Day: November 10, 2022

Su, H. published the artcileA study of the alkylation and acylation of N-acylthiazolidinethione, COA of Formula: C10H11NS2, the main research area is acylthiazolidinethione alkylation acylation.

Studying the alkylation and acylation of N-acylthiazolidinethione, the desired α-alkylated products and C-acylated products are not obtained, but rather the S-alkylated products and O-acylated products were obtained. The possible mechanism proposed shows that the deprotonation agent and electrophilic species are responsible for the stability of enolates. The enolates derived from N-acylthiazolidinethiones are decomposed in the presence of base, but they are comparatively stable in the presence of Lewis acid. When electrophilic reagent is alkyl halide, the enolate decomposition is the dominating pathway, and affords the S-alkylated products; and when electrophilic reagent is acyl chloride, the formation of a highly ordered chelated transition-state is the dominating pathway, and affords the O-acylated products.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, COA of Formula: C10H11NS2.

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

Morales-Nava, Rosmarbel published the artcileMicrowave-assisted improved synthesis of oxazolidin-2-ones, oxazolidine-2-thiones and thiazolidine-2-thione chiral auxiliaries, Name: (S)-4-Benzylthiazolidine-2-thione, the main research area is amino alc carbonate cyclization carbonylation microwave; carbon sulfide amino alc cyclization carbonylation microwave; oxazolidinone chiral auxiliary preparation; oxazolidinethione chiral auxiliary preparation; thiazolidinethione chiral auxiliary preparation.

The synthesis of the target compounds was achieved by a microwave-assisted method and typical 4-substituted oxazolidinone chiral auxiliaries were obtained. Under these conditions, treatment of (S)-phenylalaninol, (S)-phenylglycinol, (S)-valinol, and (1S,2R)-norephedrine with (EtO)2CO or CS2 under the appropriate and specific microwave reaction conditions, led to an efficient synthesis of oxazolidin-2-ones, oxazolidine-2-thiones, and thiazolidine-2-thiones. The methodol. provides these chiral auxiliaries with improved yields and a remarkable reduction in reaction times, particularly in the case of 2-thiazolidinethione derivatives, as compared with the conventional methods.

Molecules published new progress about Amino alcohols, chiral Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, Name: (S)-4-Benzylthiazolidine-2-thione.

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

Protopopov, Mykola V. published the artcileIdentification of 1,3-thiazole-5-carboxylic Acid Derivatives as Inhibitors of Protein Kinase CK2, Safety of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, the main research area is protein kinase thiazole carboxylic acid CK inhibitor.

Serine/threonine protein kinase CK2 is involved in the regulation of a number of cellular functions such as cell growth, proliferation, differentiation and apoptosis. Increased activity of CK2 is associated with the development of different types of cancer, inflammatory response, pain and virus infections. Therefore, protein kinase CK2 is an attractive mol. target for the development of small-mol. inhibitors which can be important compounds for pharmaceutical application. The main aim of this research is to identify novel chem. class of CK2 inhibitors with good lead-like properties. In order to find novel CK2 inhibitors, virtual screening experiments were performed using Autodock software. Best-scored compounds were tested in vitro using P32 radioactive kinase assay. Small-mol. inhibitors of protein kinase CK2 were identified among the derivatives of 1,3-thiazole-5-carboxylic acid. The most active compound inhibited CK2 with IC50 value of 0.4 μM. Ligand efficiency for studied derivatives of 1,3-thiazole-5-carboxylic acid was in the range from 0.45 to 0.56 kcal/mol/non-hydrogen atom. Considering the fact that the lower limit for ligand efficiency parameter is 0.3, the identified CK2 inhibitors among the derivatives of 1,3-thiazole-5-carboxylic acid are excellent candidates for further lead optimization.

Current Enzyme Inhibition published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Safety of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid.

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

Yamaguchi, Kohji published the artcile4-phenylthiazole derivatives inhibit IL-6 secretion in osteoblastic cells and suppress bone weight loss in ovariectomized mice, SDS of cas: 99822-80-7, the main research area is phenylthiazole derivative osteoblast interleukin6 secretion; osteoporosis phenylthiazole derivative structure.

A series of 4-phenylthiazole derivatives were synthesized and tested their inhibitory effect on the interleukin-6 secretion stimulated by PTH in osteoblastic cells. SCRC2941-18, 2-amino-4-(4-chlorophenyl)-5-methylthiazole, was found to be the most potent inhibitor in the derivatives Furthermore, SCRC2941-18 significantly suppressed the bone weight loss in the ovariectomized mice, an osteoporosis model.

Bioorganic & Medicinal Chemistry Letters published new progress about Interleukin 6 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 99822-80-7 belongs to class thiazole, name is Ethyl 4-phenylthiazole-5-carboxylate, and the molecular formula is C12H11NO2S, SDS of cas: 99822-80-7.

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

Sierra, Michael L. published the artcileSubstituted 2-[(4-Aminomethyl)phenoxy]-2-methylpropionic Acid PPARα Agonists. 1. Discovery of a Novel Series of Potent HDLc Raising Agents, Application In Synthesis of 144060-99-1, the main research area is arylmethylpropionic acid derivative SAR preparation PPAR agonist HDLc raising.

The peroxisome proliferator activated receptors PPARα, PPARγ, and PPARδ are ligand-activated transcription factors that play a key role in lipid homeostasis. The fibrates raise circulating levels of high-d. lipoprotein cholesterol and lower levels of triglycerides in part through their activity as PPARα agonists; however, the low potency and restricted selectivity of the fibrates may limit their efficacy, and it would be desirable to develop more potent and selective PPARα agonists. Modification of the selective PPARδ agonist 1 (GW501516) so as to incorporate the 2-aryl-2-methylpropionic acid group of the fibrates led to a marked shift in potency and selectivity toward PPARα agonism. Optimization of the series gave 25a, which shows EC50 = 4 nM on PPARα and at least 500-fold selectivity vs. PPARδ and PPARγ. Compound 25a (GW590735) has been progressed to clin. trials for the treatment of diseases of lipid imbalance.

Journal of Medicinal Chemistry published new progress about Lipid metabolism disorders Role: BIOL (Biological Study). 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Application In Synthesis of 144060-99-1.

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

Lohans, Christopher T. published the artcileBiochemical, Structural, and Genetic Characterization of Tridecaptin A1, an Antagonist of Campylobacter jejuni, COA of Formula: C10H11NS2, the main research area is sequence tridecaptin A1 paenicidin B Paenibacillus gene cluster; antimicrobial agents; bacteriocins; lipopeptides; peptides; structure elucidation.

Bacillus circulans NRRL B-30644 (now Paenibacillus terrae) was previously reported to produce SRCAM 1580, a bacteriocin active against the food pathogen Campylobacter jejuni. We have been unable to isolate SRCAM 1580, and did not find any genetic determinants in the genome of this strain. We now report the reassignment of this activity to the lipopeptide tridecaptin A1. Structural characterization of tridecaptin A1 was achieved through NMR, MS/MS and GC-MS studies. The structure was confirmed through the first chem. synthesis of tridecaptin A1, which also revealed the stereochem. of the lipid chain. The impact of this stereochem. on antimicrobial activity was examined The biosynthetic machinery responsible for tridecaptin production was identified through bioinformatic analyses. P. terrae NRRL B-30644 also produces paenicidin B, a novel lantibiotic active against Gram-pos. bacteria. MS/MS analyses indicate that this lantibiotic is structurally similar to paenicidin A.

ChemBioChem published new progress about ATP-binding cassette transporters Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (gene pabE). 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, COA of Formula: C10H11NS2.

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

Sharma, Swagat published the artcileDiscovery, synthesis and characterization of a series of (1-alkyl-3-methyl-1H-pyrazol-5-yl)-2-(5-aryl-2H-tetrazol-2-yl)acetamides as novel GIRK1/2 potassium channel activators, Product Details of C11H9NO2S, the main research area is pyrazolyl arylazolyl acetamide preparation GIRK channel activator SAR; Activator; G protein-regulated inwardly-rectifying potassium channel; GIRK; Tetrazole.

The study described the discovery and characterization of a series of 5-aryl-2H-tetrazol-3-yl acetamides as G protein-gated inwardly-rectifying potassium (GIRK) channels activators. Working from an initial hit discovered during a high-throughput screening campaign, a tetrazole scaffold was identified that shifts away from the previously reported urea-based scaffolds while remaining effective GIRK1/2 channel activators. In addition, the compounds were evaluated in Tier 1 DMPK assays and identified a (3-methyl-1H-pyrazol-1-yl)tetrahydrothiophene-1,1-dioxide head group that imparts interesting and unexpected microsomal stability compared to previously-reported pyrazole head groups.

Bioorganic & Medicinal Chemistry Letters published new progress about Drug discovery. 16441-28-4 belongs to class thiazole, name is 2-(2-Phenylthiazol-4-yl)acetic acid, and the molecular formula is C11H9NO2S, Product Details of C11H9NO2S.

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

Liu, Xiaobo published the artcileDesign, synthesis, and biological evaluation of [1,2,4]triazolo[4,3-a] pyrazine derivatives as novel dual c-Met/VEGFR-2 inhibitors, Synthetic Route of 144060-99-1, the main research area is triazolopyrazine preparation antitumor activity apoptosis hemolytic toxicity mol docking; antiproliferative activity; antitumor; c-Met inhibitor; pyrazine derivatives; targeted drug.

In this study, a series of novel [1,2,4]triazolo[4,3-a]pyrazine derivatives, I (R = 4-methyl-2-phenyl-1,3-thiazol-5-yl, 4-(4-methyl-1,3-thiazol-2-yl)pyridine, 3-(thiophen-2-yl)-1H-pyrazol-5-yl, etc.; R1 = H, Me; X = H, F) evaluated for their inhibitory activities toward c-Met/VEGFR-2 kinases and antiproliferative activities against tested three cell lines in vitro was designed and synthesized. Most of the compounds I showed satisfactory activity compared with lead compound foretinib. Among them, the most promising compound I (R = 1-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrazol-4-yl, R1 = Me; X = F) (II) exhibited excellent antiproliferative activities against A549, MCF-7, and Hela cancer cell lines with IC50 values of 0.98 ± 0.08, 1.05 ± 0.17, and 1.28 ± 0.25μM, resp., as well as excellent kinase inhibitory activities (c-Met IC50 = 26.00 nM and VEGFR-2 IC50 = 2.6μM). Moreover, compound II inhibited the growth of A549 cells in G0/G1 phase in a dose-dependent manner, and induced the late apoptosis of A549 cells. Its intervention on intracellular c-Met signaling of A549 was verified by the result of Western blot. Fluorescence quant. PCR showed that compound 17l inhibited the growth of A549 cells by inhibiting the expression of c-Met and VEGFR-2, and its hemolytic toxicity was low. Mol. docking and mol. dynamics simulation indicated that compound II could bind to c-Met and VEGFR-2 protein, which was similar to that of foretinib.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about Acids Role: RCT (Reactant), RACT (Reactant or Reagent). 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Synthetic Route of 144060-99-1.

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

Nomura, Masahiro published the artcileDiscovery of cyclic amine-substituted benzoic acids as PPARα agonists, Product Details of C11H8FNO2S, the main research area is benzoic acid cyclic amine substituted preparation SAR PPAR agonist.

A series of novel cyclic amine-substituted benzoic acid derivatives was synthesized and evaluated for PPARα agonist activity. Structure-activity relationship studies led to the identification of (S)-3-[3-[2-(4-chlorophenyl)-4-methylthiazole-5-carboxamido]piperidin-1-yl]benzoic acid (I) (KRP-105) as a potent and high subtype-selective human PPARα agonist. I showed excellent PK profile, and oral administration of I to high-fat diet dogs effectively lowered triglycerides.

Bioorganic & Medicinal Chemistry Letters published new progress about Cyclic amines Role: PAC (Pharmacological Activity), PKT (Pharmacokinetics), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Product Details of C11H8FNO2S.

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