Antiinflammatory activity of 5,6-diaryl-2,3-dihydroimidazo[2,1-b]thiazoles. Isomeric 4-pyridyl and 4-substituted-phenyl derivatives

Lantos, I.; Bender, Paul E.; Razgaitis, K. A.; Sutton, Bridget M.; DiMartino, Michael J.; Griswold, Don E.; Walz, D. T.

doi:10.1021/jm00367a014

Cited by 67 publications

(43 citation statements)

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“…Among the halogen-substituted compounds (2 -11), only compounds having the F or CF 3 group in the R position and the Cl or NH 2 group in the W position showed signifi-2-Amino-5-sulfanyl-1,3,4-thiadiazoles 23 (2,3,5,8,9,11). One possible reason could be that the fluorine atom is small in size, lipophilic in nature, has the ability to form strong H-bond, and has better metabolic stability under physiological condition.…”

Section: Resultsmentioning

confidence: 99%

2-Amino-5-sulfanyl-1,3,4-thiadiazoles: a novel series of anti-inflammatory and analgesic agents

et al. 2009

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2-Amino-5-sulfanyl-1,3,4-thiadiazole derivatives were synthesized via the interaction of 2-amino-5-sulfanyl-1,3,4-thiadiazole, Ar-Cl, and benzene sulfonamide/benzene sulfonyl chloride. Twelve compounds were synthesized, out of which six compounds show significant anti-inflammatory and analgesic activity and were devoid of gastrointestinal side effects (ulcerogenic effect), which zre the most frequent adverse reactions associated with orally ingested anti-inflammatory or antiarthritic agents.

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Section: Resultsmentioning

confidence: 99%

2-Amino-5-sulfanyl-1,3,4-thiadiazoles: a novel series of anti-inflammatory and analgesic agents

et al. 2009

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“…The early reports of a series of antiinflammatory bicyclic imidazoles [36], represented by the imidazothiazole SK&F 86002 (1) (Fig. 2), provided a starting point for these structures.…”

Section: Pyridinyl Imidazolesmentioning

confidence: 99%

Structure-Activity Relationships of p38 Mitogen-Activated Protein Kinase Inhibitors

Bolós

2005

MRMC

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Rheumatoid arthritis and other chronic inflammatory diseases constitute a major therapeutic challenge, usually not sufficiently met by the classical antiinflammatory medications. Recent research efforts provided new insights into the molecular basis of these pathologies and disclosed new opportunities for developing improved drugs directed to the chemical mediators of the disease. The enzyme p38 MAP kinase plays a central role in the signal transduction cascade that leads to the production of both the proinflammatory cytokines, TNF-alpha and IL-1 beta, thus representing an attractive therapeutic target for novel antiinflammatory therapies. A number of p38 inhibitors belonging to different structural families have been developed as potential antiinflammatory drugs, and some of them progressed into clinical trials. The initial pyridinyl imidazole inhibitors contributed to the identification and characterization of p38 MAP kinase as the molecular target of these new drugs, and were found to act as competitive inhibitors at the ATP binding site of the enzyme. A number of variations in the pyridine and imidazole rings were subsequently introduced. Other inhibitors structurally unrelated to the pyridinylimidazoles have also been developed, such as the pyridopyridazinones, diaryl ureas, aminobenzophenones and aromatic amides. One of these structural classes, the N,N'-diarylureas, has been found to interact with a distinct allosteric site of p38 MAP kinase and requires a deep conformational change prior to binding.

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“…A series of bicyclic imidazole derivatives, exemplified initially by SK&F 86002 (SmithKline Beecham), and later SB 203580 (SmithKline Beecham, 2) and SB 210313 (SmithKline Beecham) have been reported as potent inhibitors of p38 activity [49]. These agents have been termed cytokine-suppressive anti-inflammatory drugs (CSAIDs) due to their inhibition of IL-1 and TNF production by human monocytes [50,51]. These compounds also inhibit TNF production following LPS administration in vivo and significantly reduce oedema and increase bone density in animal models of arthritis.…”

Section: Novel Regulators Of Inflammatory Gene Transcriptionmentioning

confidence: 99%

Transcription inhibitors in inflammation

Manning

Mercurio²

1997

Expert Opinion on Investigational Drugs

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Advances in molecular medicine have revealed a key role for altered gene expression in the aetiology of many inflammatory diseases, including asthma, rheumatoid arthritis, inflammatory bowel disease and sepsis. Until recently, however, modulation of gene transcription has not been the subject of directed pharmaceutical research efforts. Notwithstanding, it is clear that the efficacy of several well-established anti-inflammatory therapeutics is mediated through their ability to modulate gene transcription. Understanding the mechanisms of action of these therapeutics and defining new gene regulatory pathways has stimulated a new wave of anti-inflammatory drug discovery. This update aims to cover our current understanding of transcription inhibitors in inflammation, including the mechanism of action of established therapeutics and the properties of new chemical entities recently described in the literature.

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Antiinflammatory activity of 5,6-diaryl-2,3-dihydroimidazo[2,1-b]thiazoles. Isomeric 4-pyridyl and 4-substituted-phenyl derivatives

Cited by 67 publications

References 0 publications

2-Amino-5-sulfanyl-1,3,4-thiadiazoles: a novel series of anti-inflammatory and analgesic agents

2-Amino-5-sulfanyl-1,3,4-thiadiazoles: a novel series of anti-inflammatory and analgesic agents

Structure-Activity Relationships of p38 Mitogen-Activated Protein Kinase Inhibitors

Transcription inhibitors in inflammation

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