Tag: M.W=150-200

An article Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19 WOS:000592734300030 published article about CYSTEINE PROTEASE; ALDEHYDE INHIBITORS; IN-VITRO; BIOLOGICAL EVALUATION; ANTIVIRAL ACTIVITY; SARS-CORONAVIRUS; FORMAZAN ASSAY; DESIGN; AG7088; PAPAIN in [Hoffman, Robert L.; Kania, Robert S.; Brothers, Mary A.; Davies, Jay F.; Ferre, Rose A.; Gajiwala, Ketan S.; He, Mingying; Kozminski, Kirk; Li, Lilian Y.; Lockner, Jonathan W.; Lou, Jihong; Marra, Michelle T.; Mitchell, Lennert J., Jr.; Murray, Brion W.; Nieman, James A.; Noell, Stephen; Planken, Simon P.; Ryan, Kevin; Smith, George J., III; Solowiej, James E.; Steppan, Claire M.] Pfizer Worldwide Res & Dev, San Diego, CA 92121 USA; [Hogan, Robert J.; Rowe, Thomas; Taggart, Barbara] Southern Res Inst, Birmingham, AL 35205 USA in 2020, Cited 45. SDS of cas: 385-00-2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

The novel coronavirus disease COVID-19 that emerged in 2019 is caused by the virus SARS CoV-2 and named for its close genetic similarity to SARS CoV-1 that caused severe acute respiratory syndrome (SARS) in 2002. Both SARS coronavirus genomes encode two overlapping large polyproteins, which are cleaved at specific sites by a 3C-like cysteine protease (3CL(pro)) in a post-translational processing step that is critical for coronavirus replication. The 3CL(pro) sequences for CoV-1 and CoV-2 viruses are 100% identical in the catalytic domain that carries out protein cleavage. A research effort that focused on the discovery of reversible and irreversible ketone-based inhibitors of SARS CoV-1 3CL(pro) employing ligand-protease structures solved by X-ray crystallography led to the identification of 3 and 4. Preclinical experiments reveal 4 (PF-00835231) as a potent inhibitor of CoV-2 3CL(pro) with suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.

SDS of cas: 385-00-2. Welcome to talk about 385-00-2, If you have any questions, you can contact Hoffman, RL; Kania, RS; Brothers, MA; Davies, JF; Ferre, RA; Gajiwala, KS; He, MY; Hogan, RJ; Kozminski, K; Li, LLY; Lockner, JW; Lou, JH; Marra, MT; Mitchell, LJ; Murray, BW; Nieman, JA; Noell, S; Planken, SP; Rowe, T; Ryan, K; Smith, GJ; Solowiej, JE; Steppan, CM; Taggart, B or send Email.

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

In 2019.0 J MOL STRUCT published article about ONE-POT SYNTHESIS; CARRIER PROTEIN REDUCTASE; MULTICOMPONENT SYNTHESIS; GREEN SYNTHESIS; EFFICIENT; ANTIBACTERIAL; CATALYST; FACILE; VITRO; ACID in [Vasava, Mahesh S.; Rathwa, Sanjay K.; Patel, Hitesh D.] Gujarat Univ, Sch Sci, Dept Chem, Ahmadabad, Gujarat, India; [Bhoi, Manoj N.] Piramal Enterprise Ltd, Plot 18, Ahmadabad, Gujarat, India; [Shetty, Shilpa S.; Patel, Rikin D.; Pandya, Himanshu A.] Gujarat Univ, Sch Sci, Dept Bot Bioinformat & Climate Change Impacts Man, Ahmadabad, Gujarat, India; [Rajani, Dhanji P.; Rajani, Smita D.] Microcare Lab, Surat, Gujarat, India; [Rajani, Dhanji P.; Rajani, Smita D.] TB Res Ctr, Surat, Gujarat, India; [Patel, Alpesh] Genxplore Diagnost & Res Ctr Pvt Ltd, Ahmadabad, Gujarat, India in 2019.0, Cited 66.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Formula: C9H10O3

In the present study, a series of novel and biologically potent 6-amino-1-(2,4-dinitrophenyl)-4-phenyl-1,4-dihydropyrano [2,3-clpyrazole-5-carbonitrile derivatives (5a-5u) have been synthesized through multicomponent reaction between various substituted aromatic aldehyde derivative (4a-4u), 2, 4-dinitrophenyl hydrazine (1), ethyl acetoacetate (2) and malononitrile (3) in the presence of SnCl 2 as a prompt catalyst using both microwave irradiation method as well as conventional method. The structure of synthesized compounds were confirmed by various spectroscopic methods such as H-1 NMR, C-13 NMR, IR, Mass analysis and elemental analysis. All the synthesized compounds were subjected in vitro antibacterial, anti-tuberculosis screening and cytotoxicity MTT assay. In vitro biological study revealed that the synthesized compound 5a, 7a and 8a are showing good anti-bacterial and anti-tuberculosis activity. The in silico study of ADME pharmacokinetic properties were also predicted for synthesized compounds for checking their bioavailability. Furthermore, molecular docking study of synthesized compounds with enoyl-ACP reductase (oxidoreductase) was carry out to find out the binding affinity of compounds. Docking study demonstrated that compound 7b and 7a possessed superior binding affinity with target enzyme by strong hydrogen bonding. We have also carried out molecular dynamics simulation to check the stability of docked complex, conformational changes and primary molecular interaction. (C) 2018 Elsevier B.V. All rights reserved.

Formula: C9H10O3. Welcome to talk about 93-02-7, If you have any questions, you can contact Vasava, MS; Bhoi, MN; Rathwa, SK; Shetty, SS; Patel, RD; Rajani, DP; Rajani, SD; Patel, A; Pandya, HA; Patel, HD or send Email.

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

Hatley, RJD; Barrett, TN; Slack, RJ; Watson, ME; Baillache, DJ; Gruszka, A; Washio, Y; Rowedder, JE; Pogany, P; Pal, S; Macdonald, SJF in [Hatley, Richard J. D.; Barrett, Tim N.; Slack, Robert J.; Watson, Morag E.; Baillache, Daniel J.; Gruszka, Anna; Washio, Yoshiaki; Rowedder, James E.; Pogany, Peter; Pal, Sandeep; Macdonald, Simon J. F.] GlaxoSmithKline GSK, Med Res Ctr, Gunnels Wood Rd, Stevenage SG1 2NY, Herts, England published The Design of Potent, Selective and Drug-Like RGD alpha v beta 1 Small-Molecule Inhibitors Derived from non-RGD alpha 4 beta 1 Antagonists in 2019, Cited 39. COA of Formula: C7H4F2O2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

Up to 45 % of deaths in developed nations can be attributed to chronic fibroproliferative diseases, highlighting the need for effective therapies. The RGD (Arg-Gly-Asp) integrin alpha v beta 1 was recently investigated for its role in fibrotic disease, and thus warrants therapeutic targeting. Herein we describe the identification of non-RGD hit small-molecule alpha v beta 1 inhibitors. We show that alpha v beta 1 activity is embedded in a range of published alpha 4 beta 1 (VLA-4) ligands; we also demonstrate how a non-RGD integrin inhibitor (of alpha 4 beta 1 in this case) was converted into a potent non-zwitterionic RGD integrin inhibitor (of alpha v beta 1 in this case). We designed urea ligands with excellent selectivity over alpha 4 beta 1 and the other alpha v integrins (alpha v beta 3, alpha v beta 5, alpha v beta 6, alpha v beta 8). In silico docking models and density functional theory (DFT) calculations aided the discovery of the lead urea series.

COA of Formula: C7H4F2O2. Bye, fridends, I hope you can learn more about C7H4F2O2, If you have any questions, you can browse other blog as well. See you lster.

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

Authors Shalini; Pankaj; Saha, ST; Kaur, M; Oluwakemi, E; Awolade, P; Singh, P; Kumar, V in ROYAL SOC CHEMISTRY published article about DERIVATIVES; CHALCONE; DESIGN; AMONAFIDE; DOCKING; INHIBITORS; APOPTOSIS; BINDING; BCL-2 in [Shalini; Pankaj; Kumar, Vipan] Guru Nanak Dev Univ, Dept Chem, Amritsar 143005, Punjab, India; [Saha, Sourav Taru; Kaur, Mandeep] Univ Witwatersrand, Sch Mol & Cell Biol, Private Bag 3, ZA-2050 Johannesburg, South Africa; [Oluwakemi, Ebenezer; Awolade, Paul; Singh, Parvesh] Univ Kwazulu Natal, Sch Chem & Phys, P Bag X54001, ZA-4000 Durban, South Africa in 2020.0, Cited 39.0. Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

A series of naphthalimide-chalcone/pyrazoline conjugates was prepared and evaluated for their anti-breast cancer potential against estrogen responsive, i.e. MCF-7 (ER+), and triple-negative, i.e. MDA-MB-231 (ER-), cell lines. The structure-activity-relationship (SAR) was deduced based on the influence of linker length, substituents on the phenyl ring and the generated functionalities, on anti-proliferative activities. Docking simulations further delineate the type of interactions of the designed molecules with the selected targets. This report discloses the scope of triazole tethered naphthalimide-chalcone/pyrazoline conjugates as anti breast cancer agents.

Formula: C9H10O3. Welcome to talk about 93-02-7, If you have any questions, you can contact Shalini; Pankaj; Saha, ST; Kaur, M; Oluwakemi, E; Awolade, P; Singh, P; Kumar, V or send Email.

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

COA of Formula: C7H4F2O2. Recently I am researching about MULTIDRUG-RESISTANCE; MOLECULAR-MECHANISMS; CANCER-CELLS; GLYCOPROTEIN; BIOAVAILABILITY; REVERSAL, Saw an article supported by the Major New Drugs Innovation and Development of National Science and Technology Major Projects [2018ZX09711002-007-005]. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Guo, YL; Wang, K; Chen, XY; Li, HH; Wan, Q; Morris-Natschke, S; Lee, KH; Chen, Y. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid

Twenty-five seco-4-methyl-DCK derivatives were designed, synthesized and evaluated for chemoreversal activity when combined with paclitaxel or vincristine in two drug-resistant cancer cell lines (A2780/T and KB-V) respectively. Most of the new compounds displayed moderate to significant MDR reversal activities in the P-gp overexpressing A2780/T and KB-V cells. Especially, compounds 7o and 7y showed the most potent chemosensitization activities with more than 496 and 735 reversal ratios at a concentration of 10 mu M. Unexpectedly the newly synthesized compounds did not show chemosensitization activities observed in a non-P-gp overexpressing cisplatin resistant human ovarian cancer cell line (A2780/CDDP), implying that the MDR reversal effects might be associated with P-gp overexpression. Moreover, these compounds did not exhibit significant antiproliferative activities against nontumorigenic cell lines (HUVEC, HOSEC and T29) compared to the positive control verapamil at the tested concentration, which suggested better safety than verapamil. The pharmacological actions of the compounds will be studied further to explore their merit for development as novel candidates to overcome P-gp mediated MDR cancer.

Bye, fridends, I hope you can learn more about C7H4F2O2, If you have any questions, you can browse other blog as well. See you lster.. COA of Formula: C7H4F2O2

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

Hatley, RJD; Barrett, TN; Slack, RJ; Watson, ME; Baillache, DJ; Gruszka, A; Washio, Y; Rowedder, JE; Pogany, P; Pal, S; Macdonald, SJF in [Hatley, Richard J. D.; Barrett, Tim N.; Slack, Robert J.; Watson, Morag E.; Baillache, Daniel J.; Gruszka, Anna; Washio, Yoshiaki; Rowedder, James E.; Pogany, Peter; Pal, Sandeep; Macdonald, Simon J. F.] GlaxoSmithKline GSK, Med Res Ctr, Gunnels Wood Rd, Stevenage SG1 2NY, Herts, England published The Design of Potent, Selective and Drug-Like RGD alpha v beta 1 Small-Molecule Inhibitors Derived from non-RGD alpha 4 beta 1 Antagonists in 2019, Cited 39. COA of Formula: C7H4F2O2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

Up to 45 % of deaths in developed nations can be attributed to chronic fibroproliferative diseases, highlighting the need for effective therapies. The RGD (Arg-Gly-Asp) integrin alpha v beta 1 was recently investigated for its role in fibrotic disease, and thus warrants therapeutic targeting. Herein we describe the identification of non-RGD hit small-molecule alpha v beta 1 inhibitors. We show that alpha v beta 1 activity is embedded in a range of published alpha 4 beta 1 (VLA-4) ligands; we also demonstrate how a non-RGD integrin inhibitor (of alpha 4 beta 1 in this case) was converted into a potent non-zwitterionic RGD integrin inhibitor (of alpha v beta 1 in this case). We designed urea ligands with excellent selectivity over alpha 4 beta 1 and the other alpha v integrins (alpha v beta 3, alpha v beta 5, alpha v beta 6, alpha v beta 8). In silico docking models and density functional theory (DFT) calculations aided the discovery of the lead urea series.

COA of Formula: C7H4F2O2. Bye, fridends, I hope you can learn more about C7H4F2O2, If you have any questions, you can browse other blog as well. See you lster.

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

Authors Shalini; Pankaj; Saha, ST; Kaur, M; Oluwakemi, E; Awolade, P; Singh, P; Kumar, V in ROYAL SOC CHEMISTRY published article about DERIVATIVES; CHALCONE; DESIGN; AMONAFIDE; DOCKING; INHIBITORS; APOPTOSIS; BINDING; BCL-2 in [Shalini; Pankaj; Kumar, Vipan] Guru Nanak Dev Univ, Dept Chem, Amritsar 143005, Punjab, India; [Saha, Sourav Taru; Kaur, Mandeep] Univ Witwatersrand, Sch Mol & Cell Biol, Private Bag 3, ZA-2050 Johannesburg, South Africa; [Oluwakemi, Ebenezer; Awolade, Paul; Singh, Parvesh] Univ Kwazulu Natal, Sch Chem & Phys, P Bag X54001, ZA-4000 Durban, South Africa in 2020.0, Cited 39.0. Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

A series of naphthalimide-chalcone/pyrazoline conjugates was prepared and evaluated for their anti-breast cancer potential against estrogen responsive, i.e. MCF-7 (ER+), and triple-negative, i.e. MDA-MB-231 (ER-), cell lines. The structure-activity-relationship (SAR) was deduced based on the influence of linker length, substituents on the phenyl ring and the generated functionalities, on anti-proliferative activities. Docking simulations further delineate the type of interactions of the designed molecules with the selected targets. This report discloses the scope of triazole tethered naphthalimide-chalcone/pyrazoline conjugates as anti breast cancer agents.

Formula: C9H10O3. Welcome to talk about 93-02-7, If you have any questions, you can contact Shalini; Pankaj; Saha, ST; Kaur, M; Oluwakemi, E; Awolade, P; Singh, P; Kumar, V or send Email.

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

COA of Formula: C7H4F2O2. Recently I am researching about MULTIDRUG-RESISTANCE; MOLECULAR-MECHANISMS; CANCER-CELLS; GLYCOPROTEIN; BIOAVAILABILITY; REVERSAL, Saw an article supported by the Major New Drugs Innovation and Development of National Science and Technology Major Projects [2018ZX09711002-007-005]. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Guo, YL; Wang, K; Chen, XY; Li, HH; Wan, Q; Morris-Natschke, S; Lee, KH; Chen, Y. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid

Twenty-five seco-4-methyl-DCK derivatives were designed, synthesized and evaluated for chemoreversal activity when combined with paclitaxel or vincristine in two drug-resistant cancer cell lines (A2780/T and KB-V) respectively. Most of the new compounds displayed moderate to significant MDR reversal activities in the P-gp overexpressing A2780/T and KB-V cells. Especially, compounds 7o and 7y showed the most potent chemosensitization activities with more than 496 and 735 reversal ratios at a concentration of 10 mu M. Unexpectedly the newly synthesized compounds did not show chemosensitization activities observed in a non-P-gp overexpressing cisplatin resistant human ovarian cancer cell line (A2780/CDDP), implying that the MDR reversal effects might be associated with P-gp overexpression. Moreover, these compounds did not exhibit significant antiproliferative activities against nontumorigenic cell lines (HUVEC, HOSEC and T29) compared to the positive control verapamil at the tested concentration, which suggested better safety than verapamil. The pharmacological actions of the compounds will be studied further to explore their merit for development as novel candidates to overcome P-gp mediated MDR cancer.

Bye, fridends, I hope you can learn more about C7H4F2O2, If you have any questions, you can browse other blog as well. See you lster.. COA of Formula: C7H4F2O2

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

I found the field of Chemistry very interesting. Saw the article Surfactant-assisted assembly of nanoscale zinc coordination compounds to enhance tandem conversion reactions in water published in 2019. Quality Control of 2,6-Difluorobenzoic acid, Reprint Addresses Mi, LW (corresponding author), Zhongyuan Univ Technol, Ctr Adv Mat Res, Zhengzhou 450007, Henan, Peoples R China.; Hou, HW (corresponding author), Zhengzhou Univ, Coll Chem & Mol Engn, Zhengzhou 450001, Henan, Peoples R China.. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid

Precise control over the morphology and size of coordination polymers (CPs) is crucial for extending these inorganic-organic materials to many advanced applications, in particular for heterogeneous catalysis. In this work, two Zn-based CPs, {[Zn-3(idbt)(2)(4,4 ‘-dmbpy)(2)]center dot H2O}(n) (1) and {[Zn-3(idbt)(2)(H2O)(3)]center dot H2O}(n) (2) (H(3)idbt = 5,5 ‘-(1H-imidazole-4,5-diyl)-bis-(2H-tetrazole), 4,4 ‘-dmbpy = 4,4 ”-dimethyl-2,2 ‘-bipyridine), were synthesized through solvothermal reactions. The morphologies and particle sizes of 1 and 2 could be controlled from large scale to nanoscale by regulating the amount of poly(vinyl alcohol) (PVA). Furthermore, for the conversion reactions of nitromethylbenzenes into benzoic acids, the catalytic properties of nanoscale 1 and 2 were much more efficient than those of large size of 1 and 2, because of the benefit of readily accessible active sites in the nanoscale sized particles, which provide a tunable and functionalizable platform for the conversion reaction by minimizing the diffusion distance but do little for the selectivity.

Quality Control of 2,6-Difluorobenzoic acid. Welcome to talk about 385-00-2, If you have any questions, you can contact Huang, C; Zhu, KF; Zhang, YY; Lu, GZ; Shao, ZC; Gao, K; Mi, LW; Hou, HW or send Email.

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

An article Antimalarial, antiproliferative, and apoptotic activity of quinoline-chalcone and quinoline-pyrazoline hybrids. A dual action WOS:000489305700020 published article about BETA-HEMATIN FORMATION; IN-VITRO; POTENTIAL ANTIMALARIAL; MOLECULAR-MECHANISM; HEMOZOIN FORMATION; MALARIA; ANTICANCER; QUERCETIN; DERIVATIVES; INHIBITION in [Charris, Jaime E.; Monasterios, Melina C.; Acosta, Maria E.; Rodriguez, Miguel A.; Gamboa, Neira D.] Cent Univ Venezuela, Fac Pharm, Biochem Unit, Organ Synth Lab, Los Chaguaramos 1041-A, Caracas 47206, Venezuela; [Martinez, Gricelis P.; Mijares, Michael R.] Cent Univ Venezuela, Fac Pharm, Biotechnol Unit, Los Chaguaramos 1041-A, Caracas 47206, Venezuela; [Rojas, Hector R.; Mijares, Michael R.; De Sanctis, Juan B.] Cent Univ Venezuela, Fac Med, Inst Immunol, Los Chaguaramos 1050-A, Caracas 50109, Venezuela; [De Sanctis, Juan B.] Palacky Univ, Fac Med, Inst Mol & Translat Med, Hnevotinska 1333-5, Olomouc 77900, Czech Republic in 2019, Cited 62. Recommanded Product: 93-02-7. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

A series of quinoline-chalcone (E)-1-[3 or 4-(7-chloroquinolin-4-ylamino) phenyl]-3-(phenyl substituted) prop-2-ene-1-one (4, 5), and quinoline-pyrazoline hybrids 7-Chloro-N-[3 or 4-(4,5-dihydro-5-(phenyl-substituted)-1H-pyrazol-3-yl] phenyl) quinoline-4-amine (6, 7) were synthesized with the aim of achieving an antimalarial and anticancer dual action. Most of the compounds showed significant inhibition (%>80) of beta-hematin formation. The existing structures were tested in vivo as potential antimalarials in mice infected with P. berghei ANKA, chloroquine susceptible strain. Some of the compounds exhibited antimalarial activity comparable to that of chloroquine. Moreover, the compounds induce cell death on two human cancer cell lines (Jurkat E6.1 and HL60) without affecting the primary culture of human lymphocytes. Flow cytometry analysis confirmed the increase in apoptotic cell death after 24 h. Based on the structural analysis, these quinoline hybrids represent new compounds potentially useful for malaria end leukemia treatments.

Welcome to talk about 93-02-7, If you have any questions, you can contact Charris, JE; Monasterios, MC; Acosta, ME; Rodriguez, MA; Gamboa, ND; Martinez, GP; Rojas, HR; Mijares, MR; De Sanctis, JB or send Email.. Recommanded Product: 93-02-7

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