Category: chlorides-buliding-blocks

Yuan, Yunyun published the artcileDesign, Synthesis, and Biological Evaluation of 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido]morphinan Derivatives as Peripheral Selective μ Opioid Receptor Agents, Computed Properties of 6313-54-8, the publication is Journal of Medicinal Chemistry (2012), 55(22), 10118-10129, database is CAplus and MEDLINE.

Peripheral selective μ opioid receptor (MOR) antagonists could alleviate the symptoms of opioid-induced constipation (OIC) without compromising the analgesic effect of opioids. However, a variety of adverse effects were associated with them, partially due to their relatively low MOR selectivity. A 6β-N-4′-pyridyl substituted naltrexamine derivative, NAP, I (R = 4-pyridyl) was identified previously as a potent and highly selective MOR antagonist mainly acting within the peripheral nervous system. The noticeable diarrhea associated with it prompted the design and synthesis of its analogs in order to study its structure-activity relationship. Among them, compound I (R = 2-methyl-4-pyridyl) showed improved pharmacol. profiles compared to the original lead, acting mainly at peripheral while increasing the intestinal motility in morphine-pelleted mice (ED₅₀ = 0.03 mg/kg). The slight decrease of the ED₅₀ compared to the original lead was well compensated by the unobserved adverse effect. Hence, this compound seems to be a more promising lead to develop novel therapeutic agents toward OIC.

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 C12H12N2O, Computed Properties of 6313-54-8.

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

Yuan, Yunyun published the artcileStructure selectivity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists, Name: 2-Chloroisonicotinic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(18), 5625-5629, database is CAplus and MEDLINE.

Mu opioid receptor antagonists have been applied to target a variety of diseases clin. The current study is designed to explore the structure selectivity relationship (SSR) of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido]morphinan (NAP), a lead compound identified as a selective mu opioid receptor antagonist based on the previous study. Among a series of NAP derivatives synthesized, compounds 6 (NMP) and 9 (NGP) maintained comparable binding affinity, selectivity and efficacy to the lead compound Particularly, the mu opioid receptor selectivity over kappa opioid receptor of NGP was considerably enhanced compared to that of NAP. Overall, the preliminary SSR supported our original hypothesis that an alternate address’ domain may exist in the mu opioid receptor, which favors the ligands carrying a hydrogen bond acceptor and an aromatic system to selectively recognize the mu opioid receptor.

Bioorganic & Medicinal Chemistry Letters 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 C22H18O2, Name: 2-Chloroisonicotinic acid.

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

Al Musaimi, Othman published the artcileBypassing osmotic shock dilemma in a polystyrene resin using the green solvent cyclopentyl methyl ether (CPME): a morphological perspective, Quality Control of 42074-68-0, the publication is Polymers (Basel, Switzerland) (2019), 11(5), 874, database is CAplus and MEDLINE.

The “osmotic shock” phenomenon is the main thing that is responsible for morphol. structure alteration, which can jeopardize the use of a polymer in a chem. process. This is extremely important in solid-phase peptide synthesis (SPPS), which is the method of choice for the preparation of these important biol. active compounds Herein, we have used Hildebrand solubility parameters (d) to investigate the influence of different ethers that are used in the precipitation step of the SPPS using a polystyrene resin. The green cyclopentyl Me ether (CPME) has shown to be slightly superior to 2-methyltetrahydrofurane, which is also a green ether and clearly better than the hazardous di-Et ether and tert-Bu Me ether. These results have been corroborated by scanning electron microscope (SEM) anal. and computational studies. All together, these confirm the adequacy of CPME for being the ether of choice to be used in SPPS.

Polymers (Basel, Switzerland) published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Quality Control of 42074-68-0.

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

Subiros-Funosas, Ramon published the artcileUse of Oxyma as pH modulatory agent to be used in the prevention of base-driven side reactions and its effect on 2-chlorotrityl chloride resin, Category: chlorides-buliding-blocks, the publication is Biopolymers (2012), 98(2), 89-97, database is CAplus and MEDLINE.

The presence of low pKa N-hydroxylamines is beneficial in peptide chem. as they reduce some base-mediated side reactions. Here we evaluated the applicability and buffering capacity of Et 2-cyano-2-(hydroxyimino)acetate (Oxyma) in the prevention of aspartimide/piperidide formation and Pro-based overcoupling and compared it with the performance of HOBt and HOAt. In addition, the compatibility of these additives with the highly acid-labile 2-chlorotrityl chloride resin is examined © 2011 Wiley Periodicals, Inc. Biopolymers, 2011.

Biopolymers published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C4H6N2, Category: chlorides-buliding-blocks.

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

Nafie, Mohamed S. published the artcileControl of ER-positive breast cancer by ERα expression inhibition, apoptosis induction, cell cycle arrest using semisynthetic isoeugenol derivatives, Product Details of C7H6Cl2, the publication is Chemico-Biological Interactions (2022), 109753, database is CAplus and MEDLINE.

New semi-synthetic effective and safe anticancer agents isoeugenol derivatives were synthesized, characterized, and screened for their cytotoxic activity against MCF-7. Moreover, their selective cytotoxicity was assessed against MCF-10A. Three derivatives, 2, 8 and 10 were significantly more active than the reference drug 5-FU with IC50 values of 6.59, 8.07 and 9.63 and 30.93 μM, resp. Also interestingly, these derivatives demonstrated some degree of selectivity to cancer cells over normal cells. Furthermore, derivative 2 was subjected to other in vitro experiments against MCF-7 where it inhibited colony formation by 87.5% and lowered ERα concentration to 395.7 pg/mL compared to 1129 pg/mL in untreated control cells. In continuation of the investigation, the apoptotic activity of compound 2, was assessed where it significantly enhanced total apoptotic cell death by 9.16-fold (18.70% compared to 1.64% for the untreated MCF-7 control cells) and arrested the cell cycle at the G2/M phase. Furthermore, the mol. mechanism of apoptotic activity was investigated at both the gene (RT-PCR) and protein (western plotting) levels where upregulation of pro-apoptotic and down regulation of anti-apoptotic genes was detected. Addnl., compound 2 treatment enhanced the antioxidant (GSH, CAT, SOD) activities. Finally, in vivo experiments verified the effective anticancer activity of compound 2 through inhibition of tumor proliferation by 47.6% compared to 22.9% for 5-FU and amelioration of the hematol., biochem., and histopathol. examinations near normal. In effect, compound 2 can be viewed as a promising semi-synthetic derivative of isoeugenol with some degree of selectivity for management of breast cancer through apoptotic induction and ERα downregulation.

Chemico-Biological Interactions 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, Product Details of C7H6Cl2.

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

Fu, Duo published the artcileMethanesulfinylation of Benzyl Halides with Dimethyl Sulfoxide, Related Products of chlorides-buliding-blocks, the publication is Journal of Organic Chemistry (2020), 85(4), 2752-2758, database is CAplus and MEDLINE.

A phenyltrimethylammonium tribromide-mediated nucleophilic substitution/oxygen transformation reaction of benzyl halides with DMSO has been developed. In this transition-metal-free reaction, DMSO acts as not only a solvent but also a “S(O)Me” source, thus providing a convenient method for the efficient and direct synthesis of various benzyl Me sulfoxides.

Journal of Organic Chemistry 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, Related Products of chlorides-buliding-blocks.

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

Liang, Junqing published the artcileA bench-stable reagent for C-4 selective deuteriodifluoromethylation of azines, Formula: C12H15ClO3, the publication is Chinese Chemical Letters (2022), 33(11), 4817-4821, database is CAplus.

A bench-stable reagent, deuteriodifluoromethyl phosphine (DDFP) from cheap deuterium source for selectivity deuteriodifluoromethylation of azines with a high deuterium incorporation yield was reported. The late-stage modification of complex mols. further confirmed the potential of this reagent for practical applications. This reagent would be expected to find applications in synthesis of isotope-labeled mols. of interests for drug-discovery and related ilucidation of mechanism of action.

Chinese Chemical Letters published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, Formula: C12H15ClO3.

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

Lu, Tong published the artcileDesign and synthesis of C-ring quinoxaline-substituted sinomenine 1,2,3-triazole derivatives via click reactions, Related Products of chlorides-buliding-blocks, the publication is Journal of Chemical Research (2020), 44(11-12), 699-704, database is CAplus.

The synthesis of C-ring quinoxaline-substituted sinomenine 1,2,3-triazole derivatives at the 4-OH via click reactions was accomplished, and a total of 16 novel sinomenine double N-heterocyclic derivatives are obtained in 74%-95% yields. The C-ring is first transformed into a 1,2-diketone structure under the action of hydrochloric acid, and then reacted with o-phenylenediamine to obtain a C-ring quinoxaline-substituted structure. The 4-OH of sinomenine reacted with chloropropyne to give an alkynyl sinomenine, and then reacts with sodium azide and various benzyl chlorides to give the target compounds All the synthesized derivatives were characterized by Fourier-transform IR spectrometry, high resolution mass spectrometry, ¹H NMR, and ¹³C NMR spectroscopy.

Journal of Chemical Research 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, Related Products of chlorides-buliding-blocks.

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

Liu, Xing published the artcileChemoselective Chan-Lam Coupling Reactions between Benzimidazoline-2-thiones and Arylboronic Acids, Product Details of C7H8BClO2, the publication is Journal of Organic Chemistry (2019), 84(18), 11524-11532, database is CAplus and MEDLINE.

An efficient Chan-Lam-type methodol. for the selective synthesis of S-arylbenzimidazoles and N,S-diarylbenzimidazoles was developed. The selectivity was controlled by varying the amount of the catalyst Cu(OAc)₂·H₂O, temperature, and solvent switching. These transformations feature a simple protocol, broad functional group tolerance, high selectivity, and good to excellent yields. It is noteworthy that these reactions represent the first examples of the application of the selective Chan-Lam coupling.

Journal of Organic Chemistry published new progress about 145349-62-8. 145349-62-8 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids, name is 2-Chloro-4-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Product Details of C7H8BClO2.

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

Wang, Xiao-Gang published the artcileA multifunctional metal-organic framework based tumor targeting drug delivery system for cancer therapy, COA of Formula: C19H14Cl2, the publication is Nanoscale (2015), 7(38), 16061-16070, database is CAplus and MEDLINE.

Drug delivery systems (DDSs) with biocompatibility and precise drug delivery are eagerly needed to overcome the paradox in chemotherapy that high drug doses are required to compensate for the poor biodistribution of drugs with frequent dose-related side effects. In this work, we reported a metal-organic framework (MOF) based tumor targeting DDS developed by a one-pot, and organic solvent-free “green” post-synthetic surface modification procedure, starting from the nanoscale MOF MIL-101. Owing to the multifunctional surface coating, premature drug release from this DDS was prevented. Due to the pH responsive benzoic imine bond and the redox responsive disulfide bond at the modified surface, this DDS exhibited tumor acid environment enhanced cellular uptake and intracellular reducing environment triggered drug release. In vitro and in vivo results showed that DOX loaded into this DDS exhibited effective cancer cell inhibition with much reduced side effects.

Nanoscale published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C10H9NO, COA of Formula: C19H14Cl2.

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