Synthesis and evaluation of water soluble indole pyrrolothiazole paf antagonists

✍ Scribed by George S. Sheppard; Steven K. Davidsen; George M. Carrera Jr.; Daisy Pireh; James H. Holms; H. Robin Heyman; Douglas H. Steinman; Michael L. Curtin; Richard G. Conway; David A. Rhein; Daniel H. Albert; Paul Tapang; Terrance J. Magoc; James B. Summers

• Book ID: 103983185
• Publisher: Elsevier Science
• Year: 1995
• Tongue: English
• Weight: 320 KB
• Volume: 5
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/0960-894x(95)00511-q

✦ Synopsis

3-(3-Pyridinyl)-7-(indol-3-ylcarbonyl)-lH-3H-pyrrolo[1,2-c]thiazoles represent a class of potent, orally active PAF antagonists; however, the lead compounds in this series suffered from a lack of aqueous solubility. To overcome this limitation, a number of strategies were examined to achieve improved solubility, involving the incorporation of polar substituents and the use of prodrugs.

Platelet Activating Factor (PAF) is an endogenous phospholipid inflammatory mediator which is hypothesized to be involved in a number of pathologic states having an inflammatory component, l Clinical evaluations of PAF antagonists for the treatment of asthma, allergic rhinitis, septic shock,