselective reduction of imines takes place under mild conditions to afford the corresponding amines in nearly quant. yield. Mechanistic studies indicate that dissociation of the ancillary ligands generate the active catalyst in all the complexes studied, which is the same species generated by [Ru(p-cymene)(Cl)2]2 under the reaction conditions. This results in the formation of a single catalytic species irresp. of the starting half-sandwich complex. Detailed mechanistic studies involving trapping of intermediates, in situ studies using mass spectrometry and NMR spectroscopy were carried out using the active catalyst generated by [Ru(p-cymene)(Cl)2]2. The mechanism of the reaction is dependent on the number of the hydrogen atoms in the reducing silane. The reaction proceeds via Gade-Hoffman pathway or Zheng-Chan pathway when a dihydro or trihydrosilane is the reductant. However, the use of a monohydrosilane, leads to longer reaction times presumably due to a change in the reaction pathway.

European Journal of Inorganic Chemistry published new progress about Amines Role: SPN (Synthetic Preparation), PREP (Preparation). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Product Details of C10H11NS2.

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

Curreli, Francesca; Ahmed, Shahad; Benedict Victor, Sofia M.; Iusupov, Ildar R.; Belov, Dmitry S.; Markov, Pavel O.; Kurkin, Alexander V.; Altieri, Andrea; Debnath, Asim K. published the artcile< Preclinical optimization of gp120 entry-antagonists as anti-HIV-1 agents with improved cytotoxicity and ADME properties through rational design, synthesis, and antiviral evaluation>, Formula: C4H3NOS, the main research area is pyrrolecarboxamide aryl heteroaryl thiazolyl aminoalkyl preparation antiHIV pharmacokinetics cytotoxicity.

To optimize the structure of previously reported HIV-1 gp120 antagonist NBD-14189 which showed antiviral activity against HIV-1HXB2 (IC50 = 89 nM) but had high cytotoxicity and poor aqueous solubility, a series of novel azaarenyl analogs I [R1 = H, HOCH2, HOCH2CHOH, etc.; R2 = H, HOCH2, HOCH2CHOH; R3, R4, R5 = R6 = H, Me; R7 = 5-chloro-2-pyridinyl, 6-trifluoromethyl-3-pyridazinyl, 5-chloro-2-pyrimidinyl, etc.] have been synthesized and evaluated. One of the new analogs, the compound (S)-I [R1 = H; R2 = HOCH2; R3 = R4 = R5 = H; R6 = Me; R7 = 5-trifluoromethyl-2-pyridinyl; NBD-14270] showed a marked improvement in cytotoxicity, with a 3-fold and 58-fold improvements in SI values compared with that of NBD-14189 and NBD-11021, resp. Furthermore, the in-vitro ADME data clearly showed improvements in aqueous solubility and other properties compared with those for NBD-14189.

Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Formula: C4H3NOS.

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

Saputra, Elizabeth P.; Trzeciakowski, Jerome P.; Hyde, Jenny A. published the artcile< Borrelia burgdorferi spatiotemporal regulation of transcriptional regulator bosR and decorin binding protein during murine infection>, Related Products of 2591-17-5, the main research area is Borrelia burgdorferi bosR decorin binding protein murine infection.

Lyme disease, caused by Borrelia burgdorferi, is an inflammatory multistage infection, consisting of localized, disseminated, and persistent disease stages, impacting several organ systems through poorly defined gene regulation mechanisms. The purpose of this study is to further characterize the spatiotemporal transcriptional regulation of B. burgdorferi during mammalian infection of borrelial oxidative stress regulator (bosR) and decorin binding protein (dbpBA) by utilizing bioluminescent B. burgdorferi reporter strains and in vivo imaging. Fluctuating borrelial load was also monitored and used for normalization to evaluate expression levels. BosR transcription is driven by two promoters, Pbb0648 and PbosR, and we focused on the native promoter. BosR expression is low relative to the robustly expressed dbpBA throughout infection. In distal tissues, bosR was the highest in the heart during in the first week whereas dbpBA was readily detectable at all time points with each tissue displaying a distinct expression pattern. This data suggests bosR may have a role in heart colonization and the induction of dbpBA indicates a RpoS independent transcriptional regulation occurring in the mammalian cycle of pathogenesis. These finding demonstrate that B. burgdorferi engages unknown genetic mechanisms to uniquely respond to mammalian tissue environments and/or changing host response over time.

Scientific Reports published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Related Products of 2591-17-5.

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