Design, synthesis and biological evaluation of novel 1,2,4-triazolo and 1,2,4-triazino[4,3-a]quinoxalines as potential anticancer and antimicrobial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (1) ◽  
pp. 202-211 ◽  
Author(s):  
Doaa A. E. Issa ◽  
Nargues S. Habib ◽  
Abeer E. Abdel Wahab
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Compound 9a showed dual anticancer and antimicrobial activity and compound 16 showed a broad spectrum antimicrobial activity.

scholarly journals Design, Synthesis and Biological Evaluation of New Piperazin-4-yl-(acetyl-thiazolidine-2,4-dione) Norfloxacin Analogues as Antimicrobial Agents

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3959 ◽  
Author(s):  
Marc ◽  
Araniciu ◽  
Oniga ◽  
Vlase ◽  
Pîrnău ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Binding Mode ◽  
Biological Properties ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Parent Molecule ◽  
Synthesis And Biological Evaluation

 In an effort to improve the antimicrobial activity of norfloxacin, a series of hybrid norfloxacin–thiazolidinedione molecules were synthesized and screened for their direct antimicrobial activity and their anti-biofilm properties. The new hybrids were intended to have a new binding mode to DNA gyrase, that will allow for a more potent antibacterial effect, and for activity against current quinolone-resistant bacterial strains. Moreover, the thiazolidinedione moiety aimed to include additional anti-pathogenicity by preventing biofilm formation. The resulting compounds showed promising direct activity against Gram-negative strains, and anti-biofilm activity against Gram-positive strains. Docking studies and ADMET were also used in order to explain the biological properties and revealed some potential advantages over the parent molecule norfloxacin.

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF SPIRO (INDOLE-THIAZOLIDINE) DERIVATIVES AS ANTIMICROBIAL AGENTS

2019 ◽  
pp. 71-74
Author(s):  
PRIYANKA NIVRUTTI SHINDE ◽  
MANISH ASHOK RASKAR
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Biological Evaluation ◽  
Mercaptoacetic Acid ◽  
Ir Absorption ◽  
Absorption Bands ◽  
Synthesis And Biological Evaluation ◽  
Anhydrous Zncl2

Objective: The present study aims to synthesize and biological evaluation of Spiro-[Indole-Thiazolidine] derivatives as antimicrobial agents. Methods: The reaction sequence involves microwave-induced preparation of N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene)pyridine-4-carbohydrazide [3] from isoniazid [1] and isatin [2] followed by the cyclo condensation of [3] and mercaptoacetic acid under microwave condition to achieve the synthesis of spiro-[indole-thiazolidine] derivatives [4]. The resulting compounds were then allowed to react with various aromatic and heterocyclic aromatic aldehydes to afford arylidene derivatives [5a-l]. Result: Isoniazid (1) on condensation with isatin (2) in the presence of catalytic amount of glacial acetic acid furnished N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene) pyridine-4-carbohydrazide (3), which showed characteristic IR, absorption bands. Compound (3) underwent Spiro cyclization upon its reaction with mercaptoacetic acid in the presence of anhydrous ZnCl2 to form spiro-[indole-thiazolidine] compound (4). Compound (4) was then condensed with aromatic aldehydes to give arylidene derivatives (5a-l), which were characterized by IR and 1H NMR spectral data. Conclusion: All the synthesized compounds were screened for antimicrobial activity by the cup plate method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria.

scholarly journals Design, Synthesis and Biological Evaluation ofN-Sulfonylphenyl glyoxamide-Based Antimicrobial Peptide Mimics as Novel Antimicrobial Agents

2017 ◽  
Vol 2 (12) ◽  
pp. 3452-3461 ◽  
Author(s):  
Tsz Tin Yu ◽  
Shashidhar Nizalapur ◽  
Kitty K. K. Ho ◽  
Eugene Yee ◽  
Thomas Berry ◽  
...  
Keyword(s):  
Antimicrobial Peptide ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Peptide Mimics ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, Synthesis, and Biological Evaluation of Thieno[2,3-c]pyrazole Hydrazide Derivatives as Potential Antimicrobial Agents

2015 ◽  
Vol 54 (1) ◽  
pp. 44-50 ◽  
Author(s):  
Pravin S. Mahajan ◽  
Mukesh D. Nikam ◽  
Asha V. Chate ◽  
Anil S. Bobade ◽  
Charansingh H. Gill
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of Benzimidazole-pyridine- Piperidine Hybrids as a New Class of Potent Antimicrobial Agents

2014 ◽  
Vol 12 (1) ◽  
pp. 38-45 ◽  
Author(s):  
Kothapally. Beulah ◽  
Akula Kumara ◽  
Boddupally Lingaiah ◽  
Pamulaparthy Rao ◽  
Banda Narsaiah ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
New Class ◽  
Synthesis And Biological Evaluation

Design, Synthesis, and Biological Evaluation of Hexacyclic Tetracyclines as Potent, Broad Spectrum Antibacterial Agents

2015 ◽  
Vol 58 (11) ◽  
pp. 4703-4712 ◽  
Author(s):  
Cuixiang Sun ◽  
Diana K. Hunt ◽  
Chi-Li Chen ◽  
Yonghong Deng ◽  
Minsheng He ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
Sign in / Sign up

Export Citation Format

Share Document