Synthesis and Biological Evaluation of Some Novel Pyrrole Derivatives

2021 ◽  
pp. 5749-5754
Author(s):  
Saurabh Bhardwaj ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Tumor Model ◽  
Biological Evaluation ◽  
Cytotoxic Action ◽  
Gram Positive ◽  
Pyrrole Derivatives ◽  
Gram Negative ◽  
Mass Spectral ◽  
Death Time ◽  
Standard Medication ◽  
Cox 2 Inhibitors

The Pyrrole is one of the significant classes of heterocyclic mixes having pharmacological and natural exercises, for example, antibacterial, antifungal, anthelmintic. The subbed pyrroles with chose functionalities at various position fill in as antecedents for the combination of different new functionalities. Pyrrole has additionally indicated wide organic exercises, for example, treatment of hyperlipidemias, mitigating, COX1/COX-2 inhibitors, 6 cytotoxic action against strong tumor model and assortment of marine and human models. A progression of new Schiff base (E)- N'- Substituted benzylidene-1H-pyrrole-2-carbohydrazide subsidiary (3a-3j) were combined by the response of 1H-pyrrole-2-carbohydrazide and fragrant aldehyde within the sight of ethanol with barely any drops of frosty acidic corrosive. The response blend was observed by TLC and recrystallized from wanted dissolvable. FTIR, 1HNMR, mass spectral and natural investigation were affirmed the structure of the blended mixes. All orchestrated mixes were screened against traditional strains for their antibacterial, antifungal and anthelmintic tasks: gram positive is B.subtilis, and S.aureus and gram negative are E. coli. Antifungal movement was screened against C. Albicans and A. niger and anthelmintic movement was screened against M. konkanensis and P. corethruses. The outcomes uncovered that 3f, 3g and 3i display increasingly strong action against the both two microorganism (gram negative and gram positive bacteria) on the opposite side compound 3a, 3g and 3h show progressively intense movement against the two growths (C. Albicans and A. niger) and compound 3c and 3d having most powerful movement with mean paralyzing time of 11.27 mins and 15.83 mins and mean death time of 19.25 mins and 24.45 mins individually when contrasted with standard medication.

scholarly journals Microwave Assisted Synthesis and Antimicrobial Evaluation of Schiff Bases of Indole-3-aldehyde

2011 ◽  
Vol 8 (1) ◽  
pp. 305-311 ◽  
Author(s):  
Priyanka Kamaria ◽  
N. Kawathekar ◽  
Prerna Chaturvedi
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Microwave Assisted Synthesis ◽  
Bacterial Strains ◽  
Mass Spectral Analysis ◽  
Gram Positive ◽  
Gram Negative ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Antimicrobial Evaluation

In order to develop new antimicrobial agents, a series of Schiff bases of indole-3-aldehyde were synthesized by microwave assisted synthesis by takingDMFas solvent and evaluated for their antimicrobial activity. All the synthesized compounds were characterized byIR,1HNMRand mass spectral analysis. All compounds were tested against five gram positive and five gram negative bacterial strains and one fungal strain. All compounds exhibited better activity against gram positive strains than against gram negative strains and the compounds were found more active againstS.aureusandB.subtilis.

scholarly journals DESIGN, SYNTHESIS, DOCKING STUDIES AND BIOLOGICAL EVALUATION OF 2-PHENYL-3-(SUBSTITUTED BENZO[d] THIAZOL-2-YLAMINO)-QUINAZOLINE-4(3H)-ONE DERIVATIVES AS ANTIMICROBIAL AGENTS

2018 ◽  
Vol 10 (10) ◽  
pp. 57
Author(s):  
Pooja Pisal ◽  
Meenakshi Deodhar ◽  
Amol Kale ◽  
Ganesh Nigade ◽  
Smita Pawar
Keyword(s):  
Antimicrobial Agents ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Fusion Reactions ◽  
Gram Positive ◽  
Gram Negative

Objective: A new series 2-phenyl-3-(substituted benzo[d] thiazol-2-ylamino)-quinazoline-4(3H)-one was prepared by the fusion method by reacting 2-phenyl benzoxazine with 2-hydrazino benzothiazole and it was evaluated for their antimicrobial activity against gram positive, gram negative bacteria and fungi.Methods: Titled compounds were synthesized by fusion reactions. These compounds were evaluated by in vitro antibacterial and antifungal activity using the minimum inhibitory concentration and zone of inhibition methods. The synthesized compounds were characterized with the help of infrared, NMR and mass spectral studies. The benzothiazole moiety and the quinazoline ring have previously shown DNA gyrase inhibition and target related antibacterial activity. Thus, molecular docking studies of synthesized compounds were carried out (PDB: 3G75) to study the possible interaction of compounds with the target. The batch grid docking was performed to determine the probable.Results: These compounds showed significant activity against gram positive and gram negative bacteria as well against the fungi. The compound A5 was found to be active against B. subtilis, P aeruginosa and C. albican at 12.5 µg/ml MIC. The compound A3 was found to be active against all microbial strains selected at 25 and 12.5 µg/ml MIC.Conclusion: Though the relationship between the activities shown by these compounds in, the antimicrobial study is still to be established, the docking studies conducted found to be consistent with antimicrobial results. Thus the results indicate that the designed structure can be a potential lead as an antimicrobial agent.

Synthesis, Characterization and Biological Evaluation of Ethyl-4'-(cyclopropane carboxamido-N-yl)-5-ary-3-oxo-3,4,5,6-tetrahydro-biphenyl-4-carboxylate

2019 ◽  
Vol 4 (4) ◽  
pp. 240-243
Author(s):  
P.M. Akbari ◽  
V.R. Shah
Keyword(s):  
Sodium Hydroxide ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Antimicrobial Drugs ◽  
Gram Negative ◽  
Mass Data ◽  
Condensation Method ◽  
Cyclohexenone Derivatives

A series of new substituted cyclohexenone derivatives have been synthesized by the reaction of various substituted chalcones with ethylacetoacetate. Some new N-(4-(3-aryl-acryloyl)phenyl)cyclopropane carboxamide were prepared by Claisen-Schmidt condensation method in presence of sodium hydroxide in ethanol solvent under stirring. The synthesized compounds were characterized by their spectral (IR, NMR, Mass) data and screened for their antimicrobial activities against Gram-positive and Gram-negative bacteria by using standard antimicrobial drugs.

scholarly journals Synthesis of certain pyrrole derivatives as antimicro-bial agents

2009 ◽  
Vol 59 (2) ◽  
pp. 145-158 ◽  
Author(s):  
Mosaad Mohamed ◽  
Ramdan El-Domany ◽  
Rania Abd El-Hameed
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Amines ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Pyrrole Derivatives ◽  
Gram Negative ◽  
Primary Aromatic Amines ◽  
Aryl Amines ◽  
Bacteria And Fungi

Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds was carried out against Gram-positive, Gram-negative bacteria and fungi. Some of the prepared compounds, [2-amino-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrole-3-carbonitriles (1b), 2-amino-3-carbamoyl-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrroles (2b),N-(3-cyano-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3b),N-(3-cyano-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3c), 2-amino-1-(4-methoxyphenyl)-4,5-diphenyl-3-tetrazolo-1H-pyrroles (5d),7-(4-methoxyphenyl)-5,6-diphenyl-7H-pyrrolo [2,3-d]pyrimidin-4(3H)-ones (7d), 7-(3-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-thione (9b) andN-(7-(2-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d] pyrimidine)-N-aryl amines (10a)] showed potent antimicrobial activity.

scholarly journals Design, Synthesis, and Biological Evaluation of Light-Activated Antibiotics

2021 ◽  
Author(s):  
Inga S. Shchelik ◽  
Andrea Tomio ◽  
Karl Gademann
Keyword(s):  
Small Molecules ◽  
Uv Light ◽  
Biological Evaluation ◽  
Biological Processes ◽  
Good Activity ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
Synthetic Sequence ◽  
Synthesis And Biological Evaluation

<p>The spatial and temporal control of bioactivity of small molecules by light (photopharmacology) constitutes a promising approach for study of biological processes and ultimately for the treatment of diseases. In this study, we investigated two different ‘caged’ antibiotic classes that can undergo remote activation with UV-light at λ=365 nm, via the conjugation of deactivating and photocleavable units through a short synthetic sequence. The two widely used antibiotics vancomycin and cephalosporin were thus enhanced in their performance by rendering them photoresponsive and thus suppressing undesired off-site activity. The antimicrobial activity against <i>Bacillus subtilis</i> ATCC 6633, <i>Staphylococcus aureus</i> ATCC 29213, <i>S. aureus</i> ATCC 43300 (MRSA), <i>Escherichia coli</i> ATCC 25922, and <i>Pseudomonas aeruginosa</i> ATCC 27853 could be spatiotemporally controlled with light. Both molecular series displayed a good activity window. The vancomycin derivative displayed excellent values against Gram-positive strains after uncaging, and the next-generation caged cephalosporin derivative achieved good and broad activity against both Gram-positive and Gram-negative strains after photorelease.</p>

scholarly journals SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SUBSTITUTED 1,3,4-OXADIAZOLE DERIVATIVE: DERIVED FROM CIPROFLOXACIN

2019 ◽  
pp. 205-209
Author(s):  
ANUJ SINGHAI ◽  
M.K. GUPTA
Keyword(s):  
Antibacterial Activity ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Gram Positive ◽  
Standard Drug ◽  
Gram Negative ◽  
Oxadiazole Derivatives ◽  
Gram Negative Organisms ◽  
Derivatives Of

Objective: The purpose of this research is synthesized and evaluates different derivatives of oxadiazole. Methods: A novel series of substituted 1,3,4-oxadiazole derivative were synthesized by condensing different amine with 1-cyclopropyl-6-fluoro-7- (piperazin-1-yl)-3-(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)quinolin-4(1H)-one (III) in the presence of formaldehyde. The structure of these novel synthesized compounds was characterized on the bases of physicochemical and spectral analysis. The title compounds (IVa-h) were screened for antibacterial activity by disc diffusion method. Results: Substituted 1,3,4-oxadiazole derivative was synthesized, characterized, and evaluated for antibacterial activity. Compounds IVa, IVd, IVe, IVf, and IV h showed enhance activities then ciprofloxacin against all Gram-positive and Gram-negative organisms. Compound IVe showed the highest activity against Staphylococcus aureus and compound IV showed the highest activity against Escherichia coli. Conclusion: The present study demonstrates the synthesis and characterization of 1,3,4-oxadiazole derivatives derived from ciprofloxacin. These compounds were evaluated for antibacterial activity against different Gram-positive and Gram-negative organism. In some cases, antibacterial activity is found to be enhanced as compared to standard drug ciprofloxacin.

scholarly journals Design, Synthesis and Biological Evaluation of Biphenylglyoxamide-Based Small Molecular Antimicrobial Peptide Mimics as Antibacterial Agents

2020 ◽  
Vol 21 (18) ◽  
pp. 6789
Author(s):  
Tsz Tin Yu ◽  
Rajesh Kuppusamy ◽  
Muhammad Yasir ◽  
Md. Musfizur Hassan ◽  
Amani Alghalayini ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Quaternary Ammonium ◽  
Lipid Membranes ◽  
Bacterial Infections ◽  
Biological Evaluation ◽  
In Vitro Toxicity ◽  
Ammonium Iodide ◽  
Gram Positive ◽  
Gram Negative

There has been an increasing interest in the development of antimicrobial peptides (AMPs) and their synthetic mimics as a novel class of antibiotics to overcome the rapid emergence of antibiotic resistance. Recently, phenylglyoxamide-based small molecular AMP mimics have been identified as potential leads to treat bacterial infections. In this study, a new series of biphenylglyoxamide-based small molecular AMP mimics were synthesised from the ring-opening reaction of N-sulfonylisatin bearing a biphenyl backbone with a diamine, followed by the conversion into tertiary ammonium chloride, quaternary ammonium iodide and guanidinium hydrochloride salts. Structure–activity relationship studies of the analogues identified the octanesulfonyl group as being essential for both Gram-positive and Gram-negative antibacterial activity, while the biphenyl backbone was important for Gram-negative antibacterial activity. The most potent analogue was identified to be chloro-substituted quaternary ammonium iodide salt 15c, which possesses antibacterial activity against both Gram-positive (MIC against Staphylococcus aureus = 8 μM) and Gram-negative bacteria (MIC against Escherichia coli = 16 μM, Pseudomonas aeruginosa = 63 μM) and disrupted 35% of pre-established S. aureus biofilms at 32 μM. Cytoplasmic membrane permeability and tethered bilayer lipid membranes (tBLMs) studies suggested that 15c acts as a bacterial membrane disruptor. In addition, in vitro toxicity studies showed that the potent compounds are non-toxic against human cells at therapeutic dosages.

scholarly journals Synthesis, characterization and biological evaluation of a new photoactive hydrogel against Gram-positive and Gram-negative bacteria

2016 ◽  
Vol 4 (8) ◽  
pp. 1499-1509 ◽  
Author(s):  
Cinzia Spagnul ◽  
John Greenman ◽  
Mark Wainwright ◽  
Zeeniya Kamil ◽  
Ross W. Boyle
Keyword(s):  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative

Development of a cheap material active against both Gram-positive and Gram-negative bacteria to be used as a novel water-sterilizing device.

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 Antibacterial and Antitubercular Activity of Novel Benzothiazole- Aryl Amine Derivatives Tethered through Acetamide Functionality

2021 ◽  
Vol 33 (8) ◽  
pp. 1757-1763
Author(s):  
Farhana Hakim ◽  
S. Roshan Salfidoer
Keyword(s):  
Escherichia Coli ◽  
Antitubercular Activity ◽  
Salmonella Typhi ◽  
Klebsiella Pneumonia ◽  
High Potency ◽  
Gram Positive ◽  
Gram Negative ◽  
Mass Spectral ◽  
Mycobacterial Strain ◽  
Mic Value

A novel series of substituted benzothiazole-N-phenyl acetamides were synthesized through a feasible scheme and characterized by IR, 1H NMR and mass spectral methods. All the synthesized compounds were screened for antibacterial activity against two, Gram-positive strains: Staphylococcus aureus, Bacillus subtilis; four, Gram-negative strains: Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa and Klebsiella pneumonia; and antitubercular activity against mycobacterial strain: Mycobacterium tuberculosis. Among the 15 compounds (6a-o) tested, three compounds 6e, 6l and 6m have demonstrated high potency with MIC values ranges from 6.25-12.5 μg/mL against both Gram-positive and Gram-negative strains. Compounds 6e and 6l displayed remarkable antitubercular activity with MIC value of 25 μg/mL.

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