Design, Synthesis and Biological Evaluation of 2-Aminobenzimidazole Derivatives as DPP4 Inhibitors

2020 ◽  
Vol 16 (5) ◽  
pp. 696-702
Author(s):  
Sreeja Sunil ◽  
Arul G.D.A. Smith ◽  
Mathan S.
Keyword(s):  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Spectroscopic Techniques ◽  
Aminobenzoic Acid ◽  
Inhibitor Activity ◽  
Albino Rat ◽  
Discovery Studio ◽  
Dpp Iv ◽  
Dppiv Inhibitor

Background: The objective of the research was to examine the DPPIV inhibitor activity of synthetic derivatives of 2-aminobenzimidazole derivatives by the in-vivo method. Methods: Molecular docking was performed using homology model of receptors to identify the binding sites for the inhibitory activity of diabetes by means of- CDocker energy using the Discovery Studio (DS) 4.5 Novel 2-amino benzimidazole derivatives were synthesized from orthophenylene diamine with cyanogens bromide. The synthesized compounds were identified by IR,1HNMR,13CNMR, and MASS spectroscopic techniques. The products were analyzed for their DPPIV inhibitory effects on Wistar Albino rat. Results: The results revealed that benzimidazole with para-aminobenzoic acid possesses best DPPIV inhibitor activity. 2- amino benzimidazole incorporated with aromatic compounds were synthesized and assessed for their DPP-IV inhibitor activity. Conclusion: 2- amino benzimidazole with para-aminobenzoic acid can be used as a lead compound for the development of a new class of DPP-IV inhibitor.

scholarly journals Synthesis and Biological Evaluation of Some Piperazine Derivatives as Anti-Inflammatory Agents

2019 ◽  
Vol 9 (4-s) ◽  
pp. 353-358
Author(s):  
Nalini Patel ◽  
Vaishali Karkhanis ◽  
Pinkal Patel
Keyword(s):  
Mannich Bases ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Piperazine Derivatives ◽  
Rat Paw Edema ◽  
In Series ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Synthesis And Biological Evaluation

Some 1-((4-methylpiperazin-1yl)methyl)-1H-benzo[d]imidazole & 1-((4-phenylpiperazin-1yl)methyl)-1H-benzo[d]imidazole derivatives were synthesized through reaction of 1-substituted piperazines with different benzimidazole derivatives in methanol yielded the corresponding mannich bases (42-a to 42-i). All the synthesized compounds were elucidated by IR, 1H NMR and MASS spectroscopy. They were tested for anti-inflammatory activity using in-vivo (Carrageenan- induced rat paw edema model) method at a dose of 50mg/kg. result showed that compounds 42-c, 42-d and 42-h were found to be most potent in series. Keywords: 1,4-disubstituted Piperazine, Anti-inflammatory, Mannich Base.

scholarly journals Synthesis, Characterisation and Biological Evaluation of Substituted 4- ((1H-Benzo[d]Imidazol-2-YL) Methoxy) Coumarin Derivatives as Antimicrobial Agents

2019 ◽  
Vol 7 (02) ◽  
pp. 01-08
Author(s):  
Harpreet Kaur ◽  
Baljeet Singh
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Spectroscopic Techniques ◽  
Gram Negative Bacteria ◽  
Coumarin Derivatives ◽  
Gram Positive ◽  
Standard Drug ◽  
Gram Negative

A series of coumarin-benzimidazole derivatives i.e. 4-((1H-Benzo[d]imidazol-2- yl)methoxy)coumarin derivatives (7a-j) was synthesized by reacting appropriate starting materials and evaluated for its in vitro antimicrobial activity. The newly synthesized compounds have been characterized on the basis of elemental analyses, spectroscopic techniques (FT-IR). Antimicrobial studies of these compounds were performed against the both the Gram positive, MRSA (Staphylococcus aureus, Bacillus subtilis) as well as Gram negative (Escherichia coli) bacteria. The activity was investigated by using both Agar well diffusion as well as MIC assay. All the compounds were show significant bactericidal activity against all the pathogenic strains in comparison to Ciprofloxacin, a broad spectrum antibiotic against Gram positive and Gram negative bacteria. Most of the synthesized derivatives appeared as excellent antimicrobial agents as compared to standard drug Ciprofloxacin. Compound 7b was found to be the most active antibacterial agent against Gram positive as well as Gram negative bacteria.

scholarly journals Identification of Putative Plant Based Antiviral Compounds to Fight Against SARS-CoV-2 Infection

2020 ◽  
Author(s):  
Sujit Kumar Mishra ◽  
Rajguru Rajesh Raman Mishra ◽  
Saumya Dash ◽  
Jogeswar Panigrahi
Keyword(s):  
Nucleocapsid Protein ◽  
Rna Binding ◽  
Aminobenzoic Acid ◽  
Receptor Ligand ◽  
Discovery Studio ◽  
Antiviral Compounds ◽  
Pharmacokinetic Properties ◽  
Ligand Interactions

<p><i>Background: </i>This study aimed to examine the efficacy of some natural compounds and their derivatives in inhibiting the nucleocapsid protein N-terminal RNA binding domain (NSP-NTD), of SARS-CoV-2 virus by using the molecular doacking approach.</p> <p><i>Methods:</i> Physiochemical and drug likeness properties of the compounds were characterized by using SWISS ADME server tool. ADMET and TOPKAT modules of Discovery studio 4.0 were used for prediction of pharmacokinetic properties and toxicity of the compounds. Molecular docking of the ligands with the target protein (NSP-NTD) was carried out using the receptor-ligand interactions module of DS 4.0. The CDOCKER energy, CDOCKER interaction energy and binding energy of the interactions were calculated to identify the best interacting compounds.</p> <p><i>Results:</i> Four compounds including 4-hydroxybenzoic acid, benzoic acid, 4-aminobenzoic acid and salicylic acid have been predicted as effective compounds to inhibit the NSP-NTD (responsible for packing the viral RNA into the crown like capsid) <i>vis-à-vis</i> combat the SARS-Cov-2 virus infection. </p> <p><i>Conclusions:</i> <i>In vitro</i> and <i>in vivo</i> evaluation of these compounds against SARS-CoV-2 virus is required prior to assuring their potential roles in SARS-CoV-2 infection control.</p>

scholarly journals Identification of Putative Plant Based Antiviral Compounds to Fight Against SARS-CoV-2 Infection

2020 ◽  
Author(s):  
Sujit Kumar Mishra ◽  
Rajguru Rajesh Raman Mishra ◽  
Saumya Dash ◽  
Jogeswar Panigrahi
Keyword(s):  
Nucleocapsid Protein ◽  
Rna Binding ◽  
Aminobenzoic Acid ◽  
Receptor Ligand ◽  
Discovery Studio ◽  
Antiviral Compounds ◽  
Pharmacokinetic Properties ◽  
Ligand Interactions

<p><i>Background: </i>This study aimed to examine the efficacy of some natural compounds and their derivatives in inhibiting the nucleocapsid protein N-terminal RNA binding domain (NSP-NTD), of SARS-CoV-2 virus by using the molecular doacking approach.</p> <p><i>Methods:</i> Physiochemical and drug likeness properties of the compounds were characterized by using SWISS ADME server tool. ADMET and TOPKAT modules of Discovery studio 4.0 were used for prediction of pharmacokinetic properties and toxicity of the compounds. Molecular docking of the ligands with the target protein (NSP-NTD) was carried out using the receptor-ligand interactions module of DS 4.0. The CDOCKER energy, CDOCKER interaction energy and binding energy of the interactions were calculated to identify the best interacting compounds.</p> <p><i>Results:</i> Four compounds including 4-hydroxybenzoic acid, benzoic acid, 4-aminobenzoic acid and salicylic acid have been predicted as effective compounds to inhibit the NSP-NTD (responsible for packing the viral RNA into the crown like capsid) <i>vis-à-vis</i> combat the SARS-Cov-2 virus infection. </p> <p><i>Conclusions:</i> <i>In vitro</i> and <i>in vivo</i> evaluation of these compounds against SARS-CoV-2 virus is required prior to assuring their potential roles in SARS-CoV-2 infection control.</p>

scholarly journals Identification of Putative Plant Based Antiviral Compounds to Fight Against SARS-CoV-2 Infection

2020 ◽  
Author(s):  
Sujit Kumar Mishra ◽  
Rajguru Rajesh Raman Mishra ◽  
Saumya Dash ◽  
Jogeswar Panigrahi
Keyword(s):  
Nucleocapsid Protein ◽  
Rna Binding ◽  
Aminobenzoic Acid ◽  
Receptor Ligand ◽  
Discovery Studio ◽  
Antiviral Compounds ◽  
Pharmacokinetic Properties ◽  
Ligand Interactions

<p><i>Background: </i>This study aimed to examine the efficacy of some natural compounds and their derivatives in inhibiting the nucleocapsid protein N-terminal RNA binding domain (NSP-NTD), of SARS-CoV-2 virus by using the molecular doacking approach.</p> <p><i>Methods:</i> Physiochemical and drug likeness properties of the compounds were characterized by using SWISS ADME server tool. ADMET and TOPKAT modules of Discovery studio 4.0 were used for prediction of pharmacokinetic properties and toxicity of the compounds. Molecular docking of the ligands with the target protein (NSP-NTD) was carried out using the receptor-ligand interactions module of DS 4.0. The CDOCKER energy, CDOCKER interaction energy and binding energy of the interactions were calculated to identify the best interacting compounds.</p> <p><i>Results:</i> Four compounds including 4-hydroxybenzoic acid, benzoic acid, 4-aminobenzoic acid and salicylic acid have been predicted as effective compounds to inhibit the NSP-NTD (responsible for packing the viral RNA into the crown like capsid) <i>vis-à-vis</i> combat the SARS-Cov-2 virus infection. </p> <p><i>Conclusions:</i> <i>In vitro</i> and <i>in vivo</i> evaluation of these compounds against SARS-CoV-2 virus is required prior to assuring their potential roles in SARS-CoV-2 infection control.</p>

Benzimidazole Derivatives as Potential Antimicrobial and Antiulcer Agents: A Mini Review

2019 ◽  
Vol 19 (16) ◽  
pp. 1292-1297 ◽  
Author(s):  
Ali Mohd Ganie ◽  
Ayaz Mahmood Dar ◽  
Fairooz Ahmad Khan ◽  
Bashir Ahmad Dar
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
1H Nmr ◽  
13C Nmr ◽  
Benzimidazole Derivatives ◽  
Spectroscopic Techniques ◽  
One Pot ◽  
Biological Screening ◽  
Elemental Analyses ◽  
Characterization Studies

:Here in we report the number of strategies for the synthesis of differently substituted benzimidazole derivatives. The protocols involved in the syntheses of these derivatives were one-pot or multi-component. The characterization studies of these derivatives were carried by using different spectroscopic techniques (1H NMR, 13C NMR and MS) and elemental analyses. The biological screening studies revealed that these benzimidazole derivatives show potential antibacterial as well as antifungal behavior. These benzimidazole derivatives not only depicted potential antiulcer properties but also showed moderate to good anticancer/cytotoxic behavior against different cancer cell lines.

Novel Thiazole-Based Thiazolidinones as Potent Anti-infective Agents: In silico PASS and Toxicity Prediction, Synthesis, Biological Evaluation and Molecular Modelling

2020 ◽  
Vol 23 (2) ◽  
pp. 126-140 ◽  
Author(s):  
Christophe Tratrat
Keyword(s):  
In Silico ◽  
Antimicrobial Agents ◽  
Target Identification ◽  
Biological Evaluation ◽  
Microbial Infection ◽  
Toxicity Prediction ◽  
Discovery Studio ◽  
Bacteria And Fungi ◽  
Multiple Drugs ◽  
Antibacterial And Antifungal

Aims and Objective: The infectious disease treatment remains a challenging concern owing to the increasing number of pathogenic microorganisms associated with resistance to multiple drugs. A promising approach for combating microbial infection is to combine two or more known bioactive heterocyclic pharmacophores in one molecular platform. Herein, the synthesis and biological evaluation of novel thiazole-thiazolidinone hybrids as potential antimicrobial agents were dissimilated. Materials and Methods: The preparation of the substituted 5-benzylidene-2-thiazolyimino-4- thiazolidinones was achieved in three steps from 2-amino-5-methylthiazoline. All the compounds have been screened in PASS antibacterial activity prediction and in a panel of bacteria and fungi strains. Minimum inhibitory concentration and minimum bacterial concentration were both determined by microdilution assays. Molecular modeling was conducted using Accelrys Discovery Studio 4.0 client. ToxPredict (OPEN TOX) and ProTox were used to estimate the toxicity of the title compounds. Results: PASS prediction revealed the potentiality antibacterial property of the designed thiazolethiazolidinone hybrids. All tested compounds were found to kill and to inhibit the growth of a vast variety of bacteria and fungi, and were more potent than the commercial drugs, streptomycin, ampicillin, bifomazole and ketoconazole. Further, in silico study was carried out for prospective molecular target identification and revealed favorable interaction with the target enzymes E. coli MurB and CYP51B of Aspergillus fumigatus. Toxicity prediction revealed that none of the active compounds was found toxic. Conclusion: Substituted 5-benzylidene-2-thiazolyimino-4-thiazolidinones, endowing remarkable antibacterial and antifungal properties, were identified as a novel class of antimicrobial agents and may find a potential therapeutic use to eradicate infectious diseases.

Synthesis and Biological Evaluation of Scutellarein Alkyl Derivatives as Preventing Neurodegenerative Agents with Improved Lipid Soluble Properties

2019 ◽  
Vol 15 (7) ◽  
pp. 771-780
Author(s):  
He-Min Li ◽  
Ting Gu ◽  
Wen-Yu Wu ◽  
Shao-Peng Yu ◽  
Tian-Yuan Fan ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Neuronal Damage ◽  
Thiobarbituric Acid ◽  
Rat Hepatocytes ◽  
Biological Evaluation ◽  
Thiobarbituric Acid Reactive Substance ◽  
Alkyl Derivatives ◽  
Promising Therapeutic Approach ◽  
Microsomal Membranes

Background: Exogenous antioxidants are considered as a promising therapeutic approach to treat neurodegenerative diseases since they could prevent and/or minimize the neuronal damage by oxidation. Objective: Three series of lipophilic compounds structurally based on scutellarein (2), which is one metabolite of scutellarin (1) in vivo, have been designed and synthesized. Methods: Their antioxidant activity was evaluated by detecting the 2-thiobarbituric acid reactive substance (TBARS) produced in the ferrous salt/ascorbate-induced autoxidation of lipids, which were present in microsomal membranes of rat hepatocytes. The lipophilicity of these compounds indicated as partition coefficient between n-octanol and buffer was investigated by ultraviolet (UV) spectrophotometer. Results: This study indicated that compound 5e which had a benzyl group substituted at the C4'- OH position showed a potent antioxidant activity and good lipophilicity. Conclusion: 5e could be an effective candidate for preventing or reducing the oxidative status associated with the neurodegenerative processes.

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