Tag: M.W=150-200

Tayade, D. T. published the artcileDesign, synthesis, characterization and anti-microbial screening of some novel thiocarbamidochalcones, Quality Control of 3696-23-9, the publication is American Journal of PharmTech Research (2016), 6(3), 605-612, database is CAplus.

Interactions of (2E)-1-(4-chlorophenyl)-3-(3,4 dimethoxyphenyl)prop-2-en-1-one with various substituted thioureas such as thiourea, N-phenylthiourea, 2-chlorophenylthiourea, 3-chlorophenylthiourea and 4-chlorophenylthiourea in presence of isopropanol as a medium. The products isolated in these reactions were characterized on the basis of conventional elemental anal., chem. characteristics and spectral data. All the synthesized compounds screened against various microorganisms such as gram pos. Staphylococcus aureus, gram-neg. Escherichia coli. Ciprofloxacin was used as a standard drug for the antimicrobial screening.

American Journal of PharmTech Research published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C6H4ClNO2, Quality Control of 3696-23-9.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Hayakawa, Ichiro published the artcileStructure-activity relationship study of gatastatin based on the topliss tree approach, Application In Synthesis of 620-20-2, the publication is Heterocycles (2019), 99(1), 238-247, database is CAplus.

Various analogs of gatastatin I [Ar = 3-ClC₆H₄, 4-MeC₆H₄, 4-^tButC₆H₄, etc.], a γ-tubulin-specific inhibitor, were designed and synthesized by systematically optimizing the aromatic ring at the O⁷-benzyl group in accordance with an operational Topliss tree, and their biol. activities were evaluated. Some derivatives showed stronger cytotoxicity against HeLa cells than gatastatin. Especially, the cytotoxicity of the I [Ar = 3-ClC₆H₄] derivative was about 18-fold stronger than that of gatastatin. However, these derivatives did not exhibit binding ability to the yeast γ-tubulin small complex or inhibitory activity against α,β-tubulin polymerization These results suggested that γ-tubulin strongly recognized the unsubstituted Ph ring of the O⁷-benzyl group in gatastatin.

Heterocycles published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C7H6Cl2, Application In Synthesis of 620-20-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Huang, Xiaohua published the artcileDiscovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors, Formula: C7H8BClO2, the publication is ACS Medicinal Chemistry Letters (2011), 2(8), 632-637, database is CAplus and MEDLINE.

A novel series of non-ATP-competitive MK2 inhibitors based on a furan-2-carboxyamide scaffold was discovered through high-throughput screening using the affinity selection-mass spectrometry-based Automated Ligand Identification System platform. Medicinal chem. efforts optimized the initial screening hit to lead-like compounds with significant improvements in biochem. and cellular potencies, while maintaining excellent kinase selectivity and in vitro pharmacokinetic properties. Biophys. and biochem. studies confirmed the unique non-ATP-competitive binding mode of this series and suggested that highly selective inhibitors of MK2 should be feasible by targeting the outside ATP pocket.

ACS Medicinal Chemistry Letters published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Formula: C7H8BClO2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Lugovoi, Yu. M. published the artcileKinetics of competitive addition of methyldichlorosilane to 1-hexene and to acetone, HPLC of Formula: 14799-94-1, the publication is Reaction Kinetics and Catalysis Letters (1989), 39(2), 379-85, database is CAplus.

The competitive addition of MeSiHCl₂ to 1-hexene and acetone (initiated by γ-irradiation) has been studied. The relative rate constant depends on acetone concentration and does not obey the Arrhenius equation. A possible explanation is the complexation of methyldichlorosilyl radicals with acetone mols.

Reaction Kinetics and Catalysis Letters published new progress about 14799-94-1. 14799-94-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Dichloro(hexyl)(methyl)silane, and the molecular formula is C7H16Cl2Si, HPLC of Formula: 14799-94-1.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Nishad, Ravi K. published the artcileDesign and Synthesis of 2-Substituted Benzothiazole Derivatives as Antioxidant and Antimicrobial Agents, Application of 1-(4-Chlorophenyl)thiourea, the publication is Current Bioactive Compounds (2020), 16(8), 1242-1248, database is CAplus.

An upsurge in the number of antibiotic-resistant microbial infections has warranted the discovery and development of new antibiotics. This is a matter of great concern for effective therapy for a search of novel antimicrobial agents. Literature has a number of reports of involvement of oxidative stress due to an imbalance between the generation and neutralization of free radicals in many diseases. Heterocyclic compounds have been involved in the treatment of various disorders. Benzothiazole is one such heterocyclic nucleus having benzene ring merged with the thiazole ring. Among the various substitutions possible in this nucleus, substitutions at position-2 have already been reported with potential bioactivities. Thus, different substituted compounds have been synthesized which could serve as antimicrobials and antioxidants. Benzothiazole derivatives (B₁-B₇) were synthesized by two-step reactions and the structures were confirmed through IR, mass and NMR spectroscopy. The compounds were evaluated for in vitro antioxidant and antimicrobial activities using standard methods. The results of antibacterial and antifungal activity showed that compound B₄ exhibited maximum activity against all the tested strains of microorganisms with the zone of inhibition 17.1-18.5 mm and MIC value 1.1-1.5μg/mL. Compound B₅ exhibited potent antioxidant activity. The compounds substituted with halogen on the aryl ring showed increased antimicrobial activity as seen in the case of compound B₄ (6-fluoro). The compounds substituted with a hydroxyl group (B₅) exhibited good antioxidant activity.

Current Bioactive Compounds published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Application of 1-(4-Chlorophenyl)thiourea.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Li, Shan published the artcileDiscovery of Hexahydrofuro[3,2-b]furans as New Kinase-Selective and Orally Bioavailable JAK3 Inhibitors for the Treatment of Leukemia Harboring a JAK3 Activating Mutant, COA of Formula: C6H3ClFNO2, the publication is Journal of Medicinal Chemistry (2022), 65(15), 10674-10690, database is CAplus and MEDLINE.

Janus kinase 3 (JAK3) is a potential target for the treatment of hematol. malignancies. Herein, we report the discovery of a series of new orally bioavailable irreversible JAK3 kinase inhibitors. The representative compound 12n (I) potently inhibited JAK3 kinase activity with an IC₅₀ value of 1.2 nM and was more than 900-fold selective over JAK1, JAK2, and Tyk2. Cell-based assays revealed that 12n significantly suppressed phosphorylation of JAK3 and the downstream effectors STAT3/5 and also robustly restrained proliferation of BaF3 cells transfected with JAK3^M511I activating mutation and human leukemia U937 cells harboring JAK3^M511I with IC₅₀ values of 22.9 and 20.2 nM, resp. More importantly, 12n showed reasonable pharmacokinetic (PK) properties, and oral administration of 12n at a dose of 50 mg/kg twice daily led to tumor regression in a U937 cell inoculated xenograft mouse model. Thus, 12n represents a promising lead compound for further optimization to discover new therapeutic agents for hematol. malignancies.

Journal of Medicinal Chemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, COA of Formula: C6H3ClFNO2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Sahu, Meeta published the artcileDesign, synthesis and evaluation of newer 5,6-dihydropyrimidine-2(1H)-thiones as GABA-AT inhibitors for anticonvulsant potential, Synthetic Route of 3696-23-9, the publication is Bioorganic Chemistry (2017), 166-178, database is CAplus and MEDLINE.

Several new 5,6-dihydropyrimidine-2(1H)-thione derivatives have been prepared and investigated for their potencies for anticonvulsant activity against maximal electroshock (MES) and s.c. pentylenetetrazole (scPTZ) test in mice. The acute neurotoxicity was measured by rotarod test. Compounds 3c (1-(4-methoxyphenyl)-4,6-diphenyl-5,6-dihydropyrimidine-2(1H)-thione) and 3l (4-(4-hydroxyphenyl)-1-(2-nitrophenyl)-6-phenyl-5,6-dihydropyrimidine-2(1H)-thione) were found active in both of the animal models. Further, in vitro GABA-AT enzyme activity assay was carried out to investigate the possible mechanism of action through GABA-AT inhibition. The most potent compounds 3c and 3l showed inhibitory potency (IC₅₀) of 18.42 μM and 19.23 μM, resp. The mol. modeling was performed for all the synthesized compounds The docking results were found in concordant with the observed animal studies.

Bioorganic Chemistry published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Synthetic Route of 3696-23-9.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Cragin, David W. published the artcileThe synthesis of 2-¹⁴C-N-nitrosothiazolidine, Computed Properties of 1002-41-1, the publication is Journal of Labelled Compounds and Radiopharmaceuticals (1989), 27(7), 777-81, database is CAplus.

Title compound I, labeled with ¹⁴C in the 2-position, was prepared in 30.7% yield by cyclocondensation of NH₂CH₂CH₂SH with ¹⁴C-labeled CH₂O in H₂O at pH = 8, followed by nitrosylation of the thiazolidine with NaNO₂ at pH = 4.5 adjusted with H₂SO₄. Adjustment of the pH in the latter step with HCl forms many disulfide byproducts.

Journal of Labelled Compounds and Radiopharmaceuticals published new progress about 1002-41-1. 1002-41-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is 1,2-Bis(2-chloroethyl)disulfane, and the molecular formula is C4H8Cl2S2, Computed Properties of 1002-41-1.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Yamamoto, Kosuke published the artcileRational Design and Synthesis of [5]Helicene-Derived Phosphine Ligands and Their Application in Pd-Catalyzed Asymmetric Reactions, Quality Control of 209919-30-2, the publication is Scientific Reports (2016), 36211pp., database is CAplus and MEDLINE.

A series of novel optically active [5]helicene-derived phosphine ligands I and II were synthesized. Despite their structural similarities, I and II exhibited particularly different characteristics in their use as chiral ligands. I Was highly effective in the asym. allylation of indoles with 1,3-diphenylallyl acetate, afforded substituted indoles III [R = H, Me, Ph; R¹ = H, Br, Me, OMe; R² = H, Me] (up to 99% ee), and in the etherification of alcs., afforded allylic ethers IV [R³ = Et, allyl, Bn, etc.] (up to 96% ee). In contrast, II was highly effective in the stereocontrol of helical chirality in Suzuki-Miyaura coupling (SMC) reaction, afforded biaryls V [R⁴ = Me, Et; R⁵ = H, Me, Cl, OMe; R⁶ = H, Me] (up to 99% ee). D. functional theory anal. was employed to propose a model that accounts for the origin of the enantioselectivity in these reactions.

Scientific Reports published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C2H2N4O2, Quality Control of 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Thakare, Prashant published the artcileSynthesis and biological evaluation of novel 4-(6-substituted quinolin-4-yl)-N-aryl thiazol-2-amine derivatives as potential antimicrobial agents, HPLC of Formula: 3696-23-9, the publication is Journal of Heterocyclic Chemistry (2021), 58(9), 1867-1877, database is CAplus.

Cyclocondensation reaction of 4-(2-bromoacetyl)quinolin-1-ium bromide with substituted arylthiourea, afforded 4-(6-substituted quinolin-4-yl)-N-aryl/pyridyl thiazol-2-amine I (R = H, Cl, F, Br; Ar = C₆H₄NH₂, 2-pyridylamine, 4-MeC₆H₄NH₂, etc.). These newly synthesized derivatives were evaluated for in vitro antibacterial activity against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388) (Gram-neg. strains), Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178) (Gram-pos. strains) and in vitro antifungal activity against Aspergillus niger (ATCC 504) and Candida albicans (NCIM 3100). Most of the compounds showed moderate to good antibacterial activity against S. albus. Ten derivatives showed moderate to good activity against A. niger. N-[4-(Quinolin-4-yl)-1,3-thiazol-2-yl]pyridin-2-amine presented comparable activity against A. niger with respect to standard drug Rouconazole.

Journal of Heterocyclic Chemistry published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C16H12O, HPLC of Formula: 3696-23-9.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics