Month: January 2023

Glibenclamide alters serotonin and dopamine levels in the rat striatum and hippocampus, reducing cognitive impairment was written by Zubov, Alexander S.;Ivleva, Irina S.;Pestereva, Nina S.;Tiutiunnik, Tatiana V.;Traktirov, Dmitrtii S.;Karpenko, Marina N.. And the article was included in Psychopharmacology (Heidelberg, Germany) in 2022.SDS of cas: 10238-21-8 This article mentions the following:

Glibenclamide (GD) is a widely used medical drug; therefore, identifying the mechanisms underlying its pleiotropic effects in the central nervous system is urgent. Objectives: The aim of this work was to determine the ability of GD to modulate serotonin (5-hydroxytryptamine, 5-HT) and dopamine (DA) transmission and to assess the dose-dependent effect of GD on cognitive function in rats during natural ageing. In Experiment 1, rats received 10, 25, or 50 μg/kg GD i.p. for 10 days. In Experiment 2, rats received 50 μg/kg GD i.p. for 30 days. Spatial and working memory was assessed in the MWM and Y-maze tests, resp. In both experiments, the levels of DA and 5-HT, their metabolites, and turnover rate were analyzed by HPLC-ED in the rat hippocampus and striatum. Changes in DA and 5-HT levels occurred only with a dose of 50 μg/kg GD. Therefore, in the second experiment, we administered a dose of 50 μg/kg GD. At this dose, GD prevented the development of impairments in spatial and working memory. The hippocampal concentrations of DA and DOPAC decreased, and the striatal concentrations of DA, DOPAC, 5-HT, and 5-HIAA increased. Conclusion: One of the possible mechanisms of the precognitive effect of GD is its ability to modulate monoamine transmission. Thus, in translating our results to humans, GD can be recommended as a prophylactic agent for natural ageing to reduce the risk of developing cognitive impairments. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8SDS of cas: 10238-21-8).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.SDS of cas: 10238-21-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Therapeutic potential of tranilast for the treatment of chronic graft-versus-host disease in mice was written by Mukai, Shin;Ogawa, Yoko;Saya, Hideyuki;Kawakami, Yutaka;Tsubota, Kazuo. And the article was included in PLoS One in 2018.Related Products of 53902-12-8 This article mentions the following:

Chronic graft-vs.-host disease (cGVHD) is a marked complication of hematopoietic stem cell transplantation, and multiple organs can be affected by cGVHD-induced inflammation and fibrosis. In clin. settings, immunosuppressive agents have been the last resort to treat cGVHD. However, it has been only partially effective for cGVHD. Hence, efficacious treatment of cGVHD is eagerly awaited. Our previous work suggested that oxidative stress was elevated in cGVHD-disordered lacrimal glands and that epithelial-to-mesenchymal transition (EMT) was implicated in fibrosis caused by ocular cGVHD. In addition, our recent article demonstrated that thioredoxin interaction protein (TXNIP) and transcription factor nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) were associated with the development of cGVHD. After our search for effective drugs, we chose tranilast to combat systemic cGVHD. Tranilast is known to (1) act as an inhibitor of the inflammatory mols. TXNIP and NF-κB and (2) exert anti-fibrotic, anti-EMT and anti-oxidative effects. To investigate the effectiveness of tranilast for cGVHD, we used an MHC-compatible, multiple minor histocompatibility antigen-mismatched murine model of cGVHD. Tranilast or a solvent-vehicle were orally given to the allogeneic bone marrow transplantation (allo-BMT) recipients from the day before allo-BMT (Day-1) to Day 27 after allo-BMT. Their cGVHD-vulnerable organs were collected Day 28 after allo-BMT and analyzed by using various methods such as histol., immunohistochem. and immunoblotting. As indicated by our results, tranilast alleviated cGVHD-elicited inflammation and fibrosis by suppressing the expression and/or activation of TXNIP and NF-κB and preventing EMT. Taken together, although this strategy may not be a complete cure for cGVHD, tranilast could be a promising medication to ameliorate cGVHD-triggered disabling symptoms. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Related Products of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Related Products of 53902-12-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

The study on loss in strength of fabrics oxygen bleached with PB/TAED was written by Wan, Yingying. And the article was included in Ranliao Yu Ranse in 2012.Name: N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) This article mentions the following:

The powder detergent containing PB/TAED activated oxygen bleaching system was employed to wash the cotton fabrics which dyed by four kinds of reactive dyes. The fabric tensile strength, K/S and color deviation of the fabrics before and after washing were determined in the conditions of different dyes, detergents and temperature by orthogonal test. The study results provided reference basis for better fabric care. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Name: N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide)).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Name: N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide)

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Cannabidiol Increases Proliferation, Migration, Tubulogenesis, and Integrity of Human Brain Endothelial Cells through TRPV2 Activation was written by Luo, Huilong;Rossi, Elisa;Saubamea, Bruno;Chasseigneaux, Stephanie;Cochois, Veronique;Choublier, Nina;Smirnova, Maria;Glacial, Fabienne;Perriere, Nicolas;Bourdoulous, Sandrine;Smadja, David M.;Menet, Marie-Claude;Couraud, Pierre-Olivier;Cisternino, Salvatore;Decleves, Xavier. And the article was included in Molecular Pharmaceutics in 2019.Name: 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid This article mentions the following:

The effect of cannabidiol (CBD), a high-affinity agonist of the transient receptor potential vanilloid-2 (TRPV2) channel, has been poorly investigated in human brain microvessel endothelial cells (BMEC) forming the blood-brain barrier (BBB). TRPV2 expression and its role on Ca²⁺ cellular dynamics, trans-endothelial elec. resistance (TEER), cell viability and growth, migration, and tubulogenesis were evaluated in human primary cultures of BMEC (hPBMEC) or in the human cerebral microvessel endothelial hCMEC/D3 cell line. Abundant TRPV2 expression was measured in hCMEC/D3 and hPBMEC by qRT-PCR, Western blotting, nontargeted proteomics, and cellular immunofluorescence studies. Intracellular Ca²⁺ levels were increased by heat and CBD and blocked by the nonspecific TRP antagonist ruthenium red (RR) and the selective TRPV2 inhibitor tranilast (TNL) or by silencing cells with TRPV2 siRNA. CBD dose-dependently induced the hCMEC/D3 cell number (EC₅₀ 0.3 ± 0.1 μM), and this effect was fully abolished by TNL or TRPV2 siRNA. A wound healing assay showed that CBD induced cell migration, which was also inhibited by TNL or TRPV2 siRNA. Tubulogenesis of hCMEC/D3 cells in 3D matrigel cultures was significantly increased by 41 and 73% after a 7 or 24 h CBD treatment, resp., and abolished by TNL. CBD also increased the TEER of hPBMEC monolayers cultured in transwell, and this was blocked by TNL. Our results show that CBD, at extracellular concentrations close to those observed in plasma of patients treated by CBD, induces proliferation, migration, tubulogenesis, and TEER increase in human brain endothelial cells, suggesting CBD might be a potent target for modulating the human BBB. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Name: 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Name: 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Regio- and stereoselective synthesis of γ-alkylidenebutenolides by cyclization of dilithiated 1,3-dicarbonyl compounds with N,N’-dimethoxy-N,N’-dimethylethanediamide was written by Langer, Peter;Stoll, Martin. And the article was included in Angewandte Chemie, International Edition in 1999.SDS of cas: 106675-70-1 This article mentions the following:

In most cases the title reactions gave (E)-alkylidenebutenolides [I; R¹ = H, Me; R² = H, Me, Et; R³ = OEt, OCMe₃, Me, NEt₂, Ph; R²R³ = CH₂CH₂O, (CH₂)₄, CH₂CHMeO, etc.]. In two cases the Z isomers predominated. In the experiment, the researchers used many compounds, for example, N1,N2-Dimethoxy-N1,N2-dimethyloxalamide (cas: 106675-70-1SDS of cas: 106675-70-1).

N1,N2-Dimethoxy-N1,N2-dimethyloxalamide (cas: 106675-70-1) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.SDS of cas: 106675-70-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Tranilast inhibits the expression of genes related to epithelial-mesenchymal transition and angiogenesis in neurofibromin-deficient cells was written by Harigai, Ritsuko;Sakai, Shigeki;Nobusue, Hiroyuki;Hirose, Chikako;Sampetrean, Oltea;Minami, Noriaki;Hata, Yukie;Kasama, Takashi;Hirose, Takanori;Takenouchi, Toshiki;Kosaki, Kenjiro;Kishi, Kazuo;Saya, Hideyuki;Arima, Yoshimi. And the article was included in Scientific Reports in 2018.Formula: C18H17NO5 This article mentions the following:

Neurofibromatosis type 1 (NF1) is caused by germline mutations in the NF1 gene and is characterized by cafe au lait spots and benign tumors known as neurofibromas. NF1 encodes the tumor suppressor protein neurofibromin, which neg. regulates the small GTPase Ras, with the constitutive activation of Ras signalling resulting from NF1 mutations being thought to underlie neurofibroma development. We previously showed that knockdown of neurofibromin triggers epithelial-mesenchymal transition (EMT) signalling and that such signalling is activated in NF1-associated neurofibromas. With the use of a cell-based drug screening assay, we have now identified the antiallergy drug tranilast (N-(3,4-dimethoxycinnamoyl) anthranilic acid) as an inhibitor of EMT and found that it attenuated the expression of mesenchymal markers and angiogenesis-related genes in NF1-mutated sNF96.2 cells and in neurofibroma cells from NF1 patients. Tranilast also suppressed the proliferation of neurofibromin-deficient cells in vitro more effectively than it did that of intact cells. In addition, tranilast inhibited sNF96.2 cell migration and proliferation in vivo. Knockdown of type III collagen (COL3A1) also suppressed the proliferation of neurofibroma cells, whereas expression of COL3A1 and SOX2 was increased in tranilast-resistant cells, suggesting that COL3A1 and the transcription factor SOX2 might contribute to the development of tranilast resistance. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Formula: C18H17NO5).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Formula: C18H17NO5

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Investigational drugs for hyperuricemia, an update on recent developments was written by Pascart, Tristan;Richette, Pascal. And the article was included in Expert Opinion on Investigational Drugs in 2018.HPLC of Formula: 53902-12-8 This article mentions the following:

The significant proportion of gout patients not reaching serum urate levels below 6.0 mg/dL and the debated pathogenicity of hyperuricemia (HU) itself motivate investigators to develop new drugs to decrease uricemia. This review discusses the drugs considered to be in active development from pre-clin. to phase III studies. This review covers 11 drugs in development, including a xanthine oxidase inhibitor (topiroxostat), uricosurics (verinurad, arhalofenate, UR-1102, tranilast), dual inhibitors (RLBN1001, KUX-1151), a uricase (pergsiticase), an inhibitor of hypoxanthine production (ulodesine), and drugs with yet-to-explain mechanisms of action (levotofisopam, tuna extracts). Drugs well advanced in their development – particularly arhalofenate, verinurad and topiroxostat – open the prospect of patient-comorbidity-tailored HU management. Development of novel therapies provides new insight into our understanding of gout and HU, particularly potential pathogenicity. Apart from potency to decrease serum urate levels and good tolerance profiles, novel therapies will need to focus on administration modalities facilitating treatment adherence. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8HPLC of Formula: 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.HPLC of Formula: 53902-12-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Anti-aging effects of chlorpropamide depend on mitochondrial complex-II and the production of mitochondrial reactive oxygen species was written by Mao, Zhifan;Liu, Wenwen;Huang, Yunyuan;Sun, Tianyue;Bao, Keting;Feng, Jiali;Moskalev, Alexey;Hu, Zelan;Li, Jian. And the article was included in Acta Pharmaceutica Sinica B in 2022.Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide This article mentions the following:

Sulfonylureas are widely used oral anti-diabetic drugs. However, its long-term usage effects on patients lifespan remain controversial, with no reports of influence on animal longevity. Hence, the anti-aging effects of chlorpropamide along with glimepiride, glibenclamide, and tolbutamide were studied with special emphasis on the interaction of chlorpropamide with mitochondrial ATP-sensitive K+ (mitoK-ATP) channels and mitochondrial complex II. Chlorpropamide delayed aging in Caenorhabditis elegans, human lung fibroblast MRC-5 cells and reduced doxorubicin-induced senescence in both MRC-5 cells and mice. In addition, the mitochondrial membrane potential and ATP levels were significantly increased in chlorpropamide-treated worms, which is consistent with the function of its reported targets, mitoK-ATP channels. Increased levels of mitochondrial reactive oxygen species (mtROS) were observed in chlorpropamide-treated worms. Moreover, the lifespan extension by chlorpropamide required complex II and increased mtROS levels, indicating that chlorpropamide acts on complex II directly or indirectly via mitoK-ATP to increase the production of mtROS as a pro-longevity signal. This study provides mechanistic insight into the anti-aging effects of sulfonylureas in C. elegans. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Name: 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Catalyst-free oxidative N-N coupling for the synthesis of 1,2,3-triazole compounds with tBuONO was written by Cai, Yue-Ming;Zhang, Xin;An, Cui;Yang, Ye-Fei;Liu, Wei;Gao, Wen-Xia;Huang, Xiao-Bo;Zhou, Yun-Bing;Liu, Miao-Chang;Wu, Hua-Yue. And the article was included in Organic Chemistry Frontiers in 2019.SDS of cas: 119023-25-5 This article mentions the following:

A catalyst-free method was developed to synthesize 1,2,3-benzotriazinones I [R = H, 6-Cl, 6-Br, etc.] and 1,2,3-benzothiadiazoles II [R¹ = H, 6-Cl, 6-Br, etc.] from 2-amino-benzamides and 2-amino thiols. Of particular note was that the one-step synthesis route to access [1,2,3]triazolo[1,5-a]pyridines III [R² = H, Ph, 4-ClC₆H₄; R³ = H, 7-Me, 7-Br] from pyridin-2-ylmethanamine was reported for the first time. This approach featured no use of catalyst, extremely mild conditions and excellent efficiency. In the experiment, the researchers used many compounds, for example, 2-Amino-4-fluorobenzamide (cas: 119023-25-5SDS of cas: 119023-25-5).

2-Amino-4-fluorobenzamide (cas: 119023-25-5) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.SDS of cas: 119023-25-5

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

A Catalytic Route to Pyrrole Derivatives via Copper-catalyzed Multicomponent Reaction was written by Samzadeh-Kermani, Alireza;Ghasemi, Samira. And the article was included in Journal of Heterocyclic Chemistry in 2019.Computed Properties of C13H24N2O This article mentions the following:

In the presence of CuI, Bu₄P⁺·AcO^–, and DBU in MeCN, terminal alkynes R¹CCH (R¹ = Ph, 3-MeC₆H₄, 3-MeOC₆H₄, 2-furyl, 2-thienyl, Bu, PhCH₂CH₂, Me₃Si), carbodiimides R²N:C:NR³ (R² = R³ = cyclohexyl, i-Pr, Ph; R² = Ph, 4-MeC₆H₄, 4-ClC₆H₄, R³ = cyclohexyl; R² = Ph, R³ = Bu), and malononitrile underwent regioselective three-component coupling and cyclization reactions to yield (alkylidene)iminopyrrolinecarbonitriles I (R¹ = Ph, 3-MeC₆H₄, 3-MeOC₆H₄, 2-furyl, 2-thienyl, Bu, PhCH₂CH₂, Me₃Si; R² = R³ = cyclohexyl, i-Pr, Ph; R² = Ph, 4-MeC₆H₄, 4-ClC₆H₄, R³ = cyclohexyl; R² = Ph, R³ = Bu). In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Computed Properties of C13H24N2O).

1,3-Dicyclohexylurea (cas: 2387-23-7) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Computed Properties of C13H24N2O

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics