Author: tianli

L’abbe, Gerrit; Yu, Chih-Chou published the artcile< Trapping of thiaziridinimines with thiocarbonyl compounds>, Formula: C10H9NOS2, the main research area is thiaziridinimine thiocarbonyl trap; dithiazolidine spirothiazolidine; thiazolidine spirodithiazolidine; thiatriazoline thermolysis; dithiazolidinimine.

Thermolysis of 4-benzyl-5-tosylimino-1,2,3,4-thiatriazoline (I; Ts = 4-MeC6H4SO2) at 60-70° in the presence of representative C=S unsaturated compounds furnished 1,2,4-dithiazolidin-5-imines in moderate yields. An intermediate unstable thiaziridinimine which is trapped by the C=S compound in a regiospecific manner is postulated. Among the thiocarbonyl compounds used are p,p’-dimethoxythiobenzophenone, xanthates and 3-benzylrhodanine, the latter giving a spiro adduct II.

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

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

Murty, Surya; Haile, Samuel T.; Beinat, Corinne; Aalipour, Amin; Alam, Israt S.; Murty, Tara; Shaffer, Travis M.; Patel, Chirag B.; Graves, Edward E.; Mackall, Crystal L.; Gambhir, Sanjiv S. published the artcile< Intravital imaging reveals synergistic effect of CAR T-cells and radiation therapy in a preclinical immunocompetent glioblastoma model>, HPLC of Formula: 2591-17-5, the main research area is disialoganglioside GD2 CAR T cell apoptosis glioblastoma; Chimeric antigen receptor (CAR); glioblastoma; imaging; immunotherapy; intravital microscopy.

Recent advances in novel immune strategies, particularly chimeric antigen receptor (CAR)-bearing T-cells, have shown limited efficacy against glioblastoma (GBM) in clin. trials. We currently have an incomplete understanding of how these emerging therapies integrate with the current standard of care, specifically radiation therapy (RT). Addnitionally, there is an insufficient number of preclin. studies monitoring these therapies with high spatiotemporal resolution To address these limitations, we report the first longitudinal fluorescence-based intravital microscopy imaging of CAR T-cells within an orthotopic GBM preclin. model to illustrate the necessity of RT for complete therapeutic response. Complete antitumor response in advanced syngeneic orthotopic models of GBM was achieved only when a single i.v. dose of GD2 CAR T-cells was following either sub-lethal whole-body irradiation or focal RT. Intravital microscopy imaging successfully visualized CAR T-cell homing and T-cell mediated apoptosis of tumor cells in real-time within the tumor stroma. Findings indicate that RT allows for rapid CAR T-cell extravasation from the vasculature and expansion within the tumor microenvironment. These exciting results highlight potential opportunities to improve IV adoptive T-cell administration in the treatment of GBM through concurrent RT. Addnl., they emphasize the need for advancements in immunotherapeutic homing to and extravasation through the tumor microenvironment.

OncoImmunology published new progress about Apoptosis. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, HPLC of Formula: 2591-17-5.

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

Sparey, Tim; Abeywickrema, Pravien; Almond, Sarah; Brandon, Nick; Byrne, Noel; Campbell, Alister; Hutson, Pete H.; Jacobson, Marlene; Jones, Brian; Munshi, Sanjeev; Pascarella, Danette; Pike, Andrew; Prasad, G. Sridhar; Sachs, Nancy; Sakatis, Melanie; Sardana, Vinod; Venkatraman, Shankar; Young, Mary Beth published the artcile< The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors>, Electric Literature of 1003-32-3, the main research area is fused pyrrole carboxylate preparation aminoacid oxidase DAO inhibitor structure; schizophrenia fused pyrrole carboxylic acid DAO inhibitor.

The NMDA hypofunction hypothesis of schizophrenia’ can be tested in a number of ways. DAO is the enzyme primarily responsible for the metabolism of D-serine, a co-agonist for the NMDA receptor. We identified novel DAO inhibitors, in particular, acid 1, which demonstrated moderate potency for DAO in vitro and ex vivo, and raised plasma D-serine levels after dosing i.p. to rats. In parallel, analogs were prepared to survey the SARs of 1.

Bioorganic & Medicinal Chemistry Letters published new progress about Antipsychotics. 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

Ching, Kuan-Chieh; Tran, Thi Ngoc Quy; Amrun, Siti Naqiah; Kam, Yiu-Wing; Ng, Lisa F. P.; Chai, Christina L. L. published the artcile< Structural Optimizations of Thieno[3,2-b]pyrrole Derivatives for the Development of Metabolically Stable Inhibitors of Chikungunya Virus>, Quality Control of 1003-32-3, the main research area is thieno pyrrole derivative preparation metabolic stability Chikungunya Virus antiviral.

Chikungunya virus (CHIKV) is a re-emerging vector-borne alphavirus, and there is no approved effective antiviral treatment currently available for CHIKV. We previously reported the discovery of thieno[3,2-b]pyrrole 1b that displayed good antiviral activity against CHIKV infection in vitro. However, it has a short half-life in the presence of human liver microsomes (HLMs) (T1/2 = 2.91 min). Herein, we report further optimization studies in which potential metabolically labile sites on compound 1b were removed or modified, resulting in the identification of thieno[3,2-b]pyrrole 20 and pyrrolo[2,3-d]thiazole 23c possessing up to 17-fold increase in metabolic half-lives in HLMs and good in vivo pharmacokinetic properties. Compound 20 not only attenuated viral RNA production and displayed broad-spectrum antiviral activity against other alphaviruses and CHIKV isolates but also exhibited limited cytotoxic liability (CC50 > 100 μM). These studies have identified two compounds that have the potential for further development as antiviral drugs against CHIKV infection.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 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

Stachulski, Andrew V.; Pidathala, Chandrakala; Row, Eleanor C.; Sharma, Raman; Berry, Neil G.; Iqbal, Mazhar; Bentley, Joanne; Allman, Sarah A.; Edwards, Geoffrey; Helm, Alison; Hellier, Jennifer; Korba, Brent E.; Semple, J. Edward; Rossignol, Jean-Francois published the artcile< Thiazolides as Novel Antiviral Agents. 1. Inhibition of Hepatitis B Virus Replication>, Formula: C6H10N2S, the main research area is thiazolide preparation Hepatitis replication inhibition antiviral human structure activity.

The syntheses and activities of a wide range of thiazolides [viz., 2-hydroxyaroyl-N-(thiazol-2-yl)amides] against hepatitis B virus replication, with results of QSAR anal. are reported. The prototypical thiazolide, nitazoxanide [2-hydroxybenzoyl-N-(5-nitrothiazol-2-yl)amide, NTZ] I, is a broad spectrum antiinfective agent effective against anaerobic bacteria, viruses, and parasites. By contrast, 2-hydroxybenzoyl-N-(5-chlorothiazol-2-yl)amide II is a novel, potent, and selective inhibitor of hepatitis B replication (EC50 = 0.33 μm) but is inactive against anaerobes. Several 4′- and 5′-substituted thiazolides show good activity against HBV; by contrast, some related salicyloylanilides show a narrower spectrum of activity. The ADME properties of II are similar to I, viz., the O-acetate is an effective prodrug, and the O-aryl glucuronide is a major metabolite. The QSAR study shows a good correlation of observed EC90 for intracellular virions with thiazolide structural parameters. Finally the mechanism of action of thiazolides in relation to the present results is discussed.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 101080-15-3 belongs to class thiazole, and the molecular formula is C6H10N2S, Formula: C6H10N2S.

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

Qian, Yuanyuan; Allegretta, Giuseppe; Janardhanan, Jeshina; Peng, Zhihong; Mahasenan, Kiran V.; Lastochkin, Elena; Gozun, Melissa Malia N.; Tejera, Sara; Schroeder, Valerie A.; Wolter, William R.; Feltzer, Rhona; Mobashery, Shahriar; Chang, Mayland published the artcile< Exploration of the Structural Space in 4(3H)-Quinazolinone Antibacterials>, Recommanded Product: Thiazole-5-carboxyaldehyde, the main research area is quinazolinone preparation antibacterial pharmacokinetic SAR staphylococcus aureus QSAR.

Herein the syntheses of 79 derivatives of the 4(3H)-quinazolinones and their structure-activity relationship (SAR) against methicillin-resistant Staphylococcus aureus (MRSA) is reported. Twenty-one analogs were further evaluated in in vitro assays. Subsequent investigation of the pharmacokinetic properties singled out compound I ((E)-3-(5-carboxy-2-fluorophenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one) for further study. The compound synergized with piperacillin-tazobactam (TZP) both in vitro and in vivo in a clin. relevant mouse model of MRSA infection. The TZP combination lacks activity against MRSA, yet it synergized with compound I to kill MRSA in a bactericidal manner. The synergy is rationalized by the ability of the quinazolinones to bind to the allosteric site of penicillin-binding protein (PBP)2a, resulting in opening of the active site, whereby the β-lactam antibiotic now is enabled to bind to the active site in its mechanism of action. The combination effectively treats MRSA infection, for which many antibiotics (including TZP) have faced clin. obsolescence.

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Recommanded Product: Thiazole-5-carboxyaldehyde.

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

Jeong, Siyeon; Kim, Eunmin; Kim, Minkyu; Hwang, Ye Ji; Padhi, Birakishore; Choi, Jonghoon; Lee, Yunho; Joo, Jung Min published the artcile< Divergent Strategies for the π-Extension of Heteroaryl Halides Using Norbornadiene as an Acetylene Synthon>, Category: thiazole, the main research area is three component reaction norbornadiene norbornene diheteroarylation cycloannulation.

Pd-catalyzed multicomponent coupling reactions of five-membered heteroaryl halides and norbornadiene (NBD) were developed. Either direct addition of (benzo)azoles or 2:1 annulation was achieved depending on the propensity of the intermediate complex to undergo palladacycle formation, determined by the nature and substitution pattern of the heteroarene. The obtained exo- and cis-diheteroaryl norbornenes underwent epimerization and retro-Diels-Alder reactions to afford the corresponding trans-isomers and π-extended heteroaromatic systems, resp., demonstrating the versatility of NBD as an acetylene synthon.

Organic Letters published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Category: thiazole.

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

Roe, Caroline; Hobbs, Heather; Stockman, Robert A. published the artcile< Multicomponent synthesis of chiral sulfinimines>, Reference of 1003-32-3, the main research area is chiral sulfinimine enantioselective preparation; oxathiazolidine oxide Grignard reagent aldehyde multicomponent reaction.

Two oxathiozolidine-S-oxide templates have been developed and used in a four-component coupling protocol for the synthesis of a wide range of chiral sulfinimines in high enantiomeric excesses. The templates can be synthesized from cheap commodity chems. in three steps in high yields. Furthermore the template is easily recovered in high yields for recycling.

Chemistry – A European Journal published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Reference of 1003-32-3.

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

Cheng, Lin; Su, Lantian; Tian, Xiaowen; Xia, Fan; Zhao, Chang; Yan, Wei; Shao, Zhenhua published the artcile< A pipeline to investigate the structures and signaling pathways of sphingosine 1-phosphate receptors>, Quality Control of 115144-35-9, the main research area is sphingosine 1 phosphate receptor structure signaling pathway investigation.

Lysophospholipids (LPLs) are bioactive lipids that include sphingosine 1-phosphate (S1P), lysophosphatidic acid, etc. S1P, a metabolic product of sphingolipids in the cell membrane, is one of the best-characterized LPLs that regulates a variety of cellular physiol. responses via signaling pathways mediated by sphingosine 1-phosphate receptors (S1PRs). This implicated that the S1P-S1PRs signaling system is a remarkable potential therapeutic target for disorders, including multiple sclerosis (MS), autoimmune disorders, cancer, inflammation, and even COVID-19. S1PRs, a small subset of the class A G-protein coupled receptor (GPCR) family, are composed of five subtypes: S1PR1, S1PR2, S1PR3, S1PR4, and S1PR5. The lack of detailed structural information, however, impedes the drug discovery targeting S1PRs. Here, we applied the cryo-electron microscopy method to solve the structure of the S1P-S1PRs complex, and elucidated the mechanism of activation, selective drug recognition, and G-protein coupling by using cell-based functional assays. Other lysophospholipid receptors (LPLRs) and GPCRs can also be studied using this strategy.

Journal of Visualized Experiments published new progress about Autoimmune disease. 115144-35-9 belongs to class thiazole, and the molecular formula is C11H7KN2O3S2, Quality Control of 115144-35-9.

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

De Rosa, Maria; Unge, Johan; Motwani, Hitesh V.; Rosenquist, Aasa; Vrang, Lotta; Wallberg, Hans; Larhed, Mats published the artcile< Synthesis of P1'-Functionalized Macrocyclic Transition-State Mimicking HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol>, Category: thiazole, the main research area is tertiary alc linear macrocyclic peptidomimetic preparation HIV1 protease inhibitor.

Seven novel tertiary alc.-containing linear HIV-1 protease inhibitors (PIs), decorated at the para position of the benzyl group in the P1′ side with (hetero)aromatic moieties, were synthesized and biol. evaluated. To study the inhibition and antiviral activity effect of P1-P3 macrocyclization, 14- and 15-membered macrocyclic PIs were prepared by ring-closing metathesis of the corresponding linear PIs. The macrocycles were more active than the linear precursors and compound 10f, with a 2-thiazolyl group in the P1′ position, was the most potent PI of this new series (Ki = 2.2 nM, EC50 0.2 μM). Co-crystallized complexes of both linear and macrocyclic PIs with the HIV-1 protease enzyme were prepared and analyzed.

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

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