Synthesis and Anticancer Evaluation of some Newer 2, 5-Disubstituted-1,3, 4-Oxadiazole Analogues

Somani, Rakesh R.; Shirodkar, P. Y.; Kadam, Vilasrao J.

doi:10.2174/157018008785777360

Cited by 10 publications

(3 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The second stage of synthesizing heterocyclic compounds is designing of the new prepared compounds based structurally on containing other biologically active heterocycles on side chains reported in the field of cancer therapy such as pyrazoles and oxadiazoles . This aim pushes authors to synthesize some interesting heterocyclic compounds, for example, pyrazole and/or oxadiazole derivatives incorporated with pyridazinone nucleus.…”

Section: Resultsmentioning

confidence: 99%

Synthesis of Novel Heterocyclic Compounds with Expected Antibacterial Activities from 4‐(4‐Bromophenyl)‐4‐oxobut‐2‐enoic Acid

El‐Hashash

Soliman

Bakeer

et al. 2014

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

Section: Resultsmentioning

confidence: 99%

Synthesis of Novel Heterocyclic Compounds with Expected Antibacterial Activities from 4‐(4‐Bromophenyl)‐4‐oxobut‐2‐enoic Acid

El‐Hashash

Soliman

Bakeer

et al. 2014

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

“…Especially, 1,3,4‐oxadiazole is widely studied by the chemists due to its pharmacophore feature for ligand binding . A great number of pharmacological properties have been associated with this small but important core structure such as anti‐inflammatory , antimicrobial , antitubercular , and anticancer . Non‐steroidal anti‐inflammatory drugs (NSAIDs) are good choice to use for the treatment of pain, fever, and inflammation, particularly arthritis .…”

Section: Introductionmentioning

confidence: 99%

Some Novel Mannich Bases of 5‐(3,4‐Dichlorophenyl)‐1,3,4‐oxadiazole‐2(3H)‐one and Their Anti‐Inflammatory Activity

Koksal

Ozkan-Dagliyan

Ozyazici

et al. 2017

Archiv der Pharmazie

View full text Add to dashboard Cite

Non-steroidal anti-inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group existing on their chemical structure is correlated with GI toxicity related with all routine NSAIDs. Replacing this functional group with the 1,3,4-oxadiazole bioisostere is a generally used strategy to obtain an anti-inflammatory agent devoid of GI side effects. In the present work, a novel group of 5-(3,4-dichlorophenyl)-1,3,4-oxadiazole-2(3H)-one Mannich bases were synthesized and characterized on the basis of IR, H NMR, and elemental analysis results. The target compounds were first tested for cytotoxicity to determine a non-toxic concentration for anti-inflammatory screening. Anti-inflammatory effects of the compounds were evaluated by in vitro lipopolysaccharide (LPS)-induced NO production and in vivo carrageenan footpad edema with ulcerogenic profile. In LPS-induced RAW 264.7 macrophages, most of the compounds showed inhibitory activity on nitrite production while compounds 5a, 5h, and 5j exhibited the best profiles by suppressing the NO production. To evaluate the in vivo anti-inflammatory potency of the compounds, the inflammatory response was quantified by increment in paw size in the carrageenan footpad edema assay. The anti-inflammatory data scoring showed that compounds 5a-d, 5g, and 5j, at the dose of 100 mg/kg, exhibited anti-inflammatory activity, which for compound 5g was comparable to that of the reference drug indomethacin with 53.9% and 55.5% inhibition in 60 and 120 min, respectively.

show abstract

“…Synthesis of 1,3,4-oxadiazole containing compounds and investigation of their chemical and biological properties has accelerated in recent years. 1,3,4-Oxadiazole represents an important class of biologically active species which exhibits antibacterial [1], antibiotic [2], antiviral [3], anti inflammatory [4], pesticidal [5], antiallergic [6], analgesic [7,8], ocular hypotensive [9], antimalarial [10], anticancer [11,12], anticonvulsant [13,14], antitumor [15][16][17], herbicidal [18], angiogenesis inhibitor [19], antiedema [20], anti obesity [21], antioxidant [22], anti-infective [23], anti HIV [24], antiparasitic [25], antihyperglycemic [26], anxiolytic [27],antidepressant [28], antiproliferative [29], antiplatelet [30] and gastric antisecretory activities [31]. Most of the drugs which are available in the market contains 1,3,4-oxadiazole unit.…”

Section: Introductionmentioning

confidence: 99%

A Review on the Preparation of 1,3,4-Oxadiazoles From the Dehydration of Hydrazines and Study of Their Biological Roles

Nayak

Poojary

2019

Chemistry Africa

View full text Add to dashboard Cite

Heterocyclic chemistry is the interesting area for the effective approach and for the invention of biologically active 1,3,4-oxadiazole cores. 1,3,4-Oxadiazole is a five membered heterocyclic ring which plays key role in the development of new medicinal species for the treatment of numerous diseases. Hence, nowadays researchers have developed the innovative methods for the synthesis of 1,3,4-oxadiazole derivatives and their medicinal applications. Therefore, results of recent developments in the synthesis and biological applications of 1,3,4-oxadiazole candidates over the past 15 years (2005-2019) are reviewed in the present article. The information in the present article may be useful to many researchers which lead to exploration of new therapeutic species for the society.

show abstract

Synthesis and Anticancer Evaluation of some Newer 2, 5-Disubstituted-1,3, 4-Oxadiazole Analogues

Cited by 10 publications

References 0 publications

Synthesis of Novel Heterocyclic Compounds with Expected Antibacterial Activities from 4‐(4‐Bromophenyl)‐4‐oxobut‐2‐enoic Acid

Synthesis of Novel Heterocyclic Compounds with Expected Antibacterial Activities from 4‐(4‐Bromophenyl)‐4‐oxobut‐2‐enoic Acid

Some Novel Mannich Bases of 5‐(3,4‐Dichlorophenyl)‐1,3,4‐oxadiazole‐2(3H)‐one and Their Anti‐Inflammatory Activity

A Review on the Preparation of 1,3,4-Oxadiazoles From the Dehydration of Hydrazines and Study of Their Biological Roles

Contact Info

Product

Resources

About