Day: October 19, 2021

Category: isothiazole. In 2020 EUR J MED CHEM published article about VON-WILLEBRAND-FACTOR; PLATELET ACTIVATION; PREVENTS THROMBOSIS; LACTIC-ACIDOSIS; METFORMIN; RISK; ADHESION; PRODRUG in [Xin, Guang; Ming, Yue; Wei, Zeliang; Li, Shiyi; Zhang, Xiaoyu; Yu, Kui; Li, Youping; Xing, Zhihua; He, Yarong; Chen, Zhen; Niu, Hai; Huang, Wen] Sichuan Univ, West China Hosp, West China Sch Med, Lab Ethnopharmacol, Chengdu, Peoples R China; [Ji, Chengjie] Hosp Univ Elect Sci & Technol China, Sichuan Prov Peoples Hosp, Clin Lab, Chengdu, Sichuan, Peoples R China; [Morris-Natschke, Susan L.; Lee, Kuo-Hsiung] Univ N Carolina, Nat Prod Res Labs, UNC Eshelman Sch Pharm, Chapel Hill, NC 27599 USA; [Zhang, Boli; Zhang, Junhua] Tianjin Univ Tradit Chinese Med, Tianjin, Peoples R China; [Yang, Xijing] Sichuan Univ, West China Hosp, Anim Expt Ctr, West China Sch Med, Chengdu, Sichuan, Peoples R China; [Niu, Hai] Sichuan Univ, Coll Math, Chengdu, Sichuan, Peoples R China in 2020, Cited 46. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0.

Platelet thrombosis is the main pathogeny resulting in the low curability of ischemic stroke, a leading cause of mortality and disability worldwide. Metformin, a biguanide derivative that is the first-line oral medicine for type 2 diabetes, alleviates the severity of ischemic stroke in diabetic patients and suppresses platelet activation in experimental animal model. However, the clinical implementation of commercial biguanide analogs for stroke related to platelet thrombosis remains challenging due to its weak potency, poor pharmacokinetic characteristics and possible hypoglycemia. Here, twenty-three biguanide derivatives were designed and synthesized based on the principles of bioisosteres. These derivatives were evaluated for the activity of antiplatelet thrombosis in vivo. We found that N-tri-fluoromethanesulfonyl biguanide derivative, compound b10, uniquely prevented cerebral infarction as well as neuronal function injury, and significantly decrease the mortality rate of ischemic stroke in the middle cerebral artery occlusion mice without significant side effects. We verified that b10 directly inhibited platelets thrombus formation and decreased the compactness of stroke thrombi. Particularly, b10 exhibited good potency to inhibit human platelet activation including platelet aggregation, adhesion, pseudopodia formation, integrin GPIIb/IIIa activation, CD62P expression and clot retraction. Meanwhile, the pharmacokinetics assessment showed that b10 had satisfying pharmacological characteristics including a longer duration and a higher oral absorption ratio than its parent compound. In addition, b10 remarkably ameliorated not only stroke related to platelet thrombosis but also carotid artery thrombus formation. It is concluded that the novel potent antiplatelet thrombotic agent derived from biguanide is a promising candidate for stroke treatment. (C) 2020 Elsevier Masson SAS. All rights reserved.

Category: isothiazole. About Benzoic anhydride, If you have any questions, you can contact Xin, G; Ming, Y; Ji, CJ; Wei, ZL; Li, SY; Morris-Natschke, SL; Zhang, XY; Yu, K; Li, YP; Zhang, BL; Zhang, JH; Xing, ZH; He, YR; Chen, Z; Yang, XJ; Niu, H; Lee, KH; Huang, W or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

I found the field of Chemistry very interesting. Saw the article An Indirect Strategy for Trifluoromethylation via an Iridium Catalyst: Approach to Generate Isocoumarin Skeletons in Bioactive Molecules published in 2020. Recommanded Product: 3-Methylbenzoic acid, Reprint Addresses Zhang, JY (corresponding author), Soochow Univ, Coll Energy, Soochow Inst Energy & Mat Innovat, Suzhou 215006, Peoples R China.; Zhao, YS (corresponding author), Soochow Univ, Key Lab Organ Synth Jiangsu Prov, Coll Chem Chem Engn & Mat Sci, Suzhou 215123, Peoples R China.. The CAS is 99-04-7. Through research, I have a further understanding and discovery of 3-Methylbenzoic acid

3-Bromo-1,1,1-trifluoroacetone was first disclosed as an effective indirect trifluoromethylation reagent to construct the important 3-trifluoromethyl isocoumarin skeleton. The reaction proceeds through a ligand-promoted, iridium-catalyzed ortho-selective C-H alkylation of benzoic acid and an intermolecular cyclization reaction promoted by silver acetate. A wide range of 3-trifluoromethyl isocoumarins can be easily obtained in moderate to good yields. Importantly, the isocoumarin skeleton can be easily formed in bioactive compounds, highlighting the importance of this reaction.

Recommanded Product: 3-Methylbenzoic acid. About 3-Methylbenzoic acid, If you have any questions, you can contact Zhou, KH; Geng, JY; Wang, DJ; Zhang, JY; Zhao, YS or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Mohammadi-Khanaposhtani, M; Yahyavi, H; Barzegaric, E; Imanparast, S; Heravi, MM; Faramarzi, MA; Foroumadi, A; Adibi, H; Larijani, B; Mandavi, M in [Mohammadi-Khanaposhtani, Maryam] Babol Univ Med Sci, Cellular & Mol Biol Res Ctr, Hlth Res Inst, Babol, Iran; [Yahyavi, Hoda; Heravi, Majid M.] Alzahra Univ, Fac Chem & Phys, Dept Chem, Tehran, Iran; [Barzegaric, Ebrahim] Kermanshah Univ Med Sci, Med Biol Res Ctr, Kermanshah, Iran; [Imanparast, Somaye; Faramarzi, Mohammad Ali] Univ Tehran Med Sci, Dept Pharmaceut Biotechnol, Fac Pharm, Tehran, Iran; [Imanparast, Somaye; Faramarzi, Mohammad Ali] Univ Tehran Med Sci, Biotechnol Res Ctr, Tehran, Iran; [Foroumadi, Alireza] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran; [Foroumadi, Alireza] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran, Iran; [Adibi, Hossein; Larijani, Bagher; Mandavi, Mohammad] Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Clin Sci Inst, Tehran, Iran published New Biscoumarin Derivatives as Potent alpha-Glucosidase Inhibitors: Synthesis, Biological Evaluation, Kinetic Analysis, and Docking Study in 2020.0, Cited 26.0. HPLC of Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.

A new series of biscoumarin derivatives3a-nwere synthesized and evaluated for their alpha-glucosidase inhibitory activities. The reaction of the 4-aminocoumarin with benzaldehyde derivatives led to the formation of the title compounds in good yields. All the synthesized compounds showed potent alpha-glucosidase inhibitory activity with IC(50)ranging from 20.0 +/- 0.7 to180.1 +/- 0.8 mu M, in comparison with acarbose as the standard drug (IC50= 750.0 1.5 mu M). Among the synthesized compounds, 3,3′-(p-tolylmethylene)bis(4-amino-2H-chromen-2-one)3cwas found to be the most active compound with an IC(50)value of 20.0 +/- 0.7 mu M. Kinetic study exhibited that compound3cwas a competitive inhibitor against alpha-glucosidase (K-i= 22.4 mu M). In silico docking study for the most potent compound3cwas also performed.

HPLC of Formula: C9H10O3. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Mohammadi-Khanaposhtani, M; Yahyavi, H; Barzegaric, E; Imanparast, S; Heravi, MM; Faramarzi, MA; Foroumadi, A; Adibi, H; Larijani, B; Mandavi, M or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Safety of 2,5-Dimethoxybenzaldehyde. Authors Kumar, M; Joshi, G; Arora, S; Singh, T; Biswas, S; Sharma, N; Bhat, ZR; Tikoo, K; Singh, S; Kumar, R in MDPI published article about in [Kumar, Manvendra; Joshi, Gaurav; Arora, Sahil; Biswas, Sajal; Kumar, Raj] Cent Univ Punjab, Sch Hlth Sci, Dept Pharmaceut Sci & Nat Prod, Lab Drug Design & Synth, Bathinda 151401, Punjab, India; [Joshi, Gaurav] Graph Era Hill Univ, Sch Pharm, Dehra Dun 248171, Uttarakhand, India; [Singh, Tashvinder; Singh, Sandeep] Cent Univ Punjab, Dept Human Genet & Mol Med, Bathinda 151401, Punjab, India; [Sharma, Nisha; Bhat, Zahid Rafiq; Tikoo, Kulbhushan] Natl Inst Pharmaceut Educ & Res, Dept Pharmacol & Toxicol, Sas Nagar 160062, Punjab, India in 2021.0, Cited 33.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

A series of 30 non-covalent imidazo[1,2-a]quinoxaline-based inhibitors of epidermal growth factor receptor (EGFR) were designed and synthesized. EGFR inhibitory assessment (against wild type) data of compounds revealed 6b, 7h, 7j, 9a and 9c as potent EGFR(WT) inhibitors with IC50 values of 211.22, 222.21, 193.18, 223.32 and 221.53 nM, respectively, which were comparable to erlotinib (221.03 nM), a positive control. Furthermore, compounds exhibited excellent antiproliferative activity when tested against cancer cell lines harboring EGFR(WT); A549, a non-small cell lung cancer (NSCLC), HCT-116 (colon), MDA-MB-231 (breast) and gefitinib-resistant NSCLC cell line H1975 harboring EGFR(L858R/T790M). In particular, compound 6b demonstrated significant inhibitory potential against gefitinib-resistant H1975 cells (IC50 = 3.65 mu M) as compared to gefitinib (IC50 > 20 mu M). Moreover, molecular docking disclosed the binding mode of the 6b to the domain of EGFR (wild type and mutant type), indicating the basis of inhibition. Furthermore, its effects on redox modulation, mitochondrial membrane potential, cell cycle analysis and cell death mode in A549 lung cancer cells were also reported.

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Kumar, M; Joshi, G; Arora, S; Singh, T; Biswas, S; Sharma, N; Bhat, ZR; Tikoo, K; Singh, S; Kumar, R or concate me.. Safety of 2,5-Dimethoxybenzaldehyde

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

In 2019 ORG LETT published article about 1ST TOTAL-SYNTHESIS; STEREOSELECTIVE-SYNTHESIS; NEURITOGENIC ACTIVITY; GANGLIOSIDE; ACID; FACILE; CONSTITUENTS; DERIVATIVES; CRINOIDEA; GLYCAN in [Tanaka, Hide-Nori; Ishida, Hideharu; Ando, Hiromune] Gifu Univ, Ctr Highly Adv Integrat Nano & Life Sci G CHAIN, Gifu 5011193, Japan; [Goto, Kenta; Tamai, Hideki; Takeda, Yoh; Mizuno, Takashi; Imamura, Akihiro; Ishida, Hideharu; Kiso, Makoto] Gifu Univ, Fac Appl Biol Sci, Dept Appl Bioorgan Chem, Gifu 5011193, Japan; [Kiso, Makoto; Ando, Hiromune] Kyoto Univ, Inst Integrated Cell Mat Sci WPI iCeMS, Kyoto 6068501, Japan in 2019, Cited 52. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Recommanded Product: Benzoic anhydride

The first total synthesis of three echinodermatous sialyl inositol phosphosphingolipids, which exhibit unusual neuritogenic activity in the absence of nerve growth factor, are reported. Highlights of the syntheses include 9-O-methylation on sialic acid, inter-residual amide bond formation between sialic acid residues, and highly stereo- and regioselective sialylation of inositol. A key phosphodiester linkage between the mono-, di-, and trisialyl inositols and ceramide was formed at a late state employing the phosphoramidite method.

Recommanded Product: Benzoic anhydride. About Benzoic anhydride, If you have any questions, you can contact Goto, K; Tamai, H; Takeda, Y; Tanaka, HN; Mizuno, T; Imamura, A; Ishida, H; Kiso, M; Ando, H or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Computed Properties of C9H10O3. Recently I am researching about ONE-POT SYNTHESIS; SOLID-PHASE SYNTHESIS; 2-SUBSTITUTED BENZIMIDAZOLES; EFFICIENT METHOD; SOLVENT; WATER; BENZOXAZOLES; DERIVATIVES; ACID; 2-ARYLBENZIMIDAZOLES, Saw an article supported by the . Published in ORIENTAL SCIENTIFIC PUBL CO in BHOPAL ,Authors: Halder, S. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde

Various substituted benzimidazoles have been successfully synthesized in aqueous medium by developing VO(acac)(2)-Cu(OTf)(2) catalytic system. A green synthetic protocol has been created in presence of water and cetyltrimethyl ammonium bromide (CTAB) system in an organic solvent free condition. This chemoselective cyclocondensation cumoxidation process occurred in aqueous media. In this suitable method easily synthesized 2-Substituted benzimidazoles with good yields and no 1,2-disubstituted by-products were noticed. Excellent yields, environmentally benign and mild reaction condition, easy purification of the desired products are the main attractive features of this newly devised method. [GRAPHICS]

Computed Properties of C9H10O3. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Halder, S or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

I found the field of Chemistry very interesting. Saw the article Newly synthesized 3-(4-chloro-phenyl)-3-hydroxy-2,2-dimethyl-propionic acid methyl ester derivatives selectively inhibit the proliferation of colon cancer cells published in 2020. Formula: C8H10O2, Reprint Addresses El Rayes, SM (corresponding author), Suez Canal Univ, Fac Sci, Dept Chem, Ismailia, Egypt.. The CAS is 151-10-0. Through research, I have a further understanding and discovery of 1,3-Dimethoxybenzene

A series of 24 compounds were synthesized based on structure modification of the model methyl-3-(4-chlorophenyl)-3-hydroxy-2,2-dimethylpropanoate as potent HDACIs. Saponification and hydrazinolysis of the model ester afforded the corresponding acid and hydrazide, respectively. The model ester was transformed into the corresponding trichloroacetimidate or acetate by the reaction with trichloroacetonitrile and acetic anhydride, respectively. N-Alkyl-3-(4-chlorophenyl)-3-hydroxy-2,2-dimethylpropan-amides and methyl-2-[(3-(4-chlorophenyl)-3-hydroxy-2,2-dimethylpropanoyl)amino] alkanoates were obtained by the reaction of corresponding acid or hydrazide with amines and amino acid esters via DCC and azide coupling methods. Methyl-3-aryl-3-(4-chlorophenyl)-2,2-dimethylpropanoates were obtained in good yields and short reaction time from the corresponding trichloroacetimidate or acetate by the reaction with C-active nucleophiles in the presence of TMSOTf (0.1 eq.%) via C-C bond formation. The antiproliferative and apoptotic activity were further studied with molecular docking. The 48 post-treatments showed that out of 24 compounds, 12 compounds showed inhibitory actions on HCT-116 cells, we have calculated the inhibitory action (IC50) of these compounds on HCT-116 and we have found that the IC50 values were in between 0.12 mg mL(-1) to 0.81 mg mL(-1). The compounds (7a & 7g) showed highest inhibitory activity (0.12 mg mL(-1)), whereas compound 7d showed the lowest inhibitory activity (0.81 mg mL(-1)). We have also examined inhibitory action on normal and non-cancerous cells (HEK-293 cells) and confirmed that action of these compounds was specific to cancerous cells. The cancerous cells were also examined for nuclear disintegration through staining with DAPI, (4 ‘,6-diamidino-2-phenylindole) is a blue-fluorescent DNA stain, and we have found that there was loss of DAPI staining in the compound treated cancerous cells. The compounds were found to potentially act through the HSP90 and TRAP1 mediated signaling pathway. Compounds 7a and 7g showed the highest selectivity to TRAP1 which explained its superior activity.

Formula: C8H10O2. About 1,3-Dimethoxybenzene, If you have any questions, you can contact El Rayes, SM; Aboelmagd, A; Gomaa, MS; Fathalla, W; Ali, IAI; Pottoo, FH; Khan, FA or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article A one pot protocol to convert nitro-arenes into N-aryl amides WOS:000509900800050 published article about BETA-ENAMINO ESTERS; ENANTIOSELECTIVE REDUCTION; ASYMMETRIC HYDROSILYLATION; RATIONAL DESIGN; AMINES; PERSPECTIVE; DERIVATIVES; SELECTIVITY; AMIDATION; LIGANDS in [Massolo, Elisabetta; Pirola, Margherita; Puglisi, Alessandra; Rossi, Sergio; Benaglia, Maurizio] Univ Milan, Dipartimento Chim, Via Golgi 19, I-20133 Milan, Italy in 2020, Cited 42. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Quality Control of Benzoic anhydride

A two-step one pot, experimentally simple protocol, based on readily available and inexpensive reagents allowed the conversion of nitro-arenes directly to N-aryl amides. A metal-free reduction of the nitro group, mediated by trichlorosilane, followed by the addition of an anhydride afforded the corresponding N-aryl carboxyamide, that was isolated after a simple aqueous work up in good-excellent yields. When the methodology was applied to the reaction with gamma-butyrolactone, the desired N-aryl butanamide derivative was obtained, featuring a chlorine atom at the gamma-position, a functionalized handle that can be used for further synthetic manipulation of the reaction product. Such an intermediate has already been employed as a key advanced precursor of pharmaceutically active compounds.

Quality Control of Benzoic anhydride. About Benzoic anhydride, If you have any questions, you can contact Massolo, E; Pirola, M; Puglisi, A; Rossi, S; Benaglia, M or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Synthesis and evaluation of the HIF-1 alpha inhibitory activities of novel ursolic acid tetrazole derivatives WOS:000466365200002 published article about BIOLOGICAL EVALUATION; STRUCTURAL-CHARACTERIZATION; TARGETED THERAPY; ANTICANCER; DESIGN in [Zhang, Lin-Hao; Zhang, Zhi-Hong; Li, Ming-Yue; Jin, Xue-Jun; Piao, Hu-Ri] Yanbian Univ, Key Lab Nat Resources Changbai Mt & Funct Mol, Minist Educ, Coll Pharm, Yanji 133002, Peoples R China; [Wei, Zhi-Yu] Dalian Univ, Coll Med, Dalian 116622, Liaoning, Peoples R China in 2019, Cited 37. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Recommanded Product: 93-97-0

The hypoxia-inducible factor-la (HIF-1 alpha) pathway has been implicated in tumor angiogenesis, growth, and metastasis. Therefore, the inhibition of this pathway is an important therapeutic target for the treatment of various types of cancers. Here, we designed and synthesized 31 ursolic acid (UA) derivatives containing a tetrazole moiety and evaluated them for their potential anti-tumor activities as HIF-la transcriptional inhibitors. Of these, compound 14d (IC50 0.8 +/- 0.2 mu M) displayed the most potent activity and compounds 14a (IC50 4.7 +/- 0.2 mu M) exhibited the most promising biological profile. Analysis of the structure-activity relationships of these compounds with HIF-1 alpha suggested that the presence of a tetrazole group located at C-28 of the UA derivatives was critical for their inhibitory activities.

Recommanded Product: 93-97-0. About Benzoic anhydride, If you have any questions, you can contact Zhang, LH; Zhang, ZH; Li, MY; Wei, ZY; Jin, XJ; Piao, HR or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Application In Synthesis of 3-Methylbenzoic acid. I found the field of Chemistry very interesting. Saw the article Iridium-Catalyzed Regioselective Synthesis of Trifluoromethylated Isocoumarins through Annulation of Benzoic Acids with Trifluoromethylated Alkynes published in 2019.0, Reprint Addresses Zhou, YR (corresponding author), Jiangxi Normal Univ, Coll Chem & Chem Engn, Key Lab Fuct Small Organ Mol, Minist Educ, 99 Ziyang Rd, Nanchang 330022, Jiangxi, Peoples R China.. The CAS is 99-04-7. Through research, I have a further understanding and discovery of 3-Methylbenzoic acid.

An unprecedented Ir-catalyzed oxidative coupling of benzoic acids with trifluoromethylated alkynes was successfully developed to provide diverse trifluoromethylated isocoumarins in moderate to good yields. This new practical procedure was highlighted by mild reaction conditions, broad substrate scope, good regioselectivity, high efficiency, and easy operation.

Application In Synthesis of 3-Methylbenzoic acid. About 3-Methylbenzoic acid, If you have any questions, you can contact Liu, GY; Kuang, GH; Zhang, XX; Lu, NH; Fu, Y; Peng, YY; Zhou, YR or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com