Tag: M.W=150-200

Fujii, Shinya published the artcileStructural Development of Salicylanilide-Based SPAK Inhibitors as Candidate Antihypertensive Agents, Recommanded Product: 3-Chloro-4-fluoronitrobenzene, the publication is ChemMedChem (2021), 16(18), 2817-2822, database is CAplus and MEDLINE.

Hypertension is an important target for drug discovery. We have focused on the with-no-lysine kinase (WNK)-oxidative stress-responsive 1 (OSR1) and STE20/SPS1-related proline-alanine-rich protein kinase (SPAK)-NaCl cotransporter (NCC) signal cascade as a potential target, and we previously developed a screening system for inhibitors of WNK-OSR1/SPAK-NCC signaling. Herein we used this system to examine the structure-activity relationship (SAR) of salicylanilide derivatives as SPAK kinase inhibitors. Structural design and development based on our previous hit compound, aryloxybenzanilide derivative I, and the veterinary anthelmintic closantel (II) led to the discovery of compound III as a potent SPAK inhibitor with reduced toxicity. Compound III decreased the phosphorylation level of NCC in mouse kidney in vivo, and appears to be a promising lead compound for a new class of antihypertensive drugs.

ChemMedChem 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, Recommanded Product: 3-Chloro-4-fluoronitrobenzene.

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

Fujii, Shinya published the artcileStructural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK inhibitors blocking WNK kinase signaling, Formula: C6H3ClFNO2, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(17), 127408, database is CAplus and MEDLINE.

We report here structural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK (STE20/SPS1-related proline/alanine-rich kinase) inhibitors. Abnormal activation of the signal cascade of with-no-lysine kinase (WNK) with OSR1 (oxidative stress-responsive kinase 1)/SPAK and NCC (NaCl cotransporter) results in characteristic salt-sensitive hypertension, and therefore inhibitors of the WNK-OSR1/SPAK-NCC cascade are candidates for antihypertensive drugs. Based on the structure of lead compound 2, we examined the SAR of N-(4-phenoxyphenyl)benzamide derivatives, and developed compound 20l as a potent SPAK inhibitor. Compounds 201 is a promising candidate for a new class of antihypertensive drugs.

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, Formula: C6H3ClFNO2.

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

Jung, Sung-Hyun published the artcilePalladium-Catalyzed Direct Synthesis, Photophysical Properties, and Tunable Electroluminescence of Novel Silicon-Based Alternating Copolymers, Application In Synthesis of 14799-94-1, the publication is Macromolecules (2000), 33(25), 9277-9288, database is CAplus.

A new class of silicon-based alternating copolymers with a uniform π-conjugated segment regulated by organosilicon units was synthesized using the Heck reaction between distyrylsilane monomers and appropriate arylene dibromides. The incorporation of organosilicon units with the aromatic or aliphatic groups on the silicon atoms into π-conjugated systems improved their processability and interrupted the π-conjugation length. They could be spin-cast onto various substrates to give highly transparent homogeneous thin films. Their glass transition temperatures were in the range 94-127 °C. They show strong absorption bands around 356-416 nm, which corresponds to the π-π* transition of the conjugated segments. The maximum photoluminescence appeared around 440-526 nm in the blue or green emission region. Their optical properties depend on the arylene dibromides in the Heck reaction. The single-layered light-emitting diode of an Al/SiPhPPV or SiHMPPV/ITO glass exhibits a threshold voltage of 10-12 V from the I-V curve. The electroluminescence (EL) of the SiPhPPV or SiHMPPV gives an emissive peak at 450 nm. Furthermore, the multilayered light-emitting diodes of an Al/LiAl/SiPhPVK/PANI/ITO glass and an Al/LiAl/SiPhFPV or SiHMFPV/ITO glass shows a threshold voltage of 6-12 V. The EL device based on SiPhPVK exhibits the blue emissive color at 467 nm, when an operating voltage of 7 V was applied. When an operating voltage of 11 V was applied, however, the EL device emits a white color. The EL spectra of the SiPhFPV and SiHMFPV polymers, obtained at an applied voltage of 12 V, show two strong peaks in the blue emissive region as well as in the green region.

Macromolecules 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, Application In Synthesis of 14799-94-1.

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

Kim, Mi-hyun published the artcileStructure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells, Recommanded Product: 2-Chloroisonicotinic acid, the publication is Bioorganic & Medicinal Chemistry (2011), 19(6), 1915-1923, database is CAplus and MEDLINE.

The synthesis of a novel series of N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl) amide derivatives 6a-o, 7a-s and their antiproliferative activities against A375P melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard Among them, N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(3-(4-chloro-3-(trifluoromethyl)phenyl) ureido)-2-methylbenzamide 7c exhibited potent activities (GI₅₀ = 0.27 μM). Especially, 7c was found to be a potent and selective B-Raf V600E and C-Raf inhibitor (IC₅₀ = 0.26 μM, IC₅₀ = 0.11 μM, resp.), showing a possibility as melanoma therapeutics.

Bioorganic & 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, Recommanded Product: 2-Chloroisonicotinic acid.

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

Cho, Yongsung published the artcileThe SAR analysis of TRPV1 agonists with the α-methylated B-region, Name: 3-Chloro-4-hydroxyphenylacetic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(16), 5227-5231, database is CAplus and MEDLINE.

A series of TRPV1 agonists with amide, reverse amide, and thiourea groups in the B-region and their corresponding α-methylated analogs were investigated. Whereas the α-methylation of the amide B-region enhanced the binding affinities and potencies as agonists, that of the reverse amide and thiourea led to a reduction in receptor affinity. The anal. indicated that proper hydrogen bonding as well as steric effects in the B-region are critical for receptor binding.

Bioorganic & Medicinal Chemistry Letters 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, Name: 3-Chloro-4-hydroxyphenylacetic acid.

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

Lee, Jung Kul published the artcileModification of chitosan to improve its hypocholesterolemic capacity, SDS of cas: 4584-49-0, the publication is Bioscience, Biotechnology, and Biochemistry (1999), 63(5), 833-839, database is CAplus and MEDLINE.

Cholestyramine is the most widely used bile acid sequestrant in the treatment of hypercholesterolemia. However, cholestyramine has unpleasant side effects as a consequence of its hydrophobic backbone. Therefore, high-capacity bile acid sequestering biopolymers with cationic chitosan derivatives were developed, because electrostatic interactions are important for binding with bile acid anions. Dialkylaminoalkylation and reductive amination of chitosan were done to add dialkylaminoalkyl and an addnl. free amino group at a hydroxyl site in the chitosan backbone resp. and the aminoderivatized chitosan derivatives were quaternized with Me iodide to produce a cationic polyelectrolyte. The in vitro bile acid binding capacity of the chitosan derivatives in aqueous NaCl was measured by reversed-phase HPLC. The binding capacities of sodium glycocholate (a major bile acid) to chitosan, DEAE-chitosan, quaternized DEAE-chitosan, and cholestyramine were 1.42, 3.12, 4.06, and 2.78 mmol/g resin, resp. With quaternized DEAE-chitosan, the bile acid binding capacity increased ∼50% over that of cholestyramine. The bile acid binding capacity of dialkylaminoalkyl chitosan derivatives increased with the number of carbons in the alkyl groups, indicating that hydrophobic interaction is a secondary factor for the sequestration of bile acids.

Bioscience, Biotechnology, and Biochemistry 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, SDS of cas: 4584-49-0.

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

Kang, Dong Wook published the artcileHalogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin, HPLC of Formula: 33697-81-3, the publication is Bioorganic & Medicinal Chemistry (2010), 18(22), 8092-8105, database is CAplus and MEDLINE.

As an extension of our anal. of the effect of halogenation on thiourea TRPV1 agonists, we have now modified selected 4-hydroxy(or 4-amino)-3-methoxyphenyl acetamide TRPV1 agonists by 5- or 6-halogenation on the aromatic A-region and evaluated them for potency for TRPV1 binding and regulation and for their pattern of agonism/antagonism (efficacy). Halogenation shifted the functional activity at TRPV1 toward antagonism with a greater extent of antagonism as the size of the halogen increased (I > Br > Cl), as previously observed for the thiourea series. The extent of antagonism was greater for halogenation at the 5-position than at the 6-position, in contrast to SAR for the thiourea series. In this series, compounds 55 (I) and 75 showed the most potent antagonism, with K _i (ant) = 2.77 and 2.19 nM, resp., on rTRPV1 expressed in Chinese hamster ovary cells. The compounds were thus ca. 40-60-fold more potent than 6′-iodononivamide.

Bioorganic & Medicinal Chemistry 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, HPLC of Formula: 33697-81-3.

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

Jankowiak, Aleksandra published the artcile4-Substituted 1-Acyloxypyridine-2(1 H)-thiones: Experimental and Computational Studies of the Substituent Effect on Electronic Absorption Spectra, SDS of cas: 6313-54-8, the publication is Journal of Organic Chemistry (2009), 74(19), 7441-7448, database is CAplus and MEDLINE.

A series of eight 4-substituted 1-(adamantane-1-carbonyloxy)-4-X-pyridine-2(1H)-thiones (1, X = H, OC₇H₁₅, Me, CF₃, SC₃H₇, CN, COOMe, and Cl) was prepared and characterized by UV-vis spectroscopy in MeCN and cyclohexane. The observed lowest energy transition, designated as π_CS → π*_ring, exhibits a substantial substituent effect and λ_max ranges from 333 (X = OC₇H₁₅) to 415 nm (X = CN). Exptl. λ_max values for all esters except for 1b (X = OC₇H₁₅) correlate with the σ_p^– parameter (ρ = 0.41 ± 0.03, r² = 0.95). In contrast, the energy of the absorption band at about 295 nm, designated as π_CS → π*_CS, is practically substituent independent. Both absorption bands exhibit a modest neg. solvatochromic effect. The exptl. absorption energies correlate better with excitation energies calculated for N-acetyloxy analogs 2 with the ZINDO//DFT than with the TD-DFT//DFT method. Calculations for a series of 12 N-acetates 2 predict the most blue-shifted π → π* transition for the alkoxy substituent and most red-shifted for the NO₂ group relative to the parent 2a (X = H).

Journal of Organic 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, SDS of cas: 6313-54-8.

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

Tamao, Kohei published the artcileCoupling of (amino)alkylchlorosilanes with lithium: new access to symmetrical di- and tetrafunctional alkyldisilanes, Product Details of C7H16Cl2Si, the publication is Organometallics (1993), 12(2), 580-2, database is CAplus.

Homocoupling reactions of amino- and diaminoalkylchlorosilanes with Li metal proceed readily in THF at room temperature to form the corresponding sym. diamino- and tetraaminoalkyldisilanes, resp., in high yields, which are transformed into chloroalkyldisilanes by the action of acyl chloride or dry HCl and into ethoxyalkyldisilanes by ethanolysis under mild conditions. The following are the compounds prepared in this study: XR¹R²SiSiR¹R²X where R¹ = R² = Me, X = Et₂N and Cl; R¹ = R² = iso-Pr, X = Et₂N and Cl; R¹ = Me,R² = n-hexyl, X = Et₂N, Cl and EtO, and X₂MeSiSiMeX₂ where X = Et₂N and EtO.

Organometallics 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 C38H74Cl2N2O4, Product Details of C7H16Cl2Si.

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

Sato, Masakazu published the artcileSynthesis and evaluation of novel thiazolidine derivatives as thromboxane A₂ receptor antagonists, Related Products of chlorides-buliding-blocks, the publication is Chemical & Pharmaceutical Bulletin (1994), 42(3), 521-9, database is CAplus and MEDLINE.

3-Benzoyl or 3-phenylsulfonyl-2-substituted thiazolidine derivatives were prepared, and evaluated for their thromboxane A₂ (TXA₂) receptor-antagonizing effect on (15S)-15-hydroxy-11α,9α-(epoxymethano)prostathiazolidine derivative, 3-benzoyl-2-(4-hydroxy-3-methoxyphenyl)thiazolidine, showed mild TXA₂ receptor antagonist activity. Modification of the compound led to 2-chloro-4-[3-(4-chlorophenylsulfonyl)thiazolidin-2-ylmethyl]phenoxyacetates I (X = H, Cl; R² = H, OMe, halo; n = 0-2), one of which showed TXA₂ receptor antagonist activity.

Chemical & Pharmaceutical Bulletin 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, Related Products of chlorides-buliding-blocks.

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