Tag: M.W=200-250

Song, Xin-Jian; Wang, Xu-Mei; Qi, Sun; Huang, Sheng-Tian; Yan, Wang published the artcile< Synthesis, crystal structure and antitumor activity of N-(5-aryl-1,3,4-thiadiazol-2-yl)-N'-((E)-styryl)ureas>, Name: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is aryl thiadiazolyl styryl urea preparation antitumor activity.

A series of N-(5-Aryl-1,3,4-thiadiazol-2-yl)-N’-((E)-styryl)ureas I (R = 2-F, 3-Me, 4-Cl, etc.) was designed and synthesized as antitumor agents. The single crystal of compound I (R = 2-F) was also determined by X-ray crystallog. Crystal data: monoclinic, space group P21/n, a = 4.9401(8), b = 8.7100(15), c = 36.604(6) Å, β = 93.320(3)°, V = 1572.4(5) Å3, Z = 4, F(000) = 704, Dc = 1.438 g/cm3, μ = 0.228 mm-1, R = 0.0600 and wR = 0.1448 for 2743 independent reflections (Rint = 0.0418) and 2174 observed ones (I > 2σ(I)) were provided. The in vitro antitumor activities of compounds I were preliminarily evaluated by the standard MTT assay.

Chinese Journal of Structural Chemistry published new progress about Antitumor agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Name: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Lee, Yong Ho; Denton, Elliott H.; Morandi, Bill published the artcile< Palladium-catalysed carboformylation of alkynes using acid chlorides as a dual carbon monoxide and carbon source>, Recommanded Product: 2-(Trifluoromethoxy)benzoyl chloride, the main research area is palladium catalyzed stereoselective carboformylation alkyne acid chloride.

Hydroformylation, a reaction that installs both a C-H bond and an aldehyde group across an unsaturated substrate, is one of the most important catalytic reactions in both industry and academia. Given the synthetic importance of creating new C-C bonds, the development of carboformylation reactions, wherein a new C-C bond is formed instead of a C-H bond, would bear enormous synthetic potential to rapidly increase mol. complexity in the synthesis of valuable aldehydes. However, the demanding complexity inherent in a four-component reaction, utilizing an exogenous CO source, has made the development of a direct carboformylation reaction a formidable challenge. Here, we describe a palladium-catalyzed strategy that uses readily available aroyl chlorides as a carbon electrophile and CO source, in tandem with a sterically congested hydrosilane, to perform a stereoselective carboformylation of alkynes [e.g., 2-methylbenzoyl chloride + i-Pr3SiH + n-PrCCPr-n → (Z)-I (up to 83%)]. An extension of this protocol to four chemodivergent carbonylations further highlights the creative opportunity offered by this strategy in carbonylation chem.

Nature Chemistry published new progress about Acid chlorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Recommanded Product: 2-(Trifluoromethoxy)benzoyl chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Makwane, Sunil; Srivastava, S. D.; Dua, Rajiv; Srivastava, S. K. published the artcile< Synthesis of 10-(2-phenyl-imidazo [2, 1-b] [1,3,4]thiadiazol-6-yl)-10H-phenothiazine derivatives and their in-vitro biological studies>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is phenyl dihydroimidazothiadiazolyl phenothiazine preparation antifungal antibacterial activity SAR.

New series of 10-(2-phenyl-5,6-dihydro-imidazo[2,1-b][1,3,4]thiadiazole-6-yl)-10H-phenothiazine were synthesized by cyclization of various carboxylic acid with thiosemicarbazide in presence of sulfuric acid was to get aminothiadiazoles. Another way phenothiazine treated with chloroacetyl chloride yielded chloroacetyl phenothiazine . Further, cyclization of aminothiadiazoles and chloroacetyl phenothiazine followed by refluxation about 18 h to get the final products 10-(2-phenyl-5,6-dihydro-imidazo[2,1-b][1,3,4]thiadiazole-6-yl)-10H-phenothiazines. The structures of compounds were confirmed by IR, 1H-NMR, 13C NMR and mass spectroscopy and by chem. anal. All the above compounds were screened for their antimicrobial activity against some selected bacteria and fungi such as E. coli, B. subtilis, and S. typhi bacteria and A.niger, A. flavus and F. oxisporium fungi.

Journal of Applicable Chemistry (Lumami, India) published new progress about Antibacterial agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gilfillan, Lynne; Blair, Adele; Morris, Brian J.; Pratt, Judith A.; Schweiger, Lutz; Pimlott, Sally; Sutherland, Andrew published the artcile< Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor>, Recommanded Product: 5-Chloro-2-nitro-4-(trifluoromethyl)aniline, the main research area is dihydrobenzodiazepinone preparation PET SPECT imaging agent.

A focused library of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones containing sites for 11C-, 18F- and 123I-labeling were prepared and evaluated against membrane expressing human recombinant metabotropic glutamate 2 receptor (mGluR2). The compounds are non-competitive antagonists with nanomolar affinity. HPLC evaluation of the physiochem. properties of these compounds identified two candidates for PET and SPECT imaging of mGluR2.

MedChemComm published new progress about Combinatorial library. 35375-74-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3N2O2, Recommanded Product: 5-Chloro-2-nitro-4-(trifluoromethyl)aniline.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Obydennov, Konstantin L.; Kalinina, Tatiana A.; Galieva, Nadezhda A.; Beryozkina, Tetyana V.; Zhang, Yue; Fan, Zhijin; Glukhareva, Tatiana V.; Bakulev, Vasiliy A. published the artcile< Synthesis, Fungicidal Activity and Molecular Docking of 2-Acylamino and 2-Thioacylamino Derivatives of 1H-benzo[d]imidazoles as Anti-Tubulin Agents>, Quality Control of 162046-61-9, the main research area is benzimidazole preparation fungicidal mol docking; 5CA1; antifungal activity; benzimidazoles; carbendazim; molecular docking; nocodazole; tautomerism; tubulin.

This work dealt with the synthesis and evaluation of fungicidal activity of benzimidazole derivatives, which were structural analogs of com. anti-tubulin fungicides. A series of N-acyl and N-thioacyl derivatives of 2-amino-1H-benzo[d]imidazole I [R1 = H, Me, CF3, CO2Et; R2 = H; R3 = H, Me; R4 = Me, Ph, 2-thienyl, etc.; R1R2 = OCF2O; X = O, S] was prepared and their fungicidal activity against 13 strains of phytopathogenic fungi was studied. The most active compounds against the majority of the studied strains were compounds I [R1 = H, R2 = H, R3 = H, R4 = Ph, X = O; R1 = H, R2 = H, R3 = H, R4 = CF3, X = S; R1R2 = OCF2O, R3 = H, R4 = CF3, X = S] and the EC50 values of these compounds were in the range 2.5-20μg/mL. Compound I [R1 = H, R2 = H, R3 = H, R4 = Ph, X = O] showed the highest activity against the P. infestans strain, the growth of which was not suppressed by carbendazim. The formation of ligand-receptor complexes of various tautomeric forms of the studied benzimidazoles with homologous models of β-tubulins of B. cinerea, F. oxysporum, and P. infestans was modeled. Induced fit docking had been used for the simulation. The obtained data suggested the possibility of binding of benzimidazole fungicides to β-tubulin in the “”nocodazole cavity”” in the tautomeric form bearing a double exocyclic C=N bond. The importance of the formation of hydrogen bonds of benzimidazoles with the amino acid residue Val236 along with the Glu198 residue was also revealed in the present study.

Journal of Agricultural and Food Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Quality Control of 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zender, Michael; Klein, Tobias; Henn, Claudia; Kirsch, Benjamin; Maurer, Christine K.; Kail, Dagmar; Ritter, Christiane; Dolezal, Olan; Steinbach, Anke; Hartmann, Rolf W. published the artcile< Discovery and biophysical characterization of 2-amino-oxadiazoles as novel antagonists of PqsR, an important regulator of Pseudomonas aeruginosa virulence>, COA of Formula: C8H6ClN3S, the main research area is aminooxadiazole antibacterial protein PqsR Pseudomonas.

The human pathogen Pseudomonas aeruginosa employs alkyl quinolones for cell-to-cell communication. The Pseudomonas quinolone signal (PQS) regulates various virulence factors via interaction with the transcriptional regulator PqsR. Therefore, the authors considered the development of PqsR antagonists as a novel strategy to limit the pathogenicity of P. aeruginosa. A fragment identification approach using surface plasmon resonance screening led to the discovery of chem. diverse PqsR ligands. The optimization of the most promising hit (5) resulted in the oxadiazole-2-amine 37 showing pure antagonistic activity in Escherichia coli (EC50 = 7.5 μM) and P. aeruginosa (EC50 = 38.5 μM) reporter gene assays. Compound 37 was able to diminish the production of the PQS precursor HHQ in a PqsH-deficient P. aeruginosa mutant. The level of the major virulence factor pyocyanin was significantly reduced in wild-type P. aeruginosa. In addition, site-directed mutagenesis in combination with isothermal titration calorimetry and NMR INPHARMA experiments revealed that the identified ligands bind to the same site of PqsR by adopting different binding modes. These findings might be utilized in a future fragment-growing approach aiming at novel therapeutic options for the treatment of P. aeruginosa infections.

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, COA of Formula: C8H6ClN3S.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics