Month: December 2022

Albuini-Oliveira, Nathalia M. published the artcileThe influence of ammonium and phosphonium salts on natural rubber vulcanization with experimental and commercial accelerators, Recommanded Product: N-Benzyl-N,N-dibutylbutan-1-aminium chloride, the publication is Polymer Bulletin (Heidelberg, Germany), database is CAplus.

The influence of eight different quaternary ammonium and phosphonium salts on the vulcanization of natural rubber was investigated. The central atom (P or N) of the cation was of minor importance, but the nature of the organic chains greatly affected the rheometrical parameters of the process and the mech. properties of the vulcanizates. Studies of rubber compositions containing binary mixtures of a quaternary salt and the com. accelerators ZDEC, TBBS, TMTD and MBTS showed a synergistic effect, mainly with TBBS and MBTS. With such binary systems, it is possible to reduce the amount of accelerator and improve the vulcanization parameters and the quality of the vulcanized rubber. The anionic complex bis(N-phenylsulfonyldithiocarbimato)zincate(II) (Z), one amine-free exptl. accelerator, was prepared and isolated as tetrabutylammonium (B₂Z) and benzyltriphenylphosphonium (H₂Z) salts. The H₂Z complex salt is a new substance and behaved as an ultra-accelerator, being faster than ZDEC and TMTD. B₂Z was a medium rate accelerator, being faster than TBBS and similar to MBTS. In addition, the tensile and tear strength of the specimens vulcanized with the zinc-dithiocarbimate salts were superior when compared to compositions containing the com. accelerators. The differences in the behavior of B₂Z and H₂Z showed that the zinc-dithiocarbimates are versatile accelerators for natural rubber as the process and the quality of the vulcanizate can be modulated by the choice of the cation.

Polymer Bulletin (Heidelberg, Germany) published new progress about 23616-79-7. 23616-79-7 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst, name is N-Benzyl-N,N-dibutylbutan-1-aminium chloride, and the molecular formula is C19H34ClN, Recommanded Product: N-Benzyl-N,N-dibutylbutan-1-aminium chloride.

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

Vislohuzova, Tetiana published the artcileStudy of biodegradation, biocompatibility and bactericidal activity of film materials with tiamulin fumarate based on polyurethaneurea, Related Products of chlorides-buliding-blocks, the publication is Chemistry & Chemical Technology (2020), 14(3), 318-326, database is CAplus.

The influence of the model biol. medium 199 on the structure and properties of film materials with tiamulin fumarate based on polyurethaneurea containing in its structure the hydrophilic fragments of the copolymer of N-vinylpyrrolidone with vinyl acetate and vinyl alc. has been investigated. According to IR spectroscopy, under the influence of the biol. medium 199 there are processes of biodegradation of polymer materials which are accompanied by a decrease in the intensity of the absorption band νC=O of vinylpyrrolidone ring. It is established that the introduction of tiamulin fumarate into polyurethaneurea facilitates their biodegradation, as evidenced by a decrease of the tensile strength (1.28-2.38 times) and a relative elongation at break (1.36-1.82 times) after incubation in the biol. medium 199 by physico-mech. tests. The tissue culture method has established the biocompatibility of film materials with tiamulin fumarate. According to the results of microbiol. studies, bactericidal properties were observed in relation to the bacteria Staphylococcus aureus and Escherichia coli. It allows using them for production of drainage in abdominal surgery.

Chemistry & Chemical Technology published new progress about 38146-42-8. 38146-42-8 belongs to chlorides-buliding-blocks, auxiliary class Achiral Phase-Transfer Catalysts, name is N1,N10-Bis(2-((2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-N1,N1,N10,N10-tetramethyldecane-1,10-diaminium chloride, and the molecular formula is C4H6O3, Related Products of chlorides-buliding-blocks.

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

Kedari, Chaitanya Kumar published the artcileBiarylmethoxy Nicotinamides As Novel and Specific Inhibitors of Mycobacterium tuberculosis, Computed Properties of 766549-26-2, the publication is ACS Medicinal Chemistry Letters (2014), 5(5), 491-495, database is CAplus and MEDLINE.

A whole cell based screening effort on a focused library from corporate collection resulted in the identification of biarylmethoxy nicotinamides as novel inhibitors of M. tuberculosis (Mtu) H37Rv. The series exhibited tangible structure-activity relationships, and during hit to lead exploration, a cellular potency of 100 nM was achieved, which is an improvement of >200-fold from the starting point. The series is very specific to Mtu and noncytotoxic up to 250 μM as measured in the mammalian cell line THP-1 based cytotoxicity assay. This compound class retains its potency on several drug sensitive and single drug resistant clin. isolates, which indicate that the compounds could be acting through a novel mode of action.

ACS Medicinal Chemistry Letters published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, Computed Properties of 766549-26-2.

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

Beugelmans, Rene published the artcileSynthetic studies towards western and eastern macropolypeptide subunits of kistamicin, Category: chlorides-buliding-blocks, the publication is Tetrahedron (1999), 55(16), 5089-5112, database is CAplus.

Simplified models of the western and eastern macropolypeptide subunits of kistamicin were prepared The western subunit model I (fused bicyclic 16+15 membered ring) was synthesized by sequential intramol. S_NAr reaction and the first 17-membered ring compound as model of the eastern subunit II was obtained by an intramol. Ni⁰ mediated coupling reaction.

Tetrahedron published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Category: chlorides-buliding-blocks.

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

Karimi, Nafiseh published the artcile4-(1-benzyl-1H-benzo[d]imidazol-2-yl)-4-oxo-2-butenoic acid derivatives: design, synthesis and anti-HIV-1 activity, Formula: C7H6Cl2, the publication is Iranian Journal of Pharmaceutical Research (2021), 20(1), 408-417, database is CAplus and MEDLINE.

Integrase, targeted in highly active antiretroviral therapy (HAART), was a crucial enzyme in viral replication. In this study, new benzimidazolyl diketo acid derivatives I [R = Ph, 2-MeC₆H₄, 2-FC₆H₄, etc.] were designed according to required features for inhibitors of HIV-1 integrase. Designed compounds I were evaluated for anti-HIV-1 effects and docking studies indicated that the binding mode of compound I [R = 2-FC₆H₄] was similar to INSTIs. According to the cell-based biol. assay’s results, most of the tested compounds I demonstrated good anti-HIV-1 activity, ranging from 40-90μM concentration with no severe cytotoxicity.

Iranian Journal of Pharmaceutical 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, Formula: C7H6Cl2.

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

Grimova, J. published the artcileTo what extent can results of experimental studies be extrapolated in predicting adverse side effects of drugs in man?, Application In Synthesis of 33697-81-3, the publication is Archives of Toxicology, Supplement (1986), 9(Toxic Interfaces Neurones), 240-3, database is CAplus.

A study of the pharmacokinetics and biotransformation of benzofenac (I) [60736-70-1] was conducted in exptl. animals (rats, rabbits, and dogs) and in human volunteers. The main urinary metabolites in the rat and dog are substances II  [33697-81-3], III  [90276-10-1], and IV [90276-12-3], and in the rabbit and man II and II. Man differs from animals in the quantities of the individual metabolites. Some metabolites were prepared and tested for embryotoxicity in chicken and rat embryos. Of all the metabolites, metabolite IV is responsible for the embryotoxic action of I. This metabolite never occurs in the rabbit or man. These results substantiate the necessity of carrying out concurrent comparative pharmacokinetic and biotransformation studies of new drugs in exptl. animals and man during the preclin. research stage.

Archives of Toxicology, Supplement published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Application In Synthesis of 33697-81-3.

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

Fattori, Daniela published the artcileDesign and synthesis of novel sulfonamide-containing bradykinin hB₂ receptor antagonists. 2. synthesis and structure-activity relationships of α,α-cycloalkylglycine sulfonamides, HPLC of Formula: 6249-56-5, the publication is Journal of Medicinal Chemistry (2007), 50(3), 550-565, database is CAplus and MEDLINE.

Recently, the design and synthesis of a class of selective nonpeptide bradykinin (BK) B₂ receptor antagonists (J. Med. Chem. 2006, 3602-3613) was reported. This work led to the discovery of MEN 15442 (I), an antagonist with subnanomolar affinity for the human B2 receptor (hB2R), which also displayed significant and prolonged activity in vivo (for up to 210 min) against BK-induced bronchoconstriction in the guinea-pig at a dose of 300 nmol/kg (it), while demonstrating only a slight effect on BK-induced hypotension. Herein, the further optimization of this series of compounds aimed at maximizing the effect on bronchoconstriction and minimizing the effect on hypotension, with a view to developing topically delivered drugs for airway diseases, is described. It was found that MEN 16132 (II), after intratracheal or aerosol administration, inhibited, in a dose-dependent manner, BK-induced bronchoconstricton in the airways, while showing minimal systemic activity. This compound was selected as a preclin. candidate for the topical treatment of airway diseases involving kinin B2 receptor stimulation.

Journal of Medicinal Chemistry published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C7H16ClNO2, HPLC of Formula: 6249-56-5.

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

Kamdem, Nestor published the artcileSmall-molecule inhibitors of the PDZ domain of Dishevelled proteins interrupt Wnt signalling, Computed Properties of 61551-49-3, the publication is Magnetic Resonance (2021), 2(1), 355-374, database is CAplus.

Dishevelled (Dvl) proteins are important regulators of the Wnt signalling pathway, interacting through their PDZ domains with the Wnt receptor Frizzled. Blocking the Dvl PDZ-Frizzled interaction represents a potential approach for cancer treatment, which stimulated the identification of small-mol. inhibitors, among them the anti-inflammatory drug Sulindac and Ky-02327. Aiming to develop tighter binding compounds without side effects, we investigated structure-activity relationships of sulfonamides. X-ray crystallog. showed high complementarity of anthranilic acid derivatives in the GLGF loop cavity and space for ligand growth toward the PDZ surface. Our best binding compound inhibits Wnt signalling in a dose-dependent manner as demonstrated by TOP-GFP assays (IC50 ∼ 50 μM) and Western blotting of β-catenin levels. Realtime PCR showed reduction in the expression of Wnt-specific genes. Our compound interacted with Dvl-1 PDZ (KD = 2.4 μM) stronger than Ky-02327 and may be developed into a lead compound interfering with the Wnt pathway.

Magnetic Resonance published new progress about 61551-49-3. 61551-49-3 belongs to chlorides-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 5,6,7,8-Tetrahydronaphthalene-2-sulfonyl chloride, and the molecular formula is C10H11ClO2S, Computed Properties of 61551-49-3.

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

Grassi, Luigi published the artcileAn explorative study towards the chemical synthesis of the immunoglobulin G1 Fc CH3 domain, Formula: C19H14Cl2, the publication is Journal of Peptide Science (2018), 24(12), n/a, database is CAplus and MEDLINE.

Monoclonal antibodies, fusion proteins including Ig fragment c (Ig Fc) CH2-CH3 domains, and engineered antibodies are prominent representatives of an important class of drugs and drug candidates, which are referred to as biotherapeutics or biopharmaceuticals. These recombinant proteins are highly heterogeneous due to their glycosylation pattern. In addition, enzyme-independent reactions, like deamidation, dehydration, and oxidation of sensitive side chains, may contribute to their heterogeneity in a minor amount To investigate the biol. impact of a spontaneous chem. modification, especially if found to be recurrent in a biotherapeutic, it would be necessary to reproduce it in a homogeneous manner. Here, we undertook an explorative study toward the chem. synthesis of the IgG1 Fc CH3 domain, which has been shown to undergo spontaneous changes like succinimide formation and methionine oxidation We used Fmoc-solid-phase peptide synthesis (SPPS) and native chem. ligation (NCL) to test the accessibility of large fragments of the IgG1 Fc CH3 domain. In general, the incorporation of pseudoproline dipeptides improved the quality of the crude peptide precursors; however, sequences larger than 44 residues could not be achieved by standard stepwise elongation with Fmoc-SPPS. In contrast, the application of NCL with Cys residues, which were either native or introduced ad hoc, allowed the assembly of the C-terminal IgG1 Fc CH3 sequence 371 to 450. The syntheses reported here show advantages and limitations of the chem. approaches chosen for the preparation of the synthetic IgG1 Fc CH3 domain and will guide future plans toward the synthesis of both the native and selectively modified full-length domain.

Journal of Peptide Science 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, Formula: C19H14Cl2.

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

Fu, Qiuguo published the artcileBioaccumulation, Biotransformation, and Synergistic Effects of Binary Fungicide Mixtures in Hyalella azteca and Gammarus pulex: How Different/Similar are the Two Species?, SDS of cas: 67747-01-7, the publication is Environmental Science & Technology (2018), 52(22), 13491-13500, database is CAplus and MEDLINE.

Aquatic organisms are consistently exposed to a mixture of micropollutants that can bioaccumulate, undergo biotransformation, and may exert mixture effects. However, little is known on the underlying mechanisms and species-specificity. Herein the authors investigated bioaccumulation, biotransformation and synergistic effects of azole (i.e., prochloraz) and strobilurin (i.e., azoxystrobin) fungicides in the two aquatic invertebrate species, Hyalella azteca and Gammarus pulex. Bioaccumulation of azoxystrobin was similar, whereas bioaccumulation of prochloraz was slightly different in the two species but was still significantly below the REACH criteria for bioaccumulative substances. Similar biotransformation patterns were observed in both species, and only a few unique biotransformation reactions were detected in H. azteca such as malonyl-glucose and taurine conjugation. Toxicokinetic modeling addnl. indicated that biotransformation is a more important elimination pathway in H. azteca. In mixtures, no-observed-adverse-effect levels of prochloraz decreased the LC50s of azoxystrobin in both species which correlated well with increased internal azoxystrobin concentrations This synergistic effect is partly due to the inhibition of cytochrome P 450 monooxygenases by prochloraz which subsequently triggered the reduced biotransformation of azoxystrobin (lower by 5 folds in H. azteca). The largely similar responses in both species suggest that the easier-to-cultivate H. azteca is a promising representative of invertebrates for toxicity testing.

Environmental Science & Technology published new progress about 67747-01-7. 67747-01-7 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Ether,Benzene Compounds, name is N-(2-(2,4,6-Trichlorophenoxy)ethyl)propan-1-amine, and the molecular formula is C11H14Cl3NO, SDS of cas: 67747-01-7.

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