Novel drug designing approach for dual inhibitors as anti-inflammatory agents: implication of pyridine template

Pillai, Ajay D.; Rathod, Parendu D.; P.X, Franklin; Patel, Manoj; Nivsarkar, Manish; Vasu, Kamala K.; Padh, Harish; Sudarsanam, V.

doi:10.1016/s0006-291x(02)02996-0

Cited by 95 publications

(56 citation statements)

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As shown in Scheme 1, enamine (2) was obtained by reacting ammonia with methyl acetoacetate (1). l-(a-Carbomethoxy-b-aminothiocrotonoyl)-arylamines (3) were synthesized by nucleophilic addition of arylisothiocyanate and enamine (2) as per reported procedure [13]. Arylisothiocyanates were synthesized using modified Kaluza method [21].…”

Section: Chemistrymentioning

confidence: 99%

“…Arylisothiocyanates were synthesized using modified Kaluza method [21]. 4a -4f were synthesized by adding 0.001 mol of the respective substituted phenacyl bromide to a solution of (3) (0.001 mol) in 2 mL of acetonitrile without adding base at room temperature [13]. The solution was stirred until the solid was separated from the reaction mixture or until no more of the starting materials could be detected on TLC.…”

Section: Chemistrymentioning

confidence: 99%

“…Aminobenzophenone derivatives have also been reported as a novel class of p38 MAP kinase inhibitors with high anti-inflammatory activity [12]. Bioisosteric replacement of the benzene ring in the aminobenzophenone lead compound by thiophenes has been reported [13]. Various thiophene derivatives are well documented as potent anti-inflammatory agents in the literature [14 -16].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Design, synthesis and pharmacological evaluation of novel tetrasubstituted thiophene analogues as anti-inflammatory agents

Molvi

Sudarsanam

Patel

et al. 2008

Journal of Enzyme Inhibition and Medicinal Chemistry

Self Cite

View full text Add to dashboard Cite

A new series of tetrasubstituted thiophene analogues (4a-4f, 5a-5f and 8a-8i) were designed incorporating the pharmacophoric features of COX-1 (as in fenamates), 5-LOX and the p38 MAP kinase inhibitors. The designed series was synthesized by nucleophilic addition of aryl/aroylisothiocyanate and enamine (2) yielding the addition product l-(a-Carbomethoxy-b-aminothiocrotonoyl)-aryl/aroyl amines (3/7); which on reaction with substituted phenacyl bromides gave the targeted tetrasubstituted thiophene esters (4a-4f / 8a-8i). The tetrasubstituted thiophenes esters (4a-4f ) on hydrolysis with one equivalent of potassium hydroxide solution in methanol at room temperature gave corresponding acids (5a-5f ). All the targeted compounds were evaluated for their anti-inflammatory activity in carrageenin-induced rat hind paw oedema model at the doses of 10, 20 and 40 mg/kg body weight using standard drugs mefanamic acid and ibuprofen. The compounds (4c, 4e, 4f, 5f, 8a-8i) which gave reasonable protection to the inflamed paw, eliciting good or moderate comparable anti-inflammatory activity were selected for investigating their analgesic activity using acetic acid induced writhing response test in albino mice at 10 mg/kg dose using standard drug ibuprofen and in order to arrive at possible mechanism of their anti-inflammatory activity, in vitro antioxidant nitric oxide radical scavenging assay at the concentrations of 5, 10, 15, 20, 25, 30 and 35 mg/mL were performed using standard drug ascorbic acid.

show abstract

Section: Chemistrymentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Design, synthesis and pharmacological evaluation of novel tetrasubstituted thiophene analogues as anti-inflammatory agents

Molvi

Sudarsanam

Patel

et al. 2008

Journal of Enzyme Inhibition and Medicinal Chemistry

Self Cite

View full text Add to dashboard Cite

show abstract

“…The highly substituted pyridine derivatives, like2-amino-4-aryl-3,5-dicyano-6-sulfanylpyridines have significant and diverse medicinal utility. Essentially, these compounds serve as high-potency agonists for the human adenosine receptors and act as potential therapeutic agents for the treatment of Creutzfeldt-Jacob disease, Parkinson's disease, hypoxia, asthma, cancer, kidney disease and prion disease [3][4][5]. Due to their п-stacking ability, some pyridines are used in supramolecular chemistry [6][7][8].…”

Section: Introductionmentioning

confidence: 99%

Montmorillonite K10 Clay Catalyzed One Pot Synthesis of 2,4,6-Tri Substituted Pyridine under Solvent Free Condition

Kannan¹,

Sreekumar²

2013

MRC

View full text Add to dashboard Cite

Montmorillonite K10 catalyzed synthesis of 2,4,6 triaryl pyridine under solvent free condition is described. Montmorillonite effectively catalyzed the reaction in good to excellent yields. Using this solid catalyst, the reactions could be carried out in a short period of time with very good yield of triaryl pyridines, up to 97% under solvent free condition. This catalyst could be recycled very easily, which makes this methodology environmentally benign. The catalyst is active over three cycles.

show abstract

“…Pyridine ring systems, especially 2,4,6-triarylpyridines, are of immense interest because of their unique position in medicinal chemistry [2][3][4][5][6]. Therefore, recent studies have highlighted the biological activity of triarylpyridines, providing impetus for further studies in utilizing this structure in new therapeutic drug classes [7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

A facile one-pot, three-component synthesis of 3,3′-(4-arylpyridine-2,6-diyl)bis(2H-chromen-2-one) derivatives under microwave irradiation

et al. 2012

View full text Add to dashboard Cite

A series of 3,3 0 -(4-arylpyridine-2,6-diyl)bis(2H-chromen-2-one) derivatives have been synthesized by the one-pot, three-component reaction of 3-acetylcoumarin, an aromatic aldehyde, and ammonium acetate in acetic acid under microwave irradiation. This procedure has the major advantages of short reaction time, good yields, low energy consumption, easy operation, and environmental friendliness. All of the products were characterized by IR and NMR spectroscopy, MS, and elemental analysis.

show abstract

Novel drug designing approach for dual inhibitors as anti-inflammatory agents: implication of pyridine template

Cited by 95 publications

References 14 publications

Design, synthesis and pharmacological evaluation of novel tetrasubstituted thiophene analogues as anti-inflammatory agents

Design, synthesis and pharmacological evaluation of novel tetrasubstituted thiophene analogues as anti-inflammatory agents

Montmorillonite K10 Clay Catalyzed One Pot Synthesis of 2,4,6-Tri Substituted Pyridine under Solvent Free Condition

A facile one-pot, three-component synthesis of 3,3′-(4-arylpyridine-2,6-diyl)bis(2H-chromen-2-one) derivatives under microwave irradiation

Contact Info

Product

Resources

About