Nonsteroidal Anti-Inflammatory Drugs (NSAIDs):  A Comparative QSAR Study

Michaelidou, Alexandra-Maria; Hadjipavlou‐Litina, Dimitra

doi:10.1021/cr040708m

Cited by 42 publications

(23 citation statements)

References 73 publications

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“…Organic residues like thiazole, morpholine and substituted phenyl ring has been established to impart drug-like character to the molecule for the modulations of inflammation [12,13]. Required topological characteristics for anti-inflammatory activity can be acquired if desirable pharmacophoric features are incorporated within the molecule.…”

Section: Introductionmentioning

confidence: 99%

Aminocarbonyl Arylvinylbenzamides as Gastric Sparing Anti‐inflammatory Agents

Khadse

Talele

Agrawal

2011

Archiv der Pharmazie

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Some (E/Z)-aminocarbonyl arylvinylbenzamides (B1-B15) were synthesized, evaluated for anti-inflammatory activity and ulcerogenic tendency, and their effect on gastro-intestinal motility in the rats was studied. These benzamides comprising of aliphatic unsaturated region situated between two amide linkages were synthesized by nucleophilic ring opening of appropriate azlactones (AZ1-AZ4) by suitable amines. The characterization of newly synthesized benzamides was performed by IR, (1)H- and (13)C-NMR, mass and elemental analysis. Amongst the tested compounds, benzamide B1, B2, B4, B5, and B13 were able to produce comparable or superior anti-inflammatory activity at 10 and 20 mg/kg p.o. dose with respect to standard diclofenac in carrageenan induced rat paw edema model with lessened propensity to cause gastro-intestinal hypermotility and were found to have nil tendencies to generate gastric ulcers.

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Section: Introductionmentioning

confidence: 99%

Aminocarbonyl Arylvinylbenzamides as Gastric Sparing Anti‐inflammatory Agents

Khadse

Talele

Agrawal

2011

Archiv der Pharmazie

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“…Compounds possessing all three activities are not common. Among the many reported classes of anti-inflammatory agents, aryl and heteroaryl (alkyl) carboxylic acids possessed wide clinical applications but with the incidence of gastrointestinal damage and ulceration [1,2]. b-Hydroxy carboxylic acid derivatives as salicylic acid and its derivatives are wellknown drugs for their anti-inflammatory activity [1].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of β‐Hydroxypropanoic Acid Derivatives as Potential Anti‐inflammatory, Analgesic and Antimicrobial Agents

Abdel‐Rahman¹,

Hussein

2006

Archiv der Pharmazie

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A series of new 3-(substituted) 3-hydroxy-propanoic acid ethyl esters 1a-c, hydrazides 2a-c, thiosemicarbazides 3a-f, and semicarbazides 3g, 3h has been synthesized. Cyclization of compounds 3a-d in basic medium yielded 1,2,4-triazole-5-thiones 4a-d. On the other hand, reaction of hydrazides 2a-c with CS(2 )in basic medium afforded 1,3,4-oxadiazole-5-thiones 5a-c. All the synthesized compounds were characterized by their physical and spectral analyses data. The newly synthesized compounds were evaluated for their anti-inflammatory, analgesic, and antimicrobial activities. Compounds 1c, 3g, 4a, 4b, 4c, and 5c exhibited comparable anti-inflammatory activity to that of indomethacin and compounds 1c, 4c, and 5c were more analgesics than acetyl salicylic acid. Compounds 4b, 4c, and 5c showed superior GI safety profile (33.3%, 33.3% and 50.0% ulceration) than that of indomethacin (100% ulceration) at 100 mg/kg oral dose. Compounds 4b, 4c, and 5c were also non-toxic with a median lethal dose (LD(50)) up to 200 mg/kg. The antibacterial and antifungal screenings identified compounds 3c, 4b, 4d, 5a, and 5b as the most effective against a variety of tested microorganisms.

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“…Various benzothiazole derivatives serve as drugs, dyes and industrial chemicals [1][2][3]. Benzothiazoleand its derivatives such as esters have also been reported as active against Gram-positive and Gram-negative bacteria Benzothiazole derivatives have also found to possess anticancer, antifungal and antibacterial activities [5,6].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

et al. 2016

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Abstract:A new series of N-(6-arylbenzo [d]thiazol-2-yl)acetamides were synthesized by C-C coupling methodology in the presence of Pd(0) using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolyl)benzo[d]thiazol-2-yl)acetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.

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Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): A Comparative QSAR Study

Cited by 42 publications

References 73 publications

Aminocarbonyl Arylvinylbenzamides as Gastric Sparing Anti‐inflammatory Agents

Aminocarbonyl Arylvinylbenzamides as Gastric Sparing Anti‐inflammatory Agents

Synthesis of β‐Hydroxypropanoic Acid Derivatives as Potential Anti‐inflammatory, Analgesic and Antimicrobial Agents

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

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