Synthesis, Antibacterial and Antifungal Activity of 2,5- Disubstituted-1,3,4-oxadiazole Derivatives (original) (raw)
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2014
A novel series of 2-(5-substituted)-1,3,4-oxadiazole-2-yl)-H-imidazo[1,2,α]pyridine derivatives 5a-i and 6a-d are synthesized and characterized by IR, H NMR, C NMR and Mass spectral analysis. All the synthesized compounds were tested for there antibacterial and antifungal activity of which compound 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 6a, 6c and 6d exhibited good antimicrobial activity.
International Journal of Research in Pharmacy and Pharmaceutical Sciences
A new series of some pyridine condensed oxadiazole derivatives were prepared by reacting pyridine derivative with various aromatic carboxylic acids. In the present work 9 different 2, 5-disubstituted 1, 3, 4 oxadiazole derivatives (3a-i) were synthesized. Pyridine 4-carboxylic acid (Nicotinic acid) is converted into methyl pyridine 4-carboxlate by esterification. Pyridine 4-carboxlate is converted to pyridine 4-carbohydrazide (Isoniazid) by treating with hydrazine hydrate. Pyridine 4-carbohydrazide is converted to 2, 5-disubstituted 1, 3, 4 oxadiazole derivatives by treating with different types of aromatic carboxylic acids in the presence of POCl3. Confirmation of the chemical structure of the synthesized compounds was substantiated by TLC, IR, 1H NMR, and MS spectroscopy. All the synthesized compounds were tested for in-vitro antibacterial (against Escherichia coli, Bacillus subtilis, Staphylococcus aureus) and antifungal activity (against Aspergillus niger). 5e, 5i, 5b, 5d showed...
Arabian Journal of Chemistry, 2014
A series of 2,5-disubstitued-1,3,4-oxadiazole derivatives bearing pyrazole moiety were synthesized by reacting various substituted pyrazole-4-carboxylic acids with different hydrazides in POCl 3. All the synthesized compounds (4a-n) were characterized by IR, NMR, mass spectra and elemental analyses. Synthesized 1,3,4-oxadiazole derivatives were screened for their antibacterial activity against three different strains, namely Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, while antifungal activity was determined against three different strains Aspergillus flavus, Chrysosporium keratinophilum and Candida albicans. The investigation of antimicrobial screening revealed that compounds 4i and 4j exhibited excellent activity when compared with the standard drugs.
Synthesis and antimicrobial activity of some novel oxadiazole derivatives
Acta Poloniae Pharmaceutica, 2008
A new class of 3,5-disubstituted pyrazoles and isoxazoles were prepared from the Michael acceptors 1-furanyl / thiophenyl / pyridinyl-3-indole-prop-2-en-1-ones under ultrasonication and evaluated for antimicrobial activity. Amongst all the tested compounds fluoro substituted thiophene linked compounds 12b and 18b displayed promising antibacterial activity particularly against Bacillus subtilis and antifungal activity against Aspergillus niger. Furthermore, compounds with more number of electron withdrawing groups showed higher antimicrobial activity. This result indicates that compounds 12b and 18b can be used as lead compounds in the future studies.
Synthesis of Novel Imidazole Compounds and Evaluation of Their Antimicrobial Activity
Indo Global Journal of Pharmaceutical Sciences
Imidazoles are an important class of heterocycles and include many substances of both biological and chemical interest. Insertion of the imidazole nucleus is an important synthetic strategy in drug discovery. Imidazole drugs have broad applications in many areas of clinical medicine. These are currently used as tools in pharmacological studies. The important therapeutic properties of imidazole related drugs have encouraged the medicinal chemists to synthesize and test a large number of novel molecules. In this investigation, it was of interest to synthesize imidazole by refluxing 9, 10-phenenthraquinone with aryl aldehyde, primary amines and ammonium acetate in the presence of glacial acetic acid and a novel series of imidazole derivatives. The structures of the compounds have been established on the basis of spectral analytical data. All the derivatives have been screened for their antimicrobial activities at the 100µg/ml and 200µg/ml against Candida albicans. © 2011 IGJPS. All rig...
Synthesis and anti-bacterial, anti-fungal activity of novel 1,2,4-oxadiazole
Journal of chemical and pharmaceutical research, 2011
A series of novel 1, 2, 4-oxadiazole derivatives were synthesized and evaluated for in- vitro antibacterial and antifungal activity. All the compounds tested against bacteria showed comparable or less antibacterial activities than the reference drug. Differences in their activity depend on the substitution of different groups. More specifically, best antibacterial activity among synthetic analogues was shown by compound 6 with MIC of 10 I¼g/ml and compound 14 with MIC of 50 I¼g/ml against Bacillus subtilis. All compounds tested showed significant antifungal activity against all the fungi, compared to the commercial fungicide Miconazole. Among them compounds 4 and 8 showed good antifungal activity against Fusarium solani with MIC of 10 and 50 I¼g/ml
Synthesis and Biological Evaluation of some 2, 5-Disubstituted-1, 3, 4-Oxadiazole Derivatives
ijdddonline.com
Synthesis of some new 2, 5-diaryl-1, 3, 4-oxadiazole derivatives starting from Isoniazide (INH) is described. The target compounds 11-20 were obtained by treating INH with various aromatic aldehydes and monosaccharides to give corresponding Schiff 's bases 1-10, which upon subsequent oxidation, by using either method A, B or C, yielded desired compounds. They were purified and characterized by spectroscopic techniques and elemental analyses. These compounds were evaluated for antibacterial, antifungal and antiviral activities. Compounds 11, 16 and 17 exhibited good antibacterial and antifungal activity, however, none of the compounds were enough active against various strains of virus.
Synthesis of New Imidazole Derivatives as Effective Antimicrobial Agents
World Journal of Pharmacy and Pharmaceutical Sciences, 2019
In the present work, some new imidazole derivatives (3i-xii) were synthesized as per design synthetic protocol scheme. The structures of newly prepared compounds were confirmed by modern analytical technique (IR, 1 H-NMR, Mass spectral data) and elemental analysis, results found in full agreement with their assigned structures. All the synthetic compounds were screened for their antimicrobial activity against bacterial strains viz. Escherichia coli (E. coli, MTCC 2961), Staphylococcus aureus (S. aureus, MTCC 3160), Bacillus subtilis (B. subtilis, MTCC 121), Klebsiella pneumoniae (K. pneumoniae, MTCC 3040) and Micrococcus luteus (M. luteus, MTCC 7527)) and fungal strains viz. Candida albicans (C. albicans, MTCC 227), Aspergillus niger (A. niger, MTCC 277) and Aspergillus flavus (A. flavus, MTCC 418); results showed good to remarkable activity. The MIC (minimum inhibitory concentration) values were determined by comparison to ciprofloxacin (anti-bacterial) and fluconazole (anti-fungal) as standard drug. Among them, compound 3iv and 3x exhibited notable antimicrobial activity.