Synthesis of 2‐Oxo‐2H‐chromene‐3‐carboxylic Acid (5‐Methyl‐3‐isoxazolyl) and (3‐Methyl‐5‐styryl‐4‐isoxazolyl) Amides as Potential Bioactive Compounds.

Rajanarendar, E.; Ramu, K.; Ramesh, P.

doi:10.1002/chin.200450100

Cited by 3 publications

(3 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The synthesized compounds are characterized by elemental analysis and spectral studies and evaluated for its antimicrobial activity. Rajanarendar et al [36] reported the synthesis of 2-oxo-2H-chromene-3-carboxylic acid(5-methyl-3-isoxazolyl) and (3-methyl-5-styryl-4-isoxazolyl)amides 41 ( fig. 5) from amino isoxazoles, by treatment with diethyl malonoate followed by cyclization with salicylaldehydes.…”

Section: Fig 3: Structures Of Antimicrobial Isoxazoles 15-23mentioning

confidence: 99%

Isoxazole – A Potent Pharmacophore

Chikkula¹,

Raja

2017

Int J Pharm Pharm Sci

View full text Add to dashboard Cite

Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib. Furoxan, a nitric oxide donor is containing isoxazolyl group and found in many β-lactamase resistant antibiotics, such as cloxacillin, dicloxacillin and flucloxacillin. The synthetic androgenic steroid danazol also has an isoxazole ring. The substituted isoxazoles are well developed in literature to possess significant biological activities. The disubstituted and trisubstituted isoxazoles have been reported to exhibit broad range of biological activities such as antimicrobial activity, analgesic activity, anti-inflammatory activity, antioxidant activity, anticancer activity, CNS (central nervous system) activity, antitubercular activity and miscellaneous activities like GABA (γ-amino butyric acid) agonistic activity, inhibitory activity, antihypertensive activity, and glutamate transporter activity. The present review summarizes up to date information of various biological activities of isoxazole analogs.

show abstract

Section: Fig 3: Structures Of Antimicrobial Isoxazoles 15-23mentioning

confidence: 99%

Isoxazole – A Potent Pharmacophore

Chikkula¹,

Raja

2017

Int J Pharm Pharm Sci

View full text Add to dashboard Cite

show abstract

“…New 3-acylamido coumarins derived from 3-amino-5-substituted isoxazoles (51) have been designed and synthesized for possible anti-microbial agents [130]. Promisingly, Radulovic et al screened a new 3,4-annelated coumarin derivative (52), which showed a greater antibiotic activity than both Ampicillin and Nystatin, and four times as much anti-oxidant activity as -tocopherol acetate [130].…”

Section: Structure Activity Relationships (Sars) Referencementioning

confidence: 99%

“…The dichloroacetamido moiety has also been inserted in to the allylic position of the pyran ring of coumarin, and the resulting compound (50) have moderate activity against B. cirroflagellosus, E. coli, A. niger, and C. albicans [129]. New 3-acylamido coumarins derived from 3-amino-5-substituted isoxazoles (51) have been designed and synthesized for possible anti-microbial agents [130]. Promisingly, Radulovic et al screened a new 3,4-annelated coumarin derivative (52), which showed a greater antibiotic activity than both Ampicillin and Nystatin, and four times as much anti-oxidant activity as -tocopherol acetate [130].…”

Section: Structure Activity Relationships (Sars) Referencementioning

confidence: 99%

The Structure and Pharmacological Functions of Coumarins and Their Derivatives

Wang²,

Xu³

et al. 2009

CMC

255

132

View full text Add to dashboard Cite

Coumarins are of many different structures. They constitute an important class of pharmacological agents possessing a range of different physiological activities including anti-cancer, anti-oxidant, anti- inflammation, anti-HIV, anti-coagulant, anti-bacterial, analgesic and comparative immune-modulation. Recently, coumarins have attracted intense research interest. Of great interest is the possibility that this class of molecules could be a source of drugs for the therapy of several diseases. These include recent insights into inhibiting cell proliferation by interfering with mitotic spindle microtubule function, decrease Matrix Metalloproteinase (MMP) activity, block the cell cycle in the S or G2/M phases to interfere with processes of cell division, suppress O2(-) generation in leukocytes, inhibit different protein kinases, modulate the signalings, induce carcinogen-detoxifying enzymes glutathione S-transferases (GSTs) and/or NAD(P)H quinine oxidoreductase (NQO1), suppress the phosphorylation of Akt/PKB as a mechanism inhibiting inflammation, progress in structure modification to increase in anti-fungal action, to broaden against bacteria spectrum, to enhance inhibiting activities of nitric oxide synthase (NOS) and cyclooxygenase (COX), to strengthen anti-oxidant activity and to exhibite a much higher cytotoxicity against human umbilical vein endothelial cell (HUVEC). With fewer non-hemorrhagic side effects than the indanedione derivatives, they can be applied as an oral anticoagulant commonly for preventing venous thromboembolism following orthopedic surgery, recurrent myocardial infarction and the treatment of systemic embolism in atrial fibrillation, together with the significant advances in the basis of drug action. It is therefore useful to build up some correlations with the data available in order to better explore the molecular and cellular mechanism of coumarin action in the treatment of diseases. This review will focus on recent advances in molecular and cellular mechanisms of coumarin action involved with the relationship between structure and activity.

show abstract