Design, synthesis and anti-inflammatory vel 5-(Indol-3-yl)thiazolidinone derivatives as COX-2 inhibitors.

Atta-Allah, Saad R.; Nassar, Ibrahim F.; El‐Sayed, Wael A.

doi:10.35841/pharmacology-therapeutic.5.2.1-3-16

Cited by 6 publications

(5 citation statements)

References 25 publications

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“…N-Substituted 5-(oxoindolinyl)-2-thioxothiazolidinone derivatives (Scheme 30) were designed and developed by Attah-Allah et al [70] All the derivatives were tested for their COX-2 inhibitory activity. Five compounds (35a, 35b, 35c, 35d, and 35e) (Figure 15)…”

Section: Cyclooxygenase Inhibitionmentioning

confidence: 99%

“…N ‐Substituted 5‐(oxoindolinyl)‐2‐thioxothiazolidinone derivatives (Scheme 30) were designed and developed by Attah‐Allah et al [ 70 ] All the derivatives were tested for their COX‐2 inhibitory activity. Five compounds ( 35a , 35b , 35c , 35d , and 35e ) (Figure 15) were capable of significantly inhibiting the conversion of arachidonic acid to prostaglandin H 2 (PGH 2 ) with IC 50 values of 5.91, 5.85, 5.4, 5.63, and 5.87, respectively.…”

Section: Development Of Antiarthritic Agents So Farmentioning

confidence: 99%

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Therapeutic management of arthritis: A review on structural and target‐based approaches

Mahore

Kamboj

Kaleem

et al. 2022

Archiv der Pharmazie

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Inflammation is the natural defense mechanism against any external stimuli in the human body and it saves us from foreign entities that may alter our bodies' normal functioning. Any anomaly in this natural defense system leads to the development of different pathological conditions associated with chronic inflammation like rheumatoid arthritis, osteoarthritis, atopy, asthma, allergic rhino-conjunctivitis, coronary artery disease, cardiac arrhythmias, obesity, insulin resistance and type-2 diabetes, depression, and aging. These disorders impair the quality of life of affected people in different ways. Among these, rheumatoid arthritis and osteoarthritis are the most common chronic inflammation-associated disorders. Different therapeutic strategies are already available for the treatment of rheumatoid arthritis and osteoarthritis, but all with pros and cons. Here, we discuss the emergence of several antiarthritic analogs developed by different researchers which could provide the basis for the evolution of newer therapeutic strategies with better activity and safety profiles.

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Section: Cyclooxygenase Inhibitionmentioning

confidence: 99%

Section: Development Of Antiarthritic Agents So Farmentioning

confidence: 99%

Therapeutic management of arthritis: A review on structural and target‐based approaches

Mahore

Kamboj

Kaleem

et al. 2022

Archiv der Pharmazie

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“…Another heterocyclic ring possessing numerous types of biological activities is thiazolidinone. Among them are anti-inflammatory [ 25 , 26 , 27 ], antimicrobial [ 28 , 29 ], anticancer [ 30 , 31 ], antidiabetic [ 32 ], anti-HIV [ 33 ].…”

Section: Introductionmentioning

confidence: 99%

New Substituted 5-Benzylideno-2-Adamantylthiazol[3,2-b][1,2,4]Triazol-6(5H)ones as Possible Anti-Inflammatory Agents

et al. 2021

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Background: Inflammation is a complex response to noxious stimuli promoted by the release of chemical mediators from the damaged cells. Metabolic products of arachidonic acid, produced by the action of cyclooxygenase and lipoxygenase, play important roles in this process. Several non-steroidal anti-inflammatory drugs act as cyclooxygenase inhibitors. However, almost all of them have undesired side effects. Methods: Prediction of the anti-inflammatory action of the compounds was performed using PASS Program. The anti-inflammatory activity was evaluated by the carrageenan paw edema test. COX and LOX inhibitory actions were tested using ovine COX-1, human recombinant COX-2 and soybean LOX-1, respectively. Docking analysis was performed using Autodock. Results: All designed derivatives had good prediction results according to PASS and were synthesized and experimentally evaluated. The compounds exhibited in vivo anti-inflammatory action with eleven being equal or better than indomethacin. Although, some of them had no or low inhibitory effect on COX-1/2 or LOX, certain compounds exhibited COX-1 inhibition much higher than naproxen and COX-2 inhibition, well explained by Docking analysis. Conclusions: A number of compounds with good anti-inflammatory action were obtained. Although, some exhibited remarkable COX inhibitory action this activity did not follow the anti-inflammatory results, indicating the implication of other mechanisms.

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“…Indole, an aromatic heterocyclic organic compound, has attracted the interest of scientists since it possesses a wide variety of pharmacological properties, such as analgesic [3,4], anti-inflammatory [3,5,6], antimicrobial [7][8][9][10], anticancer [11][12][13], anticonvulsant [14,15] and antiviral [16,17], COX-inhibitory [18,19], antidiabetic [20,21], and antitubercular [22,23] activities. Furthermore, indole moiety is present in some drug molecules, such as: indomethacin; yohimbine, an approved drug for the treatment of sexual disorders [24,25]; delavirdine, anti-HIV drug [26]; reserpine (Figure 1), and many others.…”

Section: Introductionmentioning

confidence: 99%

4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation

Simakov

Карцев²,

Petrou

et al. 2021

Pharmaceuticals

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This manuscript deals with the synthesis and computational and experimental evaluation of the antimicrobial activity of twenty-nine 4-(indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole acylamines. An evaluation of antibacterial activity against Gram (+) and Gram (−) bacteria revealed that the MIC of indole derivatives is in the range of 0.06–1.88 mg/mL, while among fourteen methylindole derivatives, only six were active, with an MIC in the range of of 0.47–1.88 mg/mL. S. aureus appeared to be the most resistant strain, while S. Typhimurium was the most sensitive. Compound 5x was the most promising, with an MIC in the range of 0.06–0.12 mg/mL, followed by 5d and 5m. An evaluation of these three compounds against resistant strains, namely MRSA P. aeruginosa and E. coli, revealed that they were more potent against MRSA than ampicillin. Furthermore, compounds 5m and 5x were superior inhibitors of biofilm formation, compared to ampicillin and streptomycin, in terms Compounds 5d, 5m, and 5x interact with streptomycin in additive manner. The antifungal activity of some compounds exceeded or was equipotent to those of the reference antifungal agents bifonazole and ketoconazole. The most potent antifungal agent was found to be compound 5g. Drug likeness scores of compounds was in a range of −0.63 to 0.29, which is moderate to good. According to docking studies, E. coli MurB inhibition is probably responsible for the antibacterial activity of compounds, whereas CYP51 inhibition was implicated in antifungal activity. Compounds appeared to be non-toxic, according to the cytotoxicity assessment in MRC-5 cells.

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Design, synthesis and anti-inflammatory vel 5-(Indol-3-yl)thiazolidinone derivatives as COX-2 inhibitors.

Cited by 6 publications

References 25 publications

Therapeutic management of arthritis: A review on structural and target‐based approaches

Therapeutic management of arthritis: A review on structural and target‐based approaches

New Substituted 5-Benzylideno-2-Adamantylthiazol[3,2-b][1,2,4]Triazol-6(5H)ones as Possible Anti-Inflammatory Agents

4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation

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