Tag: M.W=150-200

Pokhodylo, N. T.; Shyyka, O. Ya.; Obushak, M. D. published the artcile< A Convenient One-Pot Synthesis of 1,5-Disubstituted Tetrazoles Containing an Amino or a Carboxy Group>, Application In Synthesis of 17082-09-6, the main research area is tetrazole preparation.

A convenient method is proposed for constructing the tetrazole ring by a one-pot reaction of amides with phosphorus oxychloride and sodium azide. A series of 1,5-disubstituted tetrazoles containing an amino or a carboxy group, which present interest as buildings blocks for the synthesis of biol. active substances, were obtained.

Russian Journal of Organic Chemistry published new progress about Acid chlorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 17082-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H7ClO, Application In Synthesis of 17082-09-6.

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

Liu, Dachuan; Cheng, Xiu; Wang, Ying published the artcile< Design, synthesis and biological evaluation of benzo[d]thiazole with dimethylpyrazole derivatives>, Application of C7H6Cl2, the main research area is dimethylpyrazolyl benzothiazole preparation antitumor anticonvulsant SAR neurotoxicity; Benzothiazole; Dimethylpyrazol; MTT assay, GABAergic; Maximal Electroshock.

A series of new benzothiazole derivatives containing dimethylpyrazole I [R = H, n-pentyl, benzyl, etc.] were synthesized and evaluated for their anticonvulsant activity, neurotoxicity and cytotoxicity by using the maximal electroshock (MES), rotarod neurotoxicity (TOX) and MTT colorimetric assay. Among the compounds studied, four compounds I [R = Bu, n-pentyl, 2-fluorobenzyl, 2,6-dichlorobenzyl] showed better anticonvulsant than the others at 300 mg/kg and they also showed anticonvulsant activity at the dose of 100 mg/kg. All the synthetic compounds I showed lower neurotoxicity and little cytotoxicity, so that the compounds, which with better activities, also had higher protective index. In particular, the compound I [R = 2-fluorobenzyl] showed better activity with an ED50 value of 160.4 mg/kg and higher protective index (PI) values of 2.74 in the MES test than the standard drugs sodium valproate, which used as pos. controls in this study. After that the compound I [R = 2-fluorobenzyl] demonstrated antagonistic activity against seizures induced by pentylenetetrazol, which proved compound I [R = 2-fluorobenzyl] may be exert activity through effecting GABAergic neurotransmission.

Asian Pacific Journal of Cancer Prevention published new progress about Anticonvulsants. 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Application of C7H6Cl2.

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

Liu, Luxiao; Zhang, Hong-Yu; Yin, Guohui; Zhang, Yuecheng; Zhao, Jiquan published the artcile< Synthesis of N-unsubstituted cyclic imides from anhydride with urea in deep eutectic solvent (DES) choline chloride/urea>, Application In Synthesis of 118-45-6, the main research area is cyclic imide green preparation.

N-Unsubstituted cyclic imides, e.g., I were synthesized in deep eutectic solvent (DES) choline chloride (ChCl)/urea from anhydrides with urea. Urea served as both a DES component and a nitrogen source, which endowed the protocol with advantages of smooth reaction, easy separation of products, simple recovery and recycling of ChCl/urea.

Chemical Papers published new progress about Anhydrides, cyclic Role: RCT (Reactant), RACT (Reactant or Reagent). 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Application In Synthesis of 118-45-6.

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

Xu, Guowei; Yang, Yaqing; Yang, Yanming; Song, Gao; Li, Shanshan; Zhang, Jiajun; Yang, Weimin; Wang, Liang-Liang; Weng, Zhiying; Zuo, Zhili published the artcile< The discovery, design and synthesis of potent agonists of adenylyl cyclase type 2 by virtual screening combining biological evaluation>, Category: chlorides-buliding-blocks, the main research area is adenylate cyclase agonist virtual screening cyclic adenosine monophosphate IL6; Adenylate cyclase; Agonist; Cyclic adenosine monophosphate; Interleukin-6; Virtual screening.

Adenylate cyclases (ACs), play a critical role in the conversion of ATP (ATP) into the second messenger cyclic adenosine monophosphate (cAMP). Studies have indicated that adenylyl cyclase type 2 (AC2) is potential drug target for many diseases, however, up to now, there is no AC2-selective agonist reported. In this research, docking-based virtual screening with the combination of cell-based biol. assays have been performed for discovering novel potent and selective AC2 agonists. Virtual screening disclosed a novel hit compound 8 as an AC2 agonist with EC50 value of 8.10μM on recombinant human hAC2 + HEK293 cells. The SAR (structure activity relationship) based on the derivatives of compound 8 was further explored on recombinant AC2 cells and compound 73 was found to be the most active agonist with the EC50 of 90 nM, which is 160-fold more potent than the reported agonist Forskolin and could selectively activate AC2 to inhibit the expression of Interleukin-6. The discovery of a new class of AC2-selective agonists would provide a novel chem. probe to study the physiol. function of AC2.

European Journal of Medicinal Chemistry published new progress about Drug screening (docking-based virtual screening). 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Category: chlorides-buliding-blocks.

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

Kaur, Sukhvir; Kaur, Manjinder; Kaur, Jasmeen; Bansal, Yogita; Bansal, Gulshan published the artcile< Synthesis, antimicrobial evaluation and chemical stability studies of novel trisubstitued benzimidazoles>, Safety of 1-Chloro-2-(chloromethyl)benzene, the main research area is benzoyl nitrobenzimidazole preparation antibacterial antifungal docking SAR enzyme inhibitor; benzyl nitrobenzimidazole preparation antibacterial antifungal docking SAR enzyme inhibitor.

The current study was aimed at designing, synthesizing and exploring novel benzimidazoles derived compounds I [R = H, 2-Cl, 4-Cl, 4-O2N; R1 = 3-pyridinyl, 2-furyl; X = CH2, C=O] as potential antimicrobial agents. The designed compounds were synthesized from o-phenylenediamine, nicotinic acid, furfuraldehyde and varied benzoyl/benzyl chlorides through a 4-steps synthetic scheme. In-vitro antimicrobial evaluation was carried out by measuring zone of inhibition at different concentrations (1.56-100 μg/mL) of target compounds and streptomycin. Docking anal. was carried out using GlcN-6-P synthase as target enzyme as it was essential for microbial cell wall synthesis and docking studies showed good binding affinity of target compounds toward GlcN-6-P. Hydrolytic stability of the most active compound I [R = 4-Cl; R1 = 3-pyridinyl; X = C=O] in GIT was evaluated in non-enzymic simulated gastric and intestinal fluids through HPLC method. Compounds I [R = H, 2-Cl; R1 = 3-pyridinyl; X = CH2, C=O] exhibited good antibacterial activity, whereas I [R = H, 2-Cl, 4-O2N; R1 = 2-furyl; X = C=O] had potent antifungal properties. Compound I [R = 4-Cl; R1 = 3-pyridinyl; X = C=O] was maximally lethal from the series and equipotent to streptomycin against S. aureus, E. coli and P. aeruginosa with MIC 4.16 ± 1.04, 5.20 ± 1.04 and 10.41 ± 2.08 μg/mL, resp., compound I[R = 2-Cl; R1 = 2-furyl; X= C=O] (MIC 20.83 ± 4.16 μg/mL) was equipotent to fluconazole against C. albicans. Compound I [R = 4-Cl; R1 = 3-pyridinyl; X = C=O] was found stable in non-enzymic simulated gastric and intestinal fluids up to 4h.

Chemica Sinica published new progress about Amides, tertiary Role: PAC (Pharmacological Activity), PRP (Properties), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Safety of 1-Chloro-2-(chloromethyl)benzene.

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

Abbasi, Amin; Nasef, Mohamed Mahmoud; Yahya, Wan Zaireen Nisa; Moniruzzaman, Muhammad; Ghumman, Ali Shaan Manzoor published the artcile< Preparation and characterization of sulfur-vinylbenzyl chloride polymer under optimized reaction conditions using inverse vulcanization>, Category: chlorides-buliding-blocks, the main research area is sulfur vinylbenzyl chloride polymer inverse vulcanization morphol thermal.

Inverse vulcanization offers a new method to make value to this cheap and highly abundant sulfur to produce sulfur-based polymers for different applications. However, most of the research done so far dealt with the characterization of the polymers or their efficiency in certain applications. Here, 4-vinylbenzyl chloride (VBC) is reacted with sulfur under optimized reaction conditions to produce linear sulfur-based polymer. Response Surface Methodol. (RSM) is employed to optimize the reaction conditions in terms of reaction temperature, reaction time, and initial sulfur content. The properties of the polymer produced under optimized conditions are then evaluated using proton NMR (1H NMR), CHNS elemental anal., thermogravimetric anal. (TGA), differential scanning calorimetry (DSC), Fourier transform IR spectroscopy (FTIR), powder X-Ray diffraction (PXRD), and field emission SEM (FESEM). The formation of the polymer and full conversion of the monomers were confirmed by NMR and CHNS anal. The S/VBC polymer showed a uniform morphol. and smooth surface. The polymer demonstrated an amorphous structure with a low Tg (3.7°C), high thermal stability (205°C), and great stability against depolymerization by time. The S/VBC polymer is significant due to its ability for post-functionalization which makes it possible to introduce new applications to sulfur-based polymers.

European Polymer Journal published new progress about Glass transition temperature. 1592-20-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H9Cl, Category: chlorides-buliding-blocks.

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

Mathias, L. J.; Cei, G.; Johnson, R. A.; Yoneyama, M. published the artcile< Poly(thioether imide)s via chloro-displacement polymerization>, Formula: C8H3ClO3, the main research area is polyimide polythioether preparation property; thermal property polyimide polythioether; solubility polyimide polythioether.

Thioether containing polyimides were prepared by displacement of Cl from substituted imides by aromatic and aliphatic sulfur nucleophiles. The all-aromatic monomers and polymers had poor solubility which led to precipitation during synthesis and low mol. weight polymers. However, these polymers were thermally stable to 400° and had Tg 212-233°. The polymers prepared from 1,3-propanedithiol or bis(2-mercaptoethyl) sulfide had good solubility, but lower thermal stability, showing TGA loss onset temperatures of 297° and 298°, resp.

Polymer Bulletin (Berlin) published new progress about Glass transition temperature. 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Formula: C8H3ClO3.

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

Rao, K. Sudarsana; Veeranagaiah, V.; Ratnam, C. V. published the artcile< Structure of phthalamic acids from 4-substituted phthalic anhydrides and aromatic amines>, Application of C8H3ClO3, the main research area is phthalamic acid; decarboxylation phthalamic acid; anhydride phthalic aniline.

Phthalamic acids (I, R = Ph, R1 = Cl; R = Ph, R1 = NO2) were prepared by treatment of the corresponding phthalic anhydride with PhNH2. I were decarboxylated by copper oxide and quinoline to 4-R1C6H4CONHR.

Current Science published new progress about 118-45-6. 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Application of C8H3ClO3.

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

Skidmore, John; Heer, Jag; Johnson, Christopher N.; Norton, David; Redshaw, Sally; Sweeting, Jennifer; Hurst, David; Cridland, Andrew; Vesey, David; Wall, Ian; Ahmed, Mahmood; Rivers, Dean; Myatt, James; Giblin, Gerard; Philpott, Karen; Kumar, Umesh; Stevens, Alexander; Bit, Rino A.; Haynes, Andrea; Taylor, Simon; Watson, Robert; Witherington, Jason; Demont, Emmanuel; Heightman, Tom D. published the artcile< Optimization of Sphingosine-1-phosphate-1 Receptor Agonists: Effects of Acidic, Basic, and Zwitterionic Chemotypes on Pharmacokinetic and Pharmacodynamic Profiles>, Name: Methyl 3-chloro-4-hydroxybenzoate, the main research area is sphingosine phosphate receptor agonist preparation pharmacokinetics.

The efficacy of the recently approved drug fingolimod (FTY720) in multiple sclerosis patients results from the action of its phosphate metabolite on sphingosine-1-phosphate S1P1 receptors, while a variety of side effects have been ascribed to its S1P3 receptor activity. Although S1P and phospho-fingolimod share the same structural elements of a zwitterionic headgroup and lipophilic tail, a variety of chemotypes have been found to show S1P1 receptor agonism. Here the authors describe a study of the tolerance of the S1P1 and S1P3 receptors toward bicyclic heterocycles of systematically varied shape and connectivity incorporating acidic, basic, or zwitterionic headgroups. The authors compare their physicochem. properties, their performance in in vitro and in vivo pharmacokinetic models, and their efficacy in peripheral lymphocyte lowering. The campaign resulted in the identification of several potent S1P1 receptor agonists, e.g. I, with good selectivity vs. S1P3 receptors, efficacy at <1 mg/kg oral doses, and developability properties suitable for progression into preclin. development. Journal of Medicinal Chemistry published new progress about Homo sapiens. 3964-57-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Name: Methyl 3-chloro-4-hydroxybenzoate.

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

Moreira, Natalia M.; Martelli, Lorena S. R.; de Julio, Kiyara I. R.; Zukerman-Schpector, Julio; Opatz, Till; Correa, Arlene G. published the artcile< Copper-Catalyzed One-Pot Synthesis of 3-(N-Heteroarenyl)acrylonitriles through Radical Conjugated Addition of β-Nitrostyrene to Methylazaarenes>, Electric Literature of 5153-70-8, the main research area is heteroarenylacrylonitrile preparation copper catalyst conjugated beta addition nitrostyrene methylazaarene.

A simple procedure for the copper-catalyzed synthesis of 3-(N-heteroaryl)acrylonitriles was developed. Using a combination of Lewis and Bronsted acids, this one-pot procedure undergoes via a radical conjugated addition and dehydration processes, without isolation of any intermediate, affording the acrylonitriles. This diastereoselective approach gave a broad scope of quinazoline derivatives (22 examples) with moderate to good yields and good functional-group tolerance and could be extended to other N-heterocycles such as quinolines and isoquinolines. Based on control experiments, a mechanistic proposal for this new transformation is also presented.

European Journal of Organic Chemistry published new progress about Addition reaction. 5153-70-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClNO2, Electric Literature of 5153-70-8.

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