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Heterocyclic inflammation inhibitors

100%

Sondhi S., Rajvanshi S., Singh N., Jain S., Lahoti A.

Open Chemistry

2004

vol. 2

issue 1

141-187

Non steroidal anti-inflammatory drugs are the most widely used medicines for relief of pain. These drugs have some side effects, particularly toxicity in the gastrointestinal tract and kidneys. Various approaches have been used for obtaining safer anti-inflammatory drugs. In this review we have summarized the recent developments in the following areas; (i) mode of action of NSAIDs (ii) Role of COX-1 & COX-2 in inflammation, (iii) Different approaches used to improve gastric tolerance i.e. chemical manipulation, formulation & co-administration, development of non specific (COX-1 & COX-2 inhibitors) and specific (COX-2 inhibitors) inflammation inhibitors, and development of inflammation inhibitors having a mode of action other than COX-1 & COX-2 inhibition. We have also focused on the safety of COX-2 inhibitors and the synthesis of heterocyclic compounds and their role as inflammation inhibitors.

Antiinflammatory, analgesic and kinase inhibition activities of some acridine derivatives

86%

Sondhi S., Bhattacharjee G., Jameel R., Shukla R., Raghubir R., Lozach O., Meijer L.

Open Chemistry

2004

vol. 2

issue 1

1-15

9-Chloro-2,4-(un)substituted acridines (1) on condensation with sulpha- diazine, sulphathiazole, and sulphaacetamide gave condensation products 3a-h. 3-Aryl-4-phenyl-2-imino-4-thiazolines (4) on condensation with 9-chloro-2,4-(un)substituted acridines (1) gave condensation products 5a–5o. Both 3a–3h and 5a–5o were purified by crystallization or by chromatography. Structures assigned to 3a–3h and 5a–5o are supported by correct spectral data. Antiinflammatory and analgesic activity screening of 3a, 3e, 3f and 5a–5c, 5e, 5g, 5i, 5m, 5n were carried out using carrageenin induced paw oedema and phenyl quinone writhing assay. Some of the compounds exhibited interesting antiinflammatory or analgesic activities.

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2 Open Chemistry

2 2004

2 Sondhi S.

1 Bhattacharjee G.

1 Jain S.

1 Jameel R.

1 Lahoti A.

1 Lozach O.

1 Meijer L.

1 Raghubir R.

1 Rajvanshi S.

1 Shukla R.

1 Singh N.

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Heterocyclic inflammation inhibitors

Antiinflammatory, analgesic and kinase inhibition activities of some acridine derivatives