Author: tianli

Yan, Gang; Hao, Lina; Niu, Yan; Huang, Wenjie; Wang, Wei; Xu, Fengrong; Liang, Lei; Wang, Chao; Jin, Hongwei; Xu, Ping published the artcile< 2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies>, Application In Synthesis of 57493-24-0, the main research area is thiazolyl imidazolyl acetamide preparation mol docking BACE1 inhibitor human; Alzheimer’s disease; BACE-1 inhibitors; BBB; Docking study; PAMPA; Permeability; Surface Plasmon Resonance (SPR).

In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives, I (R1 = Ph, 4-MeC6H4, 2-O2NC6H4, etc.; R2 = 2-MeOC6H4,3-MeOC6H4, 4-MeOC6H4, 3-EtOC6H4), II (R3 = Ph, 3,5-Cl2-4-NH2Ph; R4 = 3-MeOPh, 3-EtOPh), were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biol. evaluated in vitro. In addition, the selected compounds were tested with affinity (KD) towards BACE-1, blood brain barrier (BBB) permeability and cytotoxicity. The studies revealed that the most potent analog II (R3 = Ph; R4 = 3-EtOC6H4) (IC50 = 4.6 μM) with high predicted BBB permeability and low cellular cytotoxicity, could serve as a good lead structure for further optimization.

European Journal of Medicinal Chemistry published new progress about Alzheimer disease. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application In Synthesis of 57493-24-0.

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>, Category: thiazole, 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 Syntheses published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Category: thiazole.

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

Shrestha, Tej B.; Basel, Matthew T. published the artcile< Using Naturally Occurring Bioluminescent Enzymes to Track Specific Cell Populations>, SDS of cas: 2591-17-5, the main research area is review natural bioluminescent enzyme cell population tracking; Bioluminescence; Luminol; Myeloperoxidase; NADPH oxidase; Neutrophil.

A review. Luminol-based bioluminescence imaging allows noninvasive tracking of oxidatively active cells such as neutrophils. Luminol is given i.v. or i.p., followed by bioluminescence imaging at 425 nm. Here we describe a method for tracking neutrophil extravasation into an inflammatory site, especially focusing on mammary carcinoma.

Methods in Molecular Biology (New York, NY, United States) published new progress about Bioluminescent imaging. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, SDS of cas: 2591-17-5.

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

Rezania, Hamidreza published the artcile< Synthesis and characterization of novel functional hyperbranched polyamides from AB2 units: effect of extra functional groups>, Name: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is hyperbranched polyamide preparation thermal property; Novel AB2 monomers; functional groups; hyperbranched polymers; polyamide.

Hyperbranched polymers (HPs), which in terms of structure may be compared to the branching structure of trees, are referred to as tree-like materials, but role of leave in these tree-like polymers is neglected and much attention has only been paid to their branches. In fact, functional groups in these polymers play a vital role the same as the role of leaves in trees. Therefore, in this paper, an attempt has been made to design and synthesize three AB2 monomers containing extra hydroxyl and nitro groups. The benefits of their presence in the structure of produced hyperbranched polyamides (HPs) are investigated. The polymer structure was characterized by FT-IR and 1 H NMR. The solubility of synthesized HPs was studied in different protic and aprotic solvents. The thermal stability of the prepared HPs was investigated by thermogravimetric and differential scanning calorimetric analyses. The photoluminescent properties of the HPs were also investigated.

Designed Monomers and Polymers published new progress about Branched polymers Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Name: 2-Amino-4-(3-nitrophenyl)thiazole.

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

Qi, Qingqing; Shen, Qilong; Lu, Long published the artcile< Polyfluoroalkylation of 2-aminothiazoles>, Product Details of C9H7N3O2S, the main research area is thiazolamine polyfluoroalkylation.

An efficient, highly selective method for polyfluoroalkylation of 2-aminothiazole derivatives is described. Interestingly, defluorinated 2-amino-5-(1,1,1,3,3,3-hexafluoroprop-2-yl)thiazole derivative was obtained in moderate yields when 2-aminothiazole was reacted with (CF3)2CFI.

Journal of Fluorine Chemistry published new progress about Fluoroalkylation. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Product Details of C9H7N3O2S.

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

Haake, Paul; Bausher, Larry P. published the artcile< Thiazolium ions and related heteroaromatic systems. II. The acidity constants of thiazolium, oxazolium, and imidazolium ions>, Product Details of C7H9NO2S, the main research area is thiazolium acidity constant; oxazolium acidity constant; imidazolium acidity constant.

The pKa’s of the protonated forms of several oxazoles, thiazoles, and imidazoles were determined Oxazoles are ∼106 less basic than imidazoles, and thiazoles are ∼104 less basic than imidazoles. The pK’s for azolium acids indicate that zwitterionic forms are favored for imidazole acids, but uncharged forms are favored for thiazole and oxazole acids.

Journal of Physical Chemistry published new progress about Ionization. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Product Details of C7H9NO2S.

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

Fushimi, Makoto; Buck, Hannes; Balbach, Melanie; Gorovyy, Anna; Ferreira, Jacob; Rossetti, Thomas; Kaur, Navpreet; Levin, Lonny R.; Buck, Jochen; Quast, Jonathan; van den Heuvel, Joop; Steegborn, Clemens; Finkin-Groner, Efrat; Kargman, Stacia; Michino, Mayako; Foley, Michael A.; Miller, Michael; Liverton, Nigel J.; Huggins, David J.; Meinke, Peter T. published the artcile< Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10)>, Computed Properties of 1003-32-3, the main research area is adenylyl cyclase inhibitor oral bioavailability.

Soluble adenylyl cyclase (sAC) has gained attention as a potential therapeutic target given the role of this enzyme in intracellular signaling. We describe successful efforts to design improved sAC inhibitors amenable for in vivo interrogation of sAC inhibition to assess its potential therapeutic applications. This work culminated in the identification of TDI-10229 (12), which displays nanomolar inhibition of sAC in both biochem. and cellular assays and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound

ACS Medicinal Chemistry Letters published new progress about Drug design. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Computed Properties of 1003-32-3.

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

Siegel, David J.; Anderson, Grace I.; Paul, Lauren M.; Seibert, Philipp J.; Hillesheim, Patrick C.; Sheng, Yinghong; Zeller, Matthias; Taubert, Andreas; Werner, Peter; Balischewski, Christian; Michael, Scott F.; Mirjafari, Arsalan published the artcile< Design Principles of Lipid-like Ionic Liquids for Gene Delivery>, Recommanded Product: 4,5-Dihydrothiazole-2-thiol, the main research area is ionic liquid gene delivery amphiphile lipid; DNA delivery; biomaterials; cationic lipids; gene therapy; ionic liquids; lipid-like materials; nonviral vectors.

We developed lipid-like ionic liquids, containing 2-mercaptoimidazolium and 2-mercaptothiazolinium headgroups tethered to two long saturated alkyl chains, as carriers for in vitro delivery of plasmid HEK DNA into 293T cells. We employed a combination of modular design, synthesis, X-ray anal., and computational modeling to rationalize the self-assembly and desired physicochem. and biol. properties. The results suggest that thioamide-derived ionic liquids may serve as a modular platform for lipid-mediated gene delivery. This work represents a step toward understanding the structure-function relationships of these amphiphiles with long-range ordering and offering insight into design principles for synthetic vectors based on self-assembly behavior.

ACS Applied Bio Materials published new progress about Amphiphiles. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Recommanded Product: 4,5-Dihydrothiazole-2-thiol.

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

Nakajima, Kanako; Hamada, Kazuko; Ito, Ryoga; Yoshida, Yukina; Sutherland, Kenneth; Ishikawa, Masayori; Ozaki, Michitaka; Shirato, Hiroki; Hamada, Toshiyuki published the artcile< Stability of -luciferin for bioluminescence to detect gene expression in freely moving mice for long durations>, Product Details of C11H8N2O3S2, the main research area is Dluciferin L luciferin antiobesity agent obesity cancer; Period1; circadian rhythm; in vivo imaging; luciferin.

Circadian disturbance of clock gene expression is a risk factor for diseases such as obesity, cancer, and sleep disorders. To study these diseases, it is necessary to monitor and analyze the expression rhythm of clock genes in the whole body for a long duration. The bioluminescent reporter enzyme firefly luciferase and its substrate -luciferin have been used to generate optical signals from tissues in vivo with high sensitivity. However, little information is known about the stability of -luciferin to detect gene expression in living animals for a long duration. In the present study, we examined the stability of a luciferin solution over 21 days. -Luciferin, which is synthesized using racemization of -luciferin, was at high concentrations after 21 days. In addition, we showed that bioluminescence of Period1 (Per1) expression in the liver was significantly decreased compared with the day 1 solution, although locomotor activity rhythm was not affected. These results showed that -luciferin should be applied to the mouse within, at most, 7 days to detect bioluminescence of Per1 gene expression rhythm in vivo.

Luminescence published new progress about Acyl-CoA-binding proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Product Details of C11H8N2O3S2.

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

Patel, Bhargav A.; Abel, Biebele; Barbuti, Anna Maria; Velagapudi, Uday Kiran; Chen, Zhe-Sheng; Ambudkar, Suresh V.; Talele, Tanaji T. published the artcile< Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein>, Safety of Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is thiazole peptidomimetic synthesis ATPase stimulator inhibitor structure activity; drug substrate binding P glycoprotein antitumor agent mol docking; peptide coupling Boc protection.

A novel set of 64 analogs based on our lead compound (I) was designed and synthesized with an initial objective of understanding the structural requirements of ligands binding to a highly perplexing substrate-binding site of P-gp and their effect on modulating the ATPase function of the efflux pump. Compound I, a stimulator of P-gp ATPase activity, was transformed to ATPase inhibitory compounds (II), (III) and (IV). The ATPase inhibition by these compounds was predominantly contributed by the presence of a cyclohexyl group in lieu of the 2-aminobenzophenone moiety of I. The 4,4-difluorocyclohexyl analogs III and IV inhibited the photolabeling by [125I]-IAAP, with IC50 values of 0.1 and 0.76 M, resp. Selected compounds were shown to reverse paclitaxel resistance in HEK293 cells overexpressing P-gp and were selective toward P-gp over CYP3A4. Induced-fit docking highlighted a plausible binding pattern of inhibitory compounds in the putative-binding pocket of P-gp. The current study underscores the stringent requirement by P-gp to bind to chem. similar mols.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Safety of Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

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