5-aryl-2 3-dihydroimidazo [2,1-a] isoquinolines. A novel class of platelet-activating factor (PAF) receptor antagonists structurally derived from the PAF molecule

Houlihan, William J.; Cheon, Seung Hoon; Handley, Dean A.; Larson, David; Parrino, Vincent A.; Reitter, Barbara E.; Schmitt, G.; Winslow, Christine M.

doi:10.1016/0090-6980(88)90260-2

Cited by 5 publications

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“…In conclusion, it has been found that modification of the imidazo (ring A) or benzo (ring C) in the PAF receptor antagonist 1 by ring expansion (5), or introduction of a hetero ring system (6,7), results in compounds of similar or greater PAF antagonist activity. Introduction of a double bond (8a, 8b), two methyl groups (5b), or an additional nitrogen atom (12) in ring A, or a nitrogen atom (16) in ring B, resulted in loss of activity.…”

Section: Discussionmentioning

confidence: 99%

Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists

Houlihan¹,

Cheon²,

Parrino³

et al. 1993

J. Med. Chem.

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In an effort to determine the effect of modification of the imidazo[2,1-a]isoquinoline portion of the PAF-receptor antagonist SDZ 64-412 (1), several new analogs were prepared and evaluated in vitro and in vivo. One of these, 5-[4-[2-(3,4,5-trimethoxyphenyl)ethyl]phenyl]-2,3-dihydroimidazo [1,2-a]thieno[2,3-c]pyridine (6) was 4-5 times more potent than 1 in inhibiting PAF-induced bronchoconstriction and hemoconcentration when administered po to the guinea pig.

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Section: Discussionmentioning

confidence: 99%

Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists

Houlihan¹,

Cheon²,

Parrino³

et al. 1993

J. Med. Chem.

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“…Nevertheless, four other chemical classes of PAF antagonists developed by the Sandoz Research Institute were found to be cytotoxic in a number of different human tumour cell lines (DanhauserRiedl et al, 1991). One such group was a series of imidazoisoquinolines, which were originally designed as orally active, non-charged PAF antagonists based on PAF as a template (Houlihan et al, 1989). From (Valone & Ruis, 1992).…”

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confidence: 99%