Month: December 2022

Albrecht, William L. published the artcileBis-basic-substituted polycyclic aromatic compounds. New class of antiviral agents. 6. Bis-basic-substituted fluoranthenes, HPLC of Formula: 4584-49-0, the publication is Journal of Medicinal Chemistry (1974), 17(11), 1150-6, database is CAplus and MEDLINE.

Bis-basic esters, ketones, ethers, and alkanes of fluoranthene, given s.c., had potent antiviral activity against encephalomyocarditis virus in mice. The ketones were the most active when given orally. For example, 3,9-fluoranthenedicarboxylic acid bis[3-(diethylamino)propyl] ester-2HCl (I) [27086-86-8] and 1,1′-(3,9-fluoranthenediyl)bis[2-(dimethylylamino)ethanone]-2HCl (II) [35689-81-7] increased the survival time of infected mice by 1.82- 1.94-fold resp., at 50 mg/kg s.c. I and II were effective against both RNA (Semliki Forest) and DNA (vaccinia) virus infections in mice. I also enhanced the antibody response to sheep erythrocytes. II was prepared by reaction of fluoranthene [206-44-0] with 2-chloroacetyl chloride [79-04-9], followed by Me2NH.

Journal of Medicinal Chemistry published new progress about 4584-49-0. 4584-49-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Salt,Amine,Aliphatic hydrocarbon chain, name is 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, and the molecular formula is C5H13Cl2N, HPLC of Formula: 4584-49-0.

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

Cross, R. Matthew published the artcileOrally Bioavailable 6-Chloro-7-methoxy-4(1H)-quinolones Efficacious against Multiple Stages of Plasmodium, Recommanded Product: 4-Chloro-2-methylphenylboronic acid, the publication is Journal of Medicinal Chemistry (2014), 57(21), 8860-8879, database is CAplus and MEDLINE.

The continued proliferation of malaria throughout temperate and tropical regions of the world has promoted a push for more efficacious treatments to combat the disease. Unfortunately, more recent remedies such as artemisinin combination therapies have been rendered less effective due to developing parasite resistance, and new drugs are required that target the parasite in the liver to support the disease elimination efforts. Research was initiated to revisit antimalarials developed in the 1940s and 1960s that were deemed unsuitable for use as therapeutic agents as a result of poor understanding of both physicochem. properties and parasitol. Structure-activity and structure-property relationship studies were conducted to generate a set of compounds with the general 6-chloro-7-methoxy-2-methyl-4(1H)-quinolone scaffold which were substituted at the 3-position with a variety of Ph moieties possessing various properties. Extensive physicochem. evaluation of the quinolone series was carried out to down-select the most promising 4(1H)-quinolones, P4Q-391 (7), 6-Chloro-7-methoxy-2-methyl-3-(2-methyl-4-(4(trifluoromethoxy)phenoxy)phenyl)-quinolin-4(1H)-one (62), 6-Chloro-3-(6-(2-fluoro-4-(trifluoromethyl)phenyl)pyridin-3-yl)-7-methoxy-2-methylquinolin-4(1H)-one (66), and 6-Chloro-7-methoxy-2-methyl-3-(6-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)quinolin-4(1H)-one(67), which possessed low-nanomolar EC₅₀ values against W2 and TM90-C2B as well as improved microsomal stability. Addnl., in vivo Thompson test results using Plasmodium berghei in mice showed that these 4(1H)-quinolones were efficacious for the reduction of parasitemia at >99% after 6 days.

Journal of Medicinal Chemistry 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, Recommanded Product: 4-Chloro-2-methylphenylboronic acid.

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

Hahn, Elliot F. published the artcileNarcotic antagonists. 4. Carbon-6 derivatives of N-substituted noroxymorphones as narcotic antagonists, Related Products of chlorides-buliding-blocks, the publication is Journal of Medicinal Chemistry (1975), 18(3), 259-62, database is CAplus and MEDLINE.

A series of 11 title compounds was prepared from naloxone [465-65-6] and naltrexone [16590-41-3] by the Wittig reaction, or by reaction with sulfur ylides or alkyllithium reagents. Most of the derivatives had oral potencies superior to the parent compounds in hot plate and tail clip tests in mice. 6-Desoxy-6-methylenenaloxone (I) [42971-34-6] and 6-desoxy-6-methylenenaltrexone (II) [55096-26-9] had the greatest increase in potency over parent compounds Structure-activity relations were discussed.

Journal of Medicinal Chemistry published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C3H9ClOS, Related Products of chlorides-buliding-blocks.

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

Wieting, Joshua M. published the artcilePreparation and catalytic activity of BINOL-derived silanediols, COA of Formula: C10H15ClO3S, the publication is European Journal of Organic Chemistry (2015), 2015(3), 525-533, database is CAplus.

Enantiopure silanediols I (2a–d; 2a, R¹ = R² = H; 2b, R¹ = R² = Ph; 2c, R¹ = H, R² = Ph; 2d, R¹ = Ph, R² = H) derived from BINOL are an innovative family of stereoselective hydrogen-bond donor (HBD) organocatalysts. Silanediols incorporated into a BINOL framework are attractive catalysts, as they are readily accessible and highly customizable. Structural modifications of the BINOL backbone affect the reactivity and selectivity of the silanediol catalysts in the additions of silyl ketene acetals to N-acyl isoquinolinium ions. The best results were obtained when the silanediol scaffold was substituted at the 4,4′- and 6,6′-positions. This report includes details regarding the properties of selected BINOL-based silanediol catalysts, including their acidities, binding constants, and x-ray crystal structures.

European Journal of Organic Chemistry published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C22H21N3O3S, COA of Formula: C10H15ClO3S.

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

Li, Zi-Hao published the artcileN-Hydroxyphthalimide/benzoquinone-catalyzed chlorination of hydrocarbon C-H bond using N-chlorosuccinimide, Synthetic Route of 939-99-1, the publication is Organic & Biomolecular Chemistry (2019), 17(13), 3403-3408, database is CAplus and MEDLINE.

The direct chlorination of C-H bonds has received considerable attention in recent years. In this work, a metal-free protocol for hydrocarbon C-H bond chlorination with com. available N-chlorosuccinimide (NCS) catalyzed by N-hydroxyphthalimide (NHPI) with 2,3-dicyano-5,6-dichlorobenzoquinone (DDQ) functioning as an external radical initiator is presented. Aliphatic and benzylic substituents and also heteroaromatic ones were found to be well tolerated. Both the experiments and theor. anal. indicate that the reaction goes through a process wherein NHPI functions as a catalyst rather than as an initiator. On the other hand, the hydrogen abstraction of the C-H bond conducted by a PINO species rather than the highly reactive N-centered radicals rationalizes the high chemoselectivity of the monochlorination obtained by this protocol as the latter is reactive towards the C(sp³)-H bonds of the monochlorides. The present results could hold promise for further development of a nitroxy-radical system for the highly selective functionalization of the aliphatic and benzylic hydrocarbon C-H.

Organic & Biomolecular 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, Synthetic Route of 939-99-1.

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

Ahlers, Patrick published the artcileDynamic Light Scattering Investigation of the Kinetics and Fidelity of Supramolecular Copolymerizations in Water, Category: chlorides-buliding-blocks, the publication is Macromolecules (Washington, DC, United States) (2017), 50(19), 7712-7720, database is CAplus.

The self-assembly of supramol. copolymers facilitates the preparation of multifunctional materials, with tunable mech., electronic, or bioactive properties. Compared to covalent copolymerization protocols, controlling the mol. weight, stability, and monomer sequence of a multicomponent supramol. copolymer remains limited. Here, we report a light scattering investigation of the charge-regulated supramol. copolymerization in neutral buffer of physiol. ionic strength, supported with electron microscopy and CD spectroscopy experiments Dendritic anionic and cationic peptide comonomers self-assemble into AB-type heterocopolymers with a nanorod-like morphol., a thickness of 11 nm, and a mean length of up to 70 nm. The fidelity in the copolymerization is remarkably high, and excess of either monomer of up to 50 mol % in the feed ratio does not lead to chain stoppering. The narrow length distribution of the copolymers (D < 1.3) and high colloidal stability in physiol. buffer support their applications as biomedical carrier materials.

Macromolecules (Washington, DC, United States) 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, Category: chlorides-buliding-blocks.

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

Nguyen, H. published the artcileCigarette smoke impairs neutrophil respiratory burst activation by aldehyde-induced thiol modifications, Application In Synthesis of 33697-81-3, the publication is Toxicology (2001), 160(1-3), 207-217, database is CAplus and MEDLINE.

Exposure to airborne pollutants such as tobacco smoke is associated with increased activation of inflammatory-immune processes and is thought to contribute to the incidence of respiratory tract disease. We hypothezised that cigarette smoke (CS) could synergize with activated inflammatory/immune cells to cause oxidative injury or result in the formation of unique reactive oxidants. Isolated human neutrophils were exposed to gas-phase CS, and the production of nitrating and chlorinating oxidants following neutrophil stimulation was monitored using the substrate 4-hydroxyphenylacetate (HPA). Stimulation of neutrophils in the presence of CS resulted in a reduced oxidation and chlorination of HPA, suggesting inhibition of NADPH oxidase or myeloperoxidase (MPO), the two major enzymes involved in inflammatory oxidant formation. Peroxidase assays demonstrated that neutrophil MPO activity was not significantly affected after CS-exposure, leaving the NADPH oxidase as a likely target. The inhibition of neutrophil oxidant formation was found to coincide with depletion of cellular GSH, and a similar modification of critical cysteine residues, such as those in NADPH oxidase components, might be involved in reduced respiratory burst activity. As α,β-unsaturated aldehydes such as acrolein have been implicated in thiol modifications by CS, we exposed neutrophils to acrolein prior to stimulation, and observed inhibition of NADPH oxidase activation in relation to GSH depletion. Addnl., translocation of the cytosolic components of NADPH oxidase to the membrane, a necessary requirement for enzyme activation, was inhibited. Protein adducts of acrolein (or related aldehydes) could be detected in several neutrophil proteins, including NADPH oxidase components, following neutrophil exposure to either CS or acrolein. Alterations in neutrophil function by exposure to (environmental) tobacco smoke may affect inflammatory/infectious conditions and thereby contribute to tobacco-related disease.

Toxicology 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

Medusheva, E. O. published the artcilePossibilities of molecular modeling of cellulose in fabrication of therapeutically active textile materials, Synthetic Route of 38146-42-8, the publication is Fibre Chemistry (2009), 41(1), 34-37, database is CAplus.

Highly effective means of stopping capillary-parenchymatous bleeding – one of the main causes of death in people from 1 to 34 years of age in traffic accidents – were developed. Biol. active wound dressings that reduce purulent-necrotic wound cleansing time by 3 times, healing time by 2.5 times, and hospital stays by 6 times were developed.

Fibre Chemistry 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 C38H74Cl2N2O4, Synthetic Route of 38146-42-8.

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

Thurman, E. Michael published the artcileDiscovering metabolites of post-harvest fungicides in citrus with liquid chromatography/time-of-flight mass spectrometry and ion trap tandem mass spectrometry, Quality Control of 67747-01-7, the publication is Journal of Chromatography A (2005), 1082(1), 71-80, database is CAplus and MEDLINE.

In this study, we benefit from the combination of liquid chromatog. (LC)/time-of-flight (TOF) MS accurate mass measurements to generate elemental compositions of ions and LC/ion trap multiple MS (MSⁿ) providing complementary structural information, which is useful for the elucidation of unknown organic compounds at trace levels in complex food extracts We have applied this approach to investigate different citrus fruits extracts, and we have identified two post-harvest fungicides (imazalil and prochloraz), the main degradation product of imazalil ([M + H]⁺, m/z 257) and a non-previously reported prochloraz degradation product ([M + H]⁺, m/z 282). The database-mediated identification of the parent compounds was based on the generated elemental composition obtained from accurate mass measurements and addnl. qual. information from the high resolution chlorine isotopic clusters of both the protonated mols. (imazalil, [M + H]⁺ 297.0556, <0.1 ppm error, 2-Cl; prochloraz, [M + H]⁺ 376.0381, 1.9 ppm error, 3-Cl) and their characteristic fragments ions (imazalil: m/z 255 and 159; prochloraz: m/z 308 and 266). The correlation between the structural information provided by ion trap MS/MS fragmentation pathways of the parent species and the TOF accurate mass elemental composition data of the degradation products were the key to elucidate the structures of the degradation products of both post-harvest fungicides. Finally, where standards were not available (prochloraz), further confirmation was obtained by synthesizing the proposed degradation product by acid hydrolysis of the parent standard and confirmation by LC/TOF-MS.

Journal of Chromatography A 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 C5H13Cl2N, Quality Control of 67747-01-7.

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

Bouton, Jakob published the artcileRevisiting Pyrazolo[3,4-d]pyrimidine Nucleosides as Anti-Trypanosoma cruzi and Antileishmanial Agents, Quality Control of 871332-95-5, the publication is Journal of Medicinal Chemistry (2021), 64(7), 4206-4238, database is CAplus and MEDLINE.

Chagas disease and visceral leishmaniasis are two neglected tropical diseases responsible for numerous deaths around the world. For both, current treatments are largely inadequate, resulting in a continued need for new drug discovery. As both kinetoplastid parasites are incapable of de novo purine synthesis, they depend on purine salvage pathways that allow them to acquire and process purines from the host to meet their demands. Purine nucleoside analogs therefore constitute a logical source of potential antiparasitic agents. Earlier optimization efforts of the natural product tubercidin (7-deazaadenosine) involving modifications to the nucleobase 7-position and the ribofuranose 3′-position led to analogs with potent anti-Trypanosoma brucei and anti-Trypanosoma cruzi activities. In this work, we report the design and synthesis of pyrazolo[3,4-d]pyrimidine nucleosides with 3′- and 7-modifications and assess their potential as anti-Trypanosoma cruzi and antileishmanial agents. One compound was selected for in vivo evaluation in an acute Chagas disease mouse model.

Journal of Medicinal Chemistry published new progress about 871332-95-5. 871332-95-5 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (4-Chloro-3-cyanophenyl)boronic acid, and the molecular formula is C7H5BClNO2, Quality Control of 871332-95-5.

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