Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives

Raval, Jignesh P.; Akhaja, Tarunkumar Nanjibhai; Jaspara, Dhaval M.; Myangar, Kruti Navin; Patel, Nilesh H.

doi:10.1016/j.jscs.2011.05.019

Cited by 26 publications

(18 citation statements)

References 15 publications

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“…The first site is the sulfonamide group (─SO 2 NH─) which acts as an antimetabolite and competes with p ‐aminobenzoic acid for incorporation into folic acid. Thus, bacterial growth is limited through folate deficiency without effect on human cells …”

Section: Resultsmentioning

confidence: 99%

Effect of the formation of silver nano‐binuclear complex on the refinement of cytotoxic and antibacterial potency of coumarin Schiff base: Spectroscopy, thermal, X‐ray diffraction analyses and density functional theory calculations

El-Ansary

Moustafa

Abdel-Kader

et al. 2019

Applied Organom Chemis

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A new Schiff base (SCH) was prepared using 8‐acetyl‐7‐hydroxy‐4‐methylcoumarin and sulfaclozine. Its silver complex was also synthesized. These compounds were subjected to elemental and spectral analyses. The silver complex was also subjected to thermogravimetric analysis, molar conductance measurements, scanning electron microscopy, energy‐dispersive X‐ray analysis and X‐ray diffraction measurements. The formula of the complex was determined as [(Ag2SCH(NO3)2]. The molar conductance indicates its non‐electrolyte character. The electronic structure and nonlinear optical parameters of SCH and its complex were investigated theoretically at the B3LYP/GENECP level. The geometry of the studied complex is non‐planar as indicated from the dihedral angles between central Ag metal ion and coordinated centres of SCH. Density functional theory calculations were also carried out to calculate the global properties of hardness, global softness and electronegativity. The calculated energy gap between HOMO and LUMO energies shows that charge transfer occurs within the studied complex. The total static dipole moment, the mean polarizability, the anisotropy of the polarizability and the mean first‐order hyperpolarizability were calculated and compared with those of urea as a reference material. The results of the mean first‐order hyperpolarizability showed that SCH and its silver complex are excellent candidates as nonlinear optical materials. The compounds were screened for their antimicrobial effect against various species of bacteria and fungi. Their anticancer activities were evaluated in vitro against the human cancer cell line MCF‐7 (human breast adenocarcinoma).

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Section: Resultsmentioning

confidence: 99%

Effect of the formation of silver nano‐binuclear complex on the refinement of cytotoxic and antibacterial potency of coumarin Schiff base: Spectroscopy, thermal, X‐ray diffraction analyses and density functional theory calculations

El-Ansary

Moustafa

Abdel-Kader

et al. 2019

Applied Organom Chemis

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“…A series of 2(4‐pyridyl)‐5[(aryl/heteroarylamino)‐1‐oxoethyl]thio‐1,3,4‐oxadiazoles were synthesized by Ravel et al., resulting in identification of compounds 135 – 137 that caused more than 90% inhibition of M. tuberculosis at low concentrations ranged between 0.0052 and 0.0089 μM (Fig. ) …”

Section: Oxadiazolesmentioning

confidence: 99%

New structural classes of antituberculosis agents

Kumar

Patel

Jain

2017

Medicinal Research Reviews

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Tuberculosis (TB), one of the deadliest diseases is shattering the health and socioeconomic status of the society. The emergence of multidrug resistant (MDR) and extremely drug resistant (XDR) strains has provided unprecedented lethal character to TB. The development of MDR and XDR strains of TB results in more deaths, longer duration of therapy, and appearance of the disease in the immunocompromised patients. Because of the development of rapid resistance by Mycobacterium tuberculosis, researchers are confronted with serious challenges in combating TB. For instance, the need for potency and specificity in therapeutic agents approaching clinics, and the increasing demand of low toxicity due to long duration of treatment. Recently, it is proposed that such challenges could be addressed by a shift from contemporary or known classes of drugs to new scaffold-containing or entirely new structural classes of drugs that possibly act on the previously unknown targets, resulting in possibly less instances of resistance development. The exploitation of advances made in the biology of TB in the last and present decades have created opportunities to discover a large number of new structural classes that specifically targets TB by molecular mechanism of action(s) unknown earlier. We have earlier reviewed new structural classes of anti-TB agents up to year 2005. This review covers literature reports of the subsequent 10 years on the discovery of new structural classes of synthetic anti-TB agents. Due to the availability of large number of research reports, we have divided new compounds in 38 structural classes, 368 structures, and 307 references.

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“…1,2 Due to their structural diversity their biological activities include antibacterial, 3,4 antitubercular, antifungal, cytotoxic, anticancer, 5,6 and many others. So far, our work has been based on the synthesis of 1,3,4-oxadiazoles, which are present in some well-known drugs like Furamizole (antibiotic), Raltegravir (antiretroviral), Zibotentan (anticancer), and tiodazosin and nesapidil (antihypertensive).…”

Section: Introductionmentioning

confidence: 99%

Biological study on novel coumarinyl 1,3,4-oxadiazoles

Molnar¹,

Amić²,

Pavić³

et al. 2018

Turk J Chem

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Coumarinyl 1,3,4-oxadiazoles were synthesized from Schiff bases and acetic anhydride. All compounds were characterized by melting points and their structures confirmed by mass and 1 H and 13 C NMR spectrometry.These novel coumarinyl derivatives were subjected to antibacterial, antifungal, antaflatoxigenic, and antioxidant activity.Their activity varied depending on their structure, where 2-(3-acetyl-5-(((4-methyl-2-oxo-2 H -chromen-7-yl)oxy)methyl)-2,3-dihydro-1,3,4-oxadiazol-2-yl)-1,4-phenylene diacetate showed significant antioxidant and antibacterial activity on B.subtilis. 4-(3-Acetyl-5-(((4-methyl-2-oxo-2 H -chromen-7-yl)oxy)methyl)-2,3-dihydro-1,3,4-oxadiazol-2-yl)-1,2-phenylene diacetate was found to possess excellent antifungal and antiaflatoxigenic activity.

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Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives

Cited by 26 publications

References 15 publications

Effect of the formation of silver nano‐binuclear complex on the refinement of cytotoxic and antibacterial potency of coumarin Schiff base: Spectroscopy, thermal, X‐ray diffraction analyses and density functional theory calculations

Effect of the formation of silver nano‐binuclear complex on the refinement of cytotoxic and antibacterial potency of coumarin Schiff base: Spectroscopy, thermal, X‐ray diffraction analyses and density functional theory calculations

New structural classes of antituberculosis agents

Biological study on novel coumarinyl 1,3,4-oxadiazoles

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