Tag: M.W=150-200

Xu, Shengtao published the artcileSynthesis and antimycobacterial evaluation of natural oridonin and its enmein-type derivatives, Related Products of chlorides-buliding-blocks, the publication is Fitoterapia (2014), 300-306, database is CAplus and MEDLINE.

A series of enmein-type derivatives were synthesized and assayed for their antimycobacterial effects. The structures of the synthesized compounds were established by ¹H NMR, ¹³C NMR and mass spectral anal. All the compounds were screened for their antimycobacterial properties against Mycobacterium phlei, Mycobacterium smegmatis and Mycobacterium marinum. Compounds 2, 6g and 6i were found to exhibit potent antimycobacterial activity against M. phlei at a concentration of 0.5 μg/mL, which was comparable to that of pos. drug streptomycin. Furthermore, five compounds were tested against Mycobacterium tuberculosis H₃₇Rv based on the promising preliminary screening results. Among them, compound 10 showed potent activity with IC₅₀ value of 17.1 μg/mL against M. tuberculosis H₃₇Rv strain. Thus, compound 10 could emerge as a promising lead for further research work.

Fitoterapia published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C19H17N3O, Related Products of chlorides-buliding-blocks.

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

Liu, Yang published the artcileDiscovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors, COA of Formula: C6H4ClNO2, the publication is European Journal of Medicinal Chemistry (2017), 122-132, database is CAplus and MEDLINE.

FGF receptors (FGFRs) are tyrosine kinases that are overexpressed in diverse tumors by genetic alterations such as gene amplifications, somatic mutations and translocations. Owing to this characteristic, FGFRs are attractive targets for cancer treatment. It has been demonstrated that most multi-targeted, ATP competitive tyrosine kinase inhibitors are active against FGFRs as well as other kinases. The design of new and more selective inhibitors of FGFRs, which might be reduced off-target and side effects, is a difficult yet significant challenge. The results of the current investigation, show that novel Ponatinib analogs are highly active as FGFR inhibitors and that they possess reduced kinase insert domain receptor (KDR) activities. Observations made in a structure and activity relationship (SAR) investigation led to the development of a promising, orally available lead compound 4-chloro-N-(4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) phenyl)-3-((5-morpholinopyridin-3-yl) ethynyl) benzamide (compound 4, I), which displays a 50-100-fold in vitro selectivity for inhibition of FGFR1-3 over KDR. In addition, biol. evaluation of I showed that it displays significant antitumor activities in FGFR1-amplificated H1581 and FGFR2-amplificated SNU-16 xenograft models.

European Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, COA of Formula: C6H4ClNO2.

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

Chen, Jun published the artcileDiscovery of 1-(4-((3-(4-methylpiperazin-1-yl)propyl)amino)benzyl)-5-(trifluoromethyl)pyridin-2(1H)-one, an orally active multi-target agent for the treatment of diabetic nephropathy, Safety of 3-Chloro-4-fluoronitrobenzene, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(2), 222-229, database is CAplus and MEDLINE.

Oxidative stress, inflammation and fibrosis can cause irreversible damage on cell structure and function of kidney and are key pathol. factors in Diabetic Nephropathy (DN). Therefore, multi-target agents are urgently need for the clin. treatment of DN. Using Pirfenidone as a lead compound and based on the previous research, two novel series (5-trifluoromethyl)-2(1H)-pyridone analogs were designed and synthesized. SAR of (5-trifluoromethyl)-2(1H)-pyridone derivatives containing nitrogen heterocyclic ring have been established for in vitro potency. In addition, compound I, a novel agent that act on multiple targets of anti-DN with IC₅₀ of 90 μM in NIH3T3 cell lines, t_1/2 of 4.89 ± 1.33 h in male rats and LD₅₀ > 2000 mg/kg in mice, has been advanced to preclin. studies as an oral treatment for DN.

Bioorganic & Medicinal Chemistry Letters 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, Safety of 3-Chloro-4-fluoronitrobenzene.

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

Hwang, Soo-Yeon published the artcileField-based rational design of p300 histone acetyltransferase inhibitor and systematic evaluation as an anti-fibrotic agent, Recommanded Product: 3-Chlorobenzylchloride, the publication is Chemical Communications (Cambridge, United Kingdom) (2020), 56(68), 9795-9798, database is CAplus and MEDLINE.

(E)-3-(3-(4-((3-Carbamoylbenzyl)oxy)-3-iodo-5-methoxyphenyl) acryloyl)benzamide (A6) was found to be a potent p300 inhibitor (IC₅₀ = 870 nM) showing a similar binding mode to that of acetyl-CoA, a p300 substrate, and effective anti-fibrotic activity in both TGF-β1-stimulated lung fibroblast cells and bleomycin-induced in vivo lung fibrosis mice.

Chemical Communications (Cambridge, United Kingdom) 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, Recommanded Product: 3-Chlorobenzylchloride.

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

Liu, Jianbo published the artcileSynthesis of N-trifluoromethyl amides from carboxylic acids, Recommanded Product: 2-Chloroisonicotinic acid, the publication is Chem (2021), 7(8), 2245-2255, database is CAplus and MEDLINE.

Here, the synthesis of N-trifluoromethyl amides R¹C(O)NCF₃(R²) [R¹ = Et, cyclohexyl, CH₂CH₂Ph, etc.; R² = Me, allyl, CH₂CH₂Ph, etc.] from carboxylic acid halides and esters under mild conditions via isothiocyanates in the presence of silver fluoride at room temperature was reported. Through this strategy, isothiocyanates were desulfurized with AgF, and then the formed derivative was acylated to afford N-trifluoromethyl amides, including previously inaccessible structures. This method showed broad scope, provides a platform for rapidly generating N-trifluoromethyl amides by virtue of the diversity and availability of both reaction partners and should find application in the modification of advanced intermediates.

Chem published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Recommanded Product: 2-Chloroisonicotinic acid.

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

Neatu, Stefan published the artcilePhotodegradation of yperite over V, Fe and Mn-doped titania-silica photocatalysts, Name: 1,2-Bis(2-chloroethyl)disulfane, the publication is Physical Chemistry Chemical Physics (2008), 10(43), 6562-6570, database is CAplus and MEDLINE.

The photocatalytic decomposition of Yperite (bis(2-chloroethyl)sulfide), a chem. warfare agent, was achieved by using titania-silica catalysts doped with several transition metal ions. The preparation of these catalysts was achieved by impregnation of a titania-silica mixed oxide previously synthesized using a sol-gel route with salts of the doping elements (vanadium, iron, manganese). The above catalysts were characterized using several spectroscopic techniques: FTIR, Raman, DR-UV-Vis, and XPS. The band gap energy was measured for each photocatalytic system. The reaction was carried out in two different types of reactors, i.e. naturally aerated and a closed quartz tube aerated under a constant flow, and using two types of irradiation, UV-Vis and Vis. The investigated systems proved to be extremely active, leading to an almost complete degradation of yperite in 2 h of irradiation An excellent correlation between the photocatalytic performances and the band gap has been found. Based on the characterization data and on the temporal evolution of the reaction products, a reaction mechanism has been suggested. This mechanism considers two distinct pathways for the decomposition of yperite, namely the C-S bond cleavage and the S oxidation

Physical Chemistry Chemical Physics 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, Name: 1,2-Bis(2-chloroethyl)disulfane.

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

Neatu, Stefan published the artcileM/TiO₂/SiO₂ (M = Fe, Mn, and V) catalysts in photodecomposition of sulfur mustard, Quality Control of 1002-41-1, the publication is Applied Catalysis, B: Environmental (2009), 91(1-2), 546-553, database is CAplus.

The photocatalytic decomposition of Sulfur mustard (bis(2-chloroethyl)sulfide) has been examined on Fe-, Mn- and V-doped dispersed TiO₂-SiO₂ catalysts. The catalysts were prepared by successive incipient wetness impregnation. They have been characterized by means of vibrational (FTIR) and optical (UV-vis-NIR in the DRS mode) spectroscopy. Powder XRD, XPS, and BET were used to characterize the structural morphol. and texture. The reaction was carried out in two different types of reactors under both UV- and visible light irradiation The parent TiO₂-SiO₂ catalyst showed activity only under UV irradiation, while the doped ones were active in the decontamination of the persistent Sulfur mustard even under visible light irradiation

Applied Catalysis, B: Environmental 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, Quality Control of 1002-41-1.

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

Prajapati, Neelam P. published the artcileThiazole fused thiosemicarbazones: Microwave-assisted synthesis, biological evaluation and molecular docking study, SDS of cas: 3696-23-9, the publication is Journal of Molecular Structure (2019), 401-410, database is CAplus.

In the present study, series of novel compounds (E)-2-(1-(4-methyl-2-(substituted-phenylamino)thiazol-5-yl)ethylidene)hydrazinecarbothio-amide I (R¹ = H, 3-Me, 4-MeO, etc.; R² = H, cyclohexyl) and (E)-N-cyclohexyl-2-(1-(4-methyl-2-(substituted-phenylamino)thiazol-5-yl)ethylidene)hydrazinecarbothioamide II have been synthesized using microwave irradiation method in high yields. Synthesized compounds were evaluated for their in-vitro antimicrobial, antimalarial and anti-tuberculosis activity as well as in-silico study. The obtained results indicate that compound II (R¹ = 3-Me; R² = cyclohexyl) and II (R¹ = 4-OH; R² = cyclohexyl) were found to be the most potent against S. aureus bacterial strain. Further, the mol. docking study has been performed for all the new compounds with the immune system of S. aureus (PDB ID: 5D1Q) as a target enzyme, and this study validated the exptl. results.

Journal of Molecular Structure 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, SDS of cas: 3696-23-9.

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

Modak, Atanu published the artcilePalladium-Catalyzed Remote meta-Selective C-H Bond Silylation and Germanylation, Synthetic Route of 243139-71-1, the publication is Organometallics (2017), 36(13), 2418-2423, database is CAplus.

Selective meta-C-H activation of arenes until date has met with a limited number of functionalizations. Expanding the horizon of meta-C-H functionalization, herein the authors disclose an unprecedented meta-silylation and germanylation protocol by employing a simple nitrile based directing template. Longer linker between the target site and the directing template were successfully explored for meta-silylation (sp²ε and sp²ζ). Addnl., synthetic utility was demonstrated with several postsynthetic elaborations and with a formal synthesis of TAC101, a promising drug for the treatment of lung cancer.

Organometallics published new progress about 243139-71-1. 243139-71-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 2,4,5-Trifluorobenzyl chloride, and the molecular formula is C7H4ClF3, Synthetic Route of 243139-71-1.

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

Papastavrou, Argyro T. published the artcileUnprecedented Multicomponent Organocatalytic Synthesis of Propargylic Esters via CO₂ Activation, Application of 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is ChemCatChem (2019), 11(21), 5379-5386, database is CAplus.

An efficient and straightforward organocatalytic method for the direct, multicomponent carboxylation of terminal alkynes with CO₂ and organochlorides, towards propargylic esters, is reported for the first time. 1,3-Di-tert-butyl-1H-imidazol-3-ium chloride, a simple, widely-available, stable, and cost-efficient N-heterocyclic carbene (NHC) precursor salt was used as the (pre)catalyst. A wide range of phenylacetylenes, bearing electron-withdrawing or electron-donating substituents, react with allyl chlorides, benzyl chlorides, or 2-chloroacetates, providing the corresponding propargylic esters in low to excellent yields. DFT calculations on the mechanism of this transformation indicate that the reaction is initiated with the formation of an NHC-carboxylate, by addition of the carbene to a mol. of CO₂. Then, the nucleophilic addition of this species to the corresponding chlorides has been computed to be the rate limiting step of the process.

ChemCatChem published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Application of 1-(Chloromethyl)-4-(trifluoromethyl)benzene.

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