Medicinal Chemistry Research

, Volume 27, Issue 5, pp 1309–1344 | Cite as

The synthetic and therapeutic expedition of isoxazole and its analogs

Review Paper


Isoxazole, constituting an important family of five-membered heterocycles with one oxygen atom and one nitrogen atom at adjacent positions is of immense importance because of its wide spectrum of biological activities and therapeutic potential. It is, therefore, of prime importance that the development of new synthetic strategies and designing of new isoxazole derivatives should be based on the most recent knowledge emerging from the latest research. This review is an endeavor to highlight the progress in the chemistry and biological activity of isoxazole derivatives which could provide a low-height flying bird’s eye view of isoxazole derivatives to the medicinal chemists for the development of clinically viable drugs using this information.


Heterocyclic Isoxazole Biological activity Anticancer Anti-inflammatory Antimicrobial 



5-hydroxy tryptamine

A. clavatus

Aspergillus clavatus

A. fumigates

Aspergillus fumigatus

A. niger

Aspergillus niger




Adrenergic receptor

B. cinerea

Botrytis cinerea

B. subtilis

Bacillus subtilis


Blood-brain barrier

C. albicans

Candida albicans

C. elegans

Caenorhabditis elegans

C. neoformans

Cryptococcus neoformans

C. tropicum

Chrysosporium tropicum


Carbonic anhydrase


Cyclin-dependent kinase


Casein kinase


Central nervous system





D. myceliophagus

Ditylenchus myceliophagus


Diacylglycerol acyl transferase


Dipeptidyl peptidse



E. coli

Escherichia coli

E. faecalis

Enterococcus faecalis

E. floccosum

Epidermophyton floccosum


Effective concentration


Effective dose


Enzyme-linked immunosorbent assay


Exchange proteins directly activated by cAMP


5-lipoxygenase-activating protein


FMS-like tyrosine kinase


Ferric-ion reducing antioxidant power


Farnesoid X receptor


γ-amino butyric acid


Histone deacetylase


High density lipoprotein


Human immunodeficiency virus


Human microvascular endothelial cells


Heat shock protein


Herpes simplex virus


High-throughput screening


Inhibitory concentration


c-Jun N-terminal kinase

K. pneumonia

Klebsiella pneumoniae

L. donovani

Leishmania donovani


Low density lipoprotein


Lysophosphatidic acid


muscarinic acetylcholine receptor


Monoamine oxidase


Mitogen-activated protein


Mouse brain endothelial cells


Maximal electric shock


Minimum inhibitory concentration


Mycobacterium tuberculosis


3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide


nicotinic acetylcholine receptor

P. aeruginosa

Pseudomonas aeruginosa

P. chrysogenum

Penicillium chrysogenum


Peroxisome proliferator-activated receptors


Protein tyrosine phosphate

R. cerealis

Rhizoctonia cerealis

R. oryzae

Rhizopus oryzae

S. aureus

Staphylococcus aureus

S. pyogenes

Streptococcus pyogenes

S. typhi

Salmonella typhi

S. typhimurium

Salmonella typhimurium




Structure-activity relationship


subcutaneous pentylenetetrazole


Silent information regulators


Secretory phospholipase A


Signal transducer and activator of transcription

T. mentagrophytes

Trichophyton mentagrophytes

T. rubrum

Trichophyton rubrum


Transient receptor potential melastatin


Transient receptor potential vanilloid



The authors thank the authorities of GLA University, Mathura, India for their praise worthy inspiration and constant encouragement.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.


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Authors and Affiliations

  1. 1.Institute of Pharmaceutical ResearchGLA UniversityMathuraIndia

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