Synthesis, Characterization and Antimicrobial Screening of Sulphonamide Based 1, 3, 4-Oxadiazoles

Dholaria, Piyush; Parikh, Kalpesh; Joshi, Durga Datt; Joshi, Abhishek

doi:10.30731/ijcps.7.2.2018.13-26

Cited by 2 publications

(3 citation statements)

References 22 publications

(38 reference statements)

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“…In general, SAR studies showed that the presence of electron withdrawing groups (viz.-Cl, -Br and -NO 2 ) at para and ortho positions (R) improved the antibacterial activity as compared to electron-releasing groups, except in compound 47, with CH 3 group increased the activity. In view of above findings, it can be concluded that position of different substituents on phenyl ring of 1,3,4oxadiazole derivatives affecting the antibacterial and antifungal activities (Table 20) [63]. 22).…”

Section: Antibacterial and Antifungal Activities Of 25-disubstituted-...mentioning

confidence: 84%

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Antimicrobial Activity and Sar of 2,5-Disubstituted 1,3,4-Oxadiazole Derivatives

Kumar

Narang

Devgun

et al. 2022

JASR

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1,3,4-oxadiazole is a five membered heterocyclic aromatic moiety, present in a number of antimicrobial agents. 2,5- disubstituted 1,3,4-oxadiazole derivatives have shown broad spectrum of antibacterial and antifungal activities. Many scientific groups have synthesized and screened their antimicrobial potential. Reported activity data showed that some 1,3,4-oxadiazole derivatives exhibited better activity than already known antibiotics. Hence, they can be used as lead for development of promising antimicrobial agents. In present review, antimicrobial activities and SAR of 2,5-disubstituted 1,3,4-oxadiazole derivatives reported by different research groups in last ten years have been summarized.

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Section: Antibacterial and Antifungal Activities Of 25-disubstituted-...mentioning

confidence: 84%

“…Ciprofloxacin but lower against E. faecalis (MIC = 250 µg/mL) (Table26). Whereas, compounds(61)(62)(63)(64)(65) showed less antifungal activity against C. albicans and A. niger (MIC = 250 µm/mL) as compared to standard drug Fluconazole. Overall it can be concluded that…”

mentioning

confidence: 98%

Antimicrobial Activity and Sar of 2,5-Disubstituted 1,3,4-Oxadiazole Derivatives

Kumar

Narang

Devgun

et al. 2022

JASR

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“…These agents are present in various drugs, most vitamins, many natural products, biomolecules, and biologically active compounds [ 1 – 7 ]. Oxadiazoles, an essential family of this class, have significant biological activities, such as analgesic, anti-inflammatory, anticonvulsive, antiemetic, fungicidal, diuretic, muscle relaxant, and antioxidant activity [ 8 – 10 ]. Oxadiazoles have different isomers.…”

Section: Introductionmentioning

confidence: 99%

Cytotoxic effect, enzyme inhibition, and in silico studies of some novel N-substituted sulfonyl amides incorporating 1,3,4-oxadiazol structural motif

et al. 2022

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The acetylcholinesterase and carbonic anhydrase inhibitors (AChEIs and h CAIs) remain key therapeutic agents for many bioactivities such as anti-Alzheimer and antiobesity antiepileptic, anticancer, antiinfective, antiglaucoma, and diuretic effects. Here, it has been attempted to discover novel multi-target AChEIs and h CAIs that are highly potent, orally bioavailable, may be brain penetrant, and have higher effectiveness at lower doses than tacrine and acetazolamide. After detailed investigations both in vitro and in silico, novel N -substituted sulfonyl amide derivatives ( 6a–j ) were determined to be highly potent inhibitors for AChE and h CAs ( K I s are in the range of 23.11–52.49 nM, 18.66–59.62 nM, and 9.33–120.80 nM for AChE, h CA I, and h CA II, respectively). Moreover, according to the cytotoxic effect studies, such as the ADME-Tox, cortex neuron cells, and neuroblastoma SH-SY5Y cell line, compounds 6a , 6d , and 6h , which are the most potent representative versus the target enzymes, were identified as orally bioavailable, highly selective, and brain preferentially distributed AChEIs and h CAIs. The docking studies revealed precise binding modes between 6a , 6d , and 6h and h CA II, h CA I, and AChE, respectively. The results presented here might provide a solid basis for further investigation into more potent AChEIs and h CAIs. Graphical abstract Supplementary Information The online version contains supplementary material available at 10.1007/s11030-022-10422-8.

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Synthesis, Characterization and Antimicrobial Screening of Sulphonamide Based 1, 3, 4-Oxadiazoles

Abstract: A new series of

Cited by 2 publications

References 22 publications

Antimicrobial Activity and Sar of 2,5-Disubstituted 1,3,4-Oxadiazole Derivatives

Antimicrobial Activity and Sar of 2,5-Disubstituted 1,3,4-Oxadiazole Derivatives

Cytotoxic effect, enzyme inhibition, and in silico studies of some novel N-substituted sulfonyl amides incorporating 1,3,4-oxadiazol structural motif

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