Tag: M.W=200-250

Hitchin, James R.; Blagg, Julian; Burke, Rosemary; Burns, Samantha; Cockerill, Mark J.; Fairweather, Emma E.; Hutton, Colin; Jordan, Allan M.; McAndrew, Craig; Mirza, Amin; Mould, Daniel; Thomson, Graeme J.; Waddell, Ian; Ogilvie, Donald J. published the artcile< Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments>, Quality Control of 57493-24-0, the main research area is LSD1 inhibitor SAR anticancer acute myeloid leukemia MAOA protein.

Two series of aminothiazoles have been developed as reversible inhibitors of lysine specific demethylase 1 (LSD1) through the expansion of a hit derived from a high concentration biochem. fragment based screen of 2466 compounds The potency of the initial fragment hit was increased 32-fold through synthesis, with one series of compounds showing clear structure-activity relationships and inhibitory activities in the range of 7 to 187 μM in a biochem. assay. This series also showed selectivity against the related FAD-dependent enzyme mono-amine oxidase A (MAO-A). Although a wide range of irreversible inhibitors of LSD1 have been reported with activities in the low nanomolar range, this work represents one of the first reported examples of a reversible small mol. inhibitor of LSD1 with clear SAR and selectivity against MAO-A, and could provide a platform for the development of more potent reversible inhibitors. Herein, we also report the use of a recently developed cell-based assay for profiling LSD1 inhibitors, and present results on our own compounds as well as a selection of recently described reversible LSD1 inhibitors.

MedChemComm published new progress about Acute myeloid leukemia. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Quality Control of 57493-24-0.

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

Tissaoui, Khalil; Raouafi, Noureddine; Boujlel, Khaled published the artcile< Electrogenerated base-promoted synthesis of N-benzylic rhodanine and carbamodithioate derivatives>, Formula: C10H9NOS2, the main research area is rhodanine carbamodithioate benzylic electrosynthesis.

Electrogenerated magnesium-associated cyanomethyl anions/bases obtained from the electrochem. reduction of acetonitrile and the oxidation of a sacrificial magnesium rod were successfully used to promote the addition of carbon disulfide to primary benzylic amines. Alkylation with Et 3-bromopropionate or with Et 2-bromoacetate yields the corresponding carbamodithioates R1NHC(S)SCH2CH2CO2Et (R1 = PhCH2, 2-ClC6H4CH2, 2-pyridylmethyl, etc.) or cyclic rhodanines I (R2 = PhCH2, 2-ClC6H4CH2, 3-furylmethyl, etc.), resp. The effect of the amount of electrogenerated base on the yield of reaction was also evaluated.

Journal of Sulfur Chemistry published new progress about Aralkyl amines Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Formula: C10H9NOS2.

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

Jiang, Cheng; Yuan, Zhi; Wang, Ju-Fei; Fu, Jie; Jiang, Guang-Jun; Zheng, Liang-Rong published the artcile< Design of novel thiazole bearing pyrazole derivatives and their dual activities as ACE inhibitors and calcium channel blockers in cardiovascular disease>, Electric Literature of 57493-24-0, the main research area is cardiovascular disease thiazole pyrazole derivative ACE inhibitor calcium channel.

In an attempt to develop drugs for cardio-vascular disease, present manuscript deal with the development of dual acting agents targeting angiotensin converting enzyme (ACE) and calcium channel to treat hypertension. These mols. were developed via efficient multi-step synthetic route in excellent yield. In ACE inhibitors assay, these compounds showed considerable percentage of inhibition (32-94 %) with IC50 = 1.2 and 1.5 μM for most promising compound 6e and 6o, resp. In mol. docking study with ACE, compound 6e revealed similar fashion of mol. interaction with catalytic residues His353, Ala 354, Tyr 523, Tyr 520, and Glu 152, comparable with standard lisinopril. Addnl., in rat aortic strip model, these mols. significantly induce vasorelaxation via inhibiting Ca2+ channel in dose dependent manner.

Latin American Journal of Pharmacy published new progress about Angiotensin-converting enzyme inhibitors. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Electric Literature of 57493-24-0.

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

Raut, D. G.; Sonawane, K. D.; Jadhav, S. Y.; Sonawane, V. D.; Jadhav, D. B.; Dhanavade, M. J.; Bhosale, R. B. published the artcile< Synthesis and potential antibacterial activities of 2-chloro-N-(4-phenylthiazol-2-yl)acetamide derivatives>, Category: thiazole, the main research area is phenylthiazolyl chloroacetamide preparation antibacterial.

A series of substituted 2-chloro-N-(4-phenylthiazol-2-yl)acetamide derivatives I [R = H, 4-OMe, 3-NO2, 2,4-Cl2, etc.] were synthesized via condensation between 4-(substituted phenyl)-2-aminothiazoles with chloroacetyl chloride. The synthesized compounds were evaluated for antibacterial activity at three concentrations (25 μg/mL, 50 μg/mL and 100 μg/mL) and results were expressed in terms of zone of inhibition in millimeters by agar well diffusion method using Ampicillin 1mg/mL as reference standard drug. Among the tested compounds, compounds I [R = H, 4-OMe, 2,4-Cl2] showed the potent antibacterial activity against Gram pos. bacteria Bacillus subtilis and Gram neg. bacteria Salmonella typhimurium.

Pharma Chemica published new progress about Acetamides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Category: thiazole.

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

Zhu, Yu-Shen; Shi, Linlin; Fu, Lianrong; Chen, Xiran; Zhu, Xinju; Hao, Xin-Qi; Song, Mao-Ping published the artcile< Iodine-catalyzed amination of benzothiazoles with KSeCN in water to access primary 2-aminobenzothiazoles>, SDS of cas: 1160791-13-8, the main research area is primary aminobenzothiazole preparation green chem; benzothiazole selenocyanate potassium amination iodine catalyst.

A facile and sustainable approach for the amination of benzothiazoles I (X = H, N; R = H, 4-Cl, 5-OMe, 6-NO2, 7-C(O)OMe; R1 = H) with KSeCN using iodine as the catalyst in water has been disclosed under transition-metal free conditions. The reaction proceeded smoothly to afford various primary 2-amino benzothiazoles I (R1 = NH2) in up to 96% yield. A series of control experiments were performed, suggesting that a ring-opening mechanism was involved via a radical process. This protocol provides efficient synthesis of primary 2-aminobenzothiazole I (R1 = NH2).

Chinese Chemical Letters published new progress about Amination. 1160791-13-8 belongs to class thiazole, and the molecular formula is C6H4BrN3S, SDS of cas: 1160791-13-8.

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

Drobnica, L.; Knoppova, V.; Komanova, E. published the artcile< Isothiocyanates. XXXII. Microsynthesis of 3-substituted rhodanines>, Related Products of 10574-69-3, the main research area is rhodanine isothiocyanate thioglycolate.

Eleven 3-substituted rhodanines (I, R = Me, allyl, Ph, p-MeOC6H4, PhCH2, etc.) were prepared by addition of RNCS to HSCH2CO2R1(R1 = H, Et) and acid cyclization of the resultant thiocarbamoylmercaptoacetates RNHCS2CH2CO2R1. I were purified by thinlayer chromatog. Kinetic and uv data were given.

Chemicke Zvesti published new progress about 10574-69-3. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Related Products of 10574-69-3.

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

Lohans, Christopher T.; van Belkum, Marco J.; Cochrane, Stephen A.; Huang, Zedu; Sit, Clarissa S.; McMullen, Lynn M.; Vederas, John C. published the artcile< Biochemical, Structural, and Genetic Characterization of Tridecaptin A1, an Antagonist of Campylobacter jejuni>, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione, 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 16S rRNA Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione.

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

Morales-Nava, Rosmarbel; Fernandez-Zertuche, Mario; Ordonez, Mario published the artcile< Microwave-assisted improved synthesis of oxazolidin-2-ones, oxazolidine-2-thiones and thiazolidine-2-thione chiral auxiliaries>, Product Details of C10H11NS2, 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, and the molecular formula is C10H11NS2, Product Details of C10H11NS2.

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

Liang, Xiao-Ping; Luo, Min; Kang, Li; Tang, Long-Xing; Liang, Qing; Liu, Yuan-Lin; Yang, Zi; Zhang, Chun-Tao; Peng, Cai-Yun; Fu, Rong-Geng published the artcile< Facile one-pot three-component strategy for the synthesis of 2-amino-4-arylthiazoles via elemental sulfur source>, Application of C9H7N3O2S, the main research area is amino arylthiazole preparation green chem; aryl methyl ketone sulfur cyanamide three component cascade.

A novel and facile metal-free method for the green synthesis of 2-amino-4-arylthiazole derivatives I (Ar = 3-nitrophenyl, 2-naphthyl, pyridin-4-yl, etc.) through the three-component cascade reaction of aromatic Me ketones ArC(O)Me, elemental sulfur and cyanamide is reported. One C-N bond and two C-S bonds were formed in one-pot protocol without using catalysts.

Tetrahedron Letters published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application of C9H7N3O2S.

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

Martinez, Ana; Alonso, Mercedes; Castro, Ana; Dorronsoro, Isabel; Gelpi, J. Luis; Luque, F. Javier; Perez, Concepcion; Moreno, Francisco J. published the artcile< SAR and 3D-QSAR Studies on Thiadiazolidinone Derivatives: Exploration of Structural Requirements for Glycogen Synthase Kinase 3 Inhibitors>, Safety of 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is thiadiazolidinone derivative preparation QSAR glycogen synthase kinase 3 inhibitor.

The 2,4-disubstituted thiadiazolidinones (TDZD) are described as the first ATP-noncompetitive GSK-3 inhibitors. Following an SAR study about TDZD, different structural modifications in the heterocyclic ring aimed to test the influence of each heteroatom on the biol. study are here reported here. Various compounds such as hydantoins, dithiazolidindiones, rhodanines, maleimides, and triazoles were synthesized and screened as GSK-3 inhibitors. After an extensive SAR study among these different heterocyclic families, TDZDs have been revealed as a privileged scaffold for the selective inhibition of GSK-3. A Co-MFA anal. was also performed highlighting the mol. electrostatic field interaction in the interaction of TDZDs with GSK-3. Moreover, first mapping studies indicate two binding modes which in turn might imply relevant differences in the mechanism that underly the inhibitory activity of TDZDs.

Journal of Medicinal Chemistry published new progress about Conformation. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Safety of 3-Benzyl-2-thioxothiazolidin-4-one.

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