Month: October 2022

Verma, Astha; Grams, R. Justin; Rastatter, Brett P.; Santos, Webster L. published the artcile< Semireduction of alkynoic acids via a transition metal-free α borylation-protodeborylation sequence>, Recommanded Product: 3-(4-Chlorophenyl)propiolic acid, the main research area is acrylic acid preparation; alkynoic acid semiredn diastereoselective.

A method for the semi-reduction of alkynoic acids through an α-borylation and subsequent protodeborylation mechanism was developed. The transition metal-free protocol is achieved through the activation of bis(pinacolato)diboron by an in-situ generated carboxylate moiety yielding aryl acrylic acids. Our studies demonstrate an unprecedented dual role for the carboxylate anion that involves the activation of the diboron reagent and a directing effect in the α-borylation.

Tetrahedron published new progress about Alkynes Role: RCT (Reactant), RACT (Reactant or Reagent). 3240-10-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H5ClO2, Recommanded Product: 3-(4-Chlorophenyl)propiolic acid.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Capkova, Katerina; Yoneda, Yoshiyuki; Dickerson, Tobin J.; Janda, Kim D. published the artcile< Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors>, Formula: C8H7ClO2, the main research area is chlorocinnamic acid hydroxamate preparation BoNT A protease inhibitor activity; hydroxamate chlorocinnamic acid preparation structure activity relationship.

Botulinum neurotoxins are the most toxic proteins currently known. Based on a recently identified potent lead structure, 2,4-dichlorocinnamic acid hydroxamate, herein we report on the structure-activity relationship of a series of hydroxamate botulinum neurotoxin A (BoNT/A) protease inhibitors. Among them, 2-bromo-4-chlorocinnamic acid hydroxamate, e.g., I, 2-methyl-4-chlorocinnamic acid hydroxamate, and 2-trifluoromethyl-4-chlorocinnamic acid hydroxamate displayed comparable inhibitory activity to that of the lead structure.

Bioorganic & Medicinal Chemistry Letters published new progress about Biological warfare agents. 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Formula: C8H7ClO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Afanasyev, Oleg I.; Kliuev, Fedor S.; Tsygankov, Alexey A.; Nelyubina, Yulia V.; Gutsul, Evgenii; Novikov, Valentin V.; Chusov, Denis published the artcile< Fluoride Additive as a Simple Tool to Qualitatively Improve Performance of Nickel-Catalyzed Asymmetric Michael Addition of Malonates to Nitroolefins>, COA of Formula: C8H6ClNO2, the main research area is nitroalkene dialkyl malonate nickel catalyst enantioselective Michael addition; dialkylnitroethylmalonate preparation.

Described that simple in-situ addition of the fluoride source to the asym. organometallic catalyst was improved not only activity but also enantioselectivity. Bromide-nickel diimine complexes were found to catalyze asym. Michael addition in low yields and ee, but activation with fluoride leads to a significant improvement in catalyst performance. The developed approach were applied to prepare several enantioenriched GABA analogs.

Journal of Organic Chemistry published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 5153-70-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClNO2, COA of Formula: C8H6ClNO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tang, Yan-Ling; Zheng, Xi; Qi, Yan; Pu, Xiao-Jia; Liu, Bei; Zhang, Xia; Li, Xiao-Si; Xiao, Wei-Lie; Wan, Chun-Ping; Mao, Ze-Wei published the artcile< Synthesis and anti-inflammatory evaluation of new chalcone derivatives bearing bispiperazine linker as IL-1β inhibitors>, Application In Synthesis of 17082-09-6, the main research area is bispiperazinochalcone preparation antitumor antiinflammatory activity interleukin inhibitor; Anti-inflammatory activity; Chalcone derivatives; Cytotoxicity; IL-1β inhibitors.

In this work, a series of novel chalcone derivatives I (n = 1,2; R = H, 3-chloropropanoyl, (3,5-dichlorophenyl)carbonyl, (4-nitrophenyl)methyl, etc.) bearing bispiperazine linker have been synthesized and in vitro anti-inflammatory, cytotoxic activity and anti-inflammatory mechanism have been screened. The results indicated that most bispiperazinochalcone derivatives I displayed good inhibition of NO (IC50 < 20μM) and low cytotoxicity (CC50 > 40μM), and selectively inhibited the production of IL-1β via inhibiting NLRP3 inflammasome activation, as promising candidate compounds for the treatment of NLRP3 inflammasome-driven diseases.

Bioorganic Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 17082-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H7ClO, Application In Synthesis of 17082-09-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Xu, Jinhui; Cao, Jilei; Wu, Xiangyang; Wang, Han; Yang, Xiaona; Tang, Xinxin; Toh, Ren Wei; Zhou, Rong; Yeow, Edwin K. L.; Wu, Jie published the artcile< Unveiling Extreme Photoreduction Potentials of Donor-Acceptor Cyanoarenes to Access Aryl Radicals from Aryl Chlorides>, Application In Synthesis of 1435-43-4, the main research area is aryl chloride boronate light cyanoarene photoreductive borylation catalyst; arylboronate preparation; phosphine aryl chloride light cyanoarene phosphorylation catalyst; arylphosphonium salt preparation.

Since the seminal work of Zhang in 2016, donor-acceptor cyanoarene-based fluorophores, such as 1,2,3,5-tetrakis(carbazol-9-yl)-4,6-dicyanobenzene (4CzIPN), have been widely applied in photoredox catalysis and used as excellent metal-free alternatives to noble metal Ir- and Ru-based photocatalysts. However, all the reported photoredox reactions involving this chromophore family are based on harnessing the energy from a single visible light photon, with a limited range of redox potentials from -1.92 to +1.79 V vs SCE. Here, we document the unprecedented discovery that this family of fluorophores can undergo consecutive photoinduced electron transfer (ConPET) to achieve very high reduction potentials. One of the newly synthesized catalysts, 2,4,5-tri(9H-carbazol-9-yl)-6-(ethyl(phenyl)amino)isophthalonitrile (3CzEPAIPN), possesses a long-lived (12.95 ns) excited radical anion form, 3CzEPAIPN•-*, which can be used to activate reductively recalcitrant aryl chlorides (Ered ≈ -1.9 to -2.9 V vs SCE) under mild conditions. The resultant aryl radicals can be engaged in synthetically valuable aromatic C-B, C-P, and C-C bond formation to furnish arylboronates, arylphosphonium salts, arylphosphonates, and spirocyclic cyclohexadienes.

Journal of the American Chemical Society published new progress about Aromatic nitriles Role: CAT (Catalyst Use), SPN (Synthetic Preparation), USES (Uses), PREP (Preparation). 1435-43-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H3ClF2, Application In Synthesis of 1435-43-4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ofengeim, Dimitry; Shi, Peng; Miao, Benchun; Fan, Jing; Xia, Xiaofeng; Fan, Yubo; Lipinski, Marta M.; Hashimoto, Tadafumi; Polydoro, Manuela; Yuan, Junying; Wong, Stephen T. C.; Degterev, Alexei published the artcile< Identification of Small Molecule Inhibitors of Neurite Loss Induced by Aβ peptide using High Content Screening>, Computed Properties of 6055-19-2, the main research area is non steroidal antiinflammatory drug amyloid beta neurite Alzheimers disease.

Multiple lines of evidence indicate a strong relationship between Aβ peptide-induced neurite degeneration and the progressive loss of cognitive functions in Alzheimer disease (AD) patients and in AD animal models. This prompted us to develop a high content screening assay (HCS) and Neurite Image Quantitator (NeuriteIQ) software to quantify the loss of neuronal projections induced by Aβ peptide neurons and enable us to identify new classes of neurite-protective small mols., which may represent new leads for AD drug discovery. We identified thirty-six inhibitors of Aβ-induced neurite loss in the 1,040-compound National Institute of Neurol. Disorders and Stroke (NINDS) custom collection of known bioactives and FDA approved drugs. Activity clustering showed that non-steroidal anti-inflammatory drugs (NSAIDs) were significantly enriched among the hits. Notably, NSAIDs have previously attracted significant attention as potential drugs for AD; however their mechanism of action remains controversial. Our data revealed that cyclooxygenase-2 (COX-2) expression was increased following Aβ treatment. Furthermore, multiple distinct classes of COX inhibitors efficiently blocked neurite loss in primary neurons, suggesting that increased COX activity contributes to Aβ peptide-induced neurite loss. Finally, we discovered that the detrimental effect of COX activity on neurite integrity may be mediated through the inhibition of peroxisome proliferator-activated receptor γ (PPARγ) activity. Overall, our work establishes the feasibility of identifying small mol. inhibitors of Aβ-induced neurite loss using the NeuriteIQ pipeline and provides novel insights into the mechanisms of neuroprotection by NSAIDs.

Journal of Biological Chemistry published new progress about Alzheimer disease. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Computed Properties of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Rivkin, Alexey; Ahearn, Sean P.; Chichetti, Stephanie M.; Hamblett, Christopher L.; Garcia, Yudith; Martinez, Michelle; Hubbs, Jed L.; Reutershan, Michael H.; Daniels, Matthew H.; Siliphaivanh, Phieng; Otte, Karin M.; Li, Chaomin; Rosenau, Andrew; Surdi, Laura M.; Jung, Joon; Hughes, Bethany L.; Crispino, Jamie L.; Nikov, George N.; Middleton, Richard E.; Moxham, Christopher M.; Szewczak, Alexander A.; Shah, Sanjiv; Moy, Lily Y.; Kenific, Candia M.; Tanga, Flobert; Cruz, Jonathan C.; Andrade, Paula; Angagaw, Minilik H.; Shomer, Nirah H.; Miller, Thomas; Munoz, Benito; Shearman, Mark S. published the artcile< Purine derivatives as potent γ-secretase modulators>, COA of Formula: C6H4Cl2N4, the main research area is purine derivative preparation gamma secretase Alzheimer’s amyloid structure.

The development of a novel series of purines as γ-secretase modulators for potential use in the treatment of Alzheimer’s disease is disclosed herein. Optimization of a previously disclosed pyrimidine series afforded a series of potent purine-based γ-secretase modulators with 300- to 2000-fold in vitro selectivity over inhibition of Notch cleavage and that selectively reduces Αβ42 in an APP-YAC transgenic mouse model.

Bioorganic & Medicinal Chemistry Letters published new progress about Alzheimer disease. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, COA of Formula: C6H4Cl2N4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Pointon, Joanna C.; Eagle, Gina; Bailey, James; Evans, Paul; Allsup, David; Greenman, John published the artcile< Thalidomide enhances cyclophosphamide and dexamethasone-mediated cytotoxicity towards cultured chronic lymphocytic leukaemia cells>, Quality Control of 6055-19-2, the main research area is cytotoxic thalidomide cyclophosphamide monohydrate dexamethasone chronic lymphocytic leukemia.

Numerous chemotherapeutic regimens exist for the treatment of symptomatic or progressive chronic lymphocytic leukemia (CLL). However, once the disease becomes refractory to nucleoside-based therapy the prognosis is poor. In this study we investigated the cytotoxicity of thalidomide in combination with dexamethasone, fludarabine and cyclophosphamide. Cells from a cohort of 25 CLL patients were incubated for 72 h with each of these three agents, at 3 concentrations, both with and without thalidomide. Cell viability was assessed using the Annexin V:FITC assay. Fludarabine was highly toxic to the cells, producing very high levels of cell death; however, thalidomide did not increase this effect. Cyclophosphamide combined with thalidomide showed a small, non-significant improvement in toxicity compared with monotherapy. Median cell death for 5 μM dexamethasone monotherapy and for combination with thalidomide was 15% [interquartile range (IQR) 0-38%] and 17% (IQR 0-54%), resp. (Wilcoxon Signed Rank anal., p = 0.034). Cell death for 10 μM dexamethasone monotherapy was 15% (IQR 0-45%) and 16% (IQR 0-62%) in combination with thalidomide (Wilcoxon Signed Rank anal., p = 0.035). At the highest doses tested 11 of 25 cases displayed an enhancement of cyclophosphamide-mediated cytotoxicity, and 14 of 25 cases showed enhanced dexamethasone-mediated cytotoxicity in the presence of thalidomide. Some CLL cells in which dexamethasone-mediated killing was enhanced were derived from patients with poor prognostic markers, including p53 mutations and unmutated IgVH genes. In summary, thalidomide enhances cyclophosphamide- and dexamethasone-mediated cytotoxicity of CLL cells in vitro in a proportion of cases.

Oncology Reports published new progress about CD19 antigens Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Quality Control of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Shand, F. L.; Howard, J. G. published the artcile< Induction in vitro of reversible immunosuppression and inhibition of B cell receptor regeneration by defined metabolites of cyclophosphamide>, Reference of 6055-19-2, the main research area is lymphocyte Ig cyclophosphamide metabolite immunosuppression; receptor lymphocyte cyclophosphamide metabolite immunosuppression.

A number of defined metabolites and derivatives of cyclophosphamide (I) [50-18-0] were compared with the parent compound for their capacity to induce suppression of humoral antibody responses in vivo and in vitro and to inhibit the regeneration of surface Ig (sIg) receptors on B cells subsequent to capping with anti-Ig serum. Both functions were inhibited by exposing spleen cells in vitro to the most active compounds (4-hydroperoxycyclophosphamide [39800-16-3] and phosphoramide mustard [10159-53-2]) in concentrations of ≤10 μg/mL. Although these inhibitory activities were restricted to those mols. with demonstrable alkylating activity, they are nevertheless reversible and not dependent on events leading to cell death. Inhibition with microsomally activated I in vitro rendered splenic B cells hypersusceptible to tolerance induction by levan, although in the absence of this antigen they recovered full responsiveness to it within 7-10 days. Since lethally irradiated mice repopulated with adult bone marrow cells do not regenerate normal responsiveness to polysaccharide antigens in <50-100 days, the rapid recovery by I-treated spleen cells probably involves reversal of suppression in B cells and not renewal from stem cells. The previous proposal that impairment of B cell receptor regeneration by I is causally related to its capacity to promote B cell tolerance induction by thymus-independent antigens is supported. European Journal of Immunology published new progress about Antibodies and Immunoglobulins Role: BIOL (Biological Study). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Reference of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Mohr, Lisa-Marie; Bauer, Andreas; Jandl, Christian; Bach, Thorsten published the artcile< Visible light-mediated intermolecular [2 + 2] photocycloaddition of 1-aryl-2-nitroethenes and olefins>, Synthetic Route of 5153-70-8, the main research area is aryl cyclobutane preparation intermol photocycloaddition arylnitroethene olefin.

Despite the importance of cyclobutanes there are not many direct [2 + 2] photocycloaddition reactions which can be performed with visible light in the absence of a catalyst. A notable exception is the reaction of 1-aryl-2-nitroethenes and olefins which can be performed at a wavelength of λ = 419 nm or λ = 424 nm in CH2Cl2 as the solvent. In the present study, a total of 15 1-aryl-2-nitroethenes were found to undergo a [2 + 2] photocycloaddition with 2,3-dimethyl-2-butene (28-86% yield) and a set of 12 olefins was studied in their photocycloaddition to 1-phenyl-2-nitroethene (37-88% yield). All mechanistic results are in agreement with a triplet reaction pathway and with the intermediacy of a 1,4-diradical.

Organic & Biomolecular Chemistry published new progress about [2+2] Photocycloaddition reaction. 5153-70-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClNO2, Synthetic Route of 5153-70-8.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics