Charles V. Grudzinskas

Prostaglandins and congeners XIII (1). The synthesis of dℓ-erythro-16-methoxyprostaglandins

dl-Erythro-16-methoxy-PGE2, PGA2, PGF2alpha, 11-deoxy PGE1, and 11-deoxy PGF1alpha have been prepared via the cuprate conjugate addition procedure. These congeners are less potent than the parent prostaglandins as stimulators of isolated gerbil colon contractions and as bronchodilators in the guinea pig Konzett assay.

Prostaglandins and congeners XXIII (1). Synthesis of 15-deoxy-16-hydroxy-16-methylprostaglandins. The importance of the C13-C14 trans double bond for bronchodilator activity

The synthesis and bronchodilator activity in the guinea pig of several 15-deoxy-16-hydroxy-16-methylprostaglandin analogs is described. The E2 (VIa) and E1 (VIb) analogs are potent bronchodilators comparable in activity to the natrual prostaglandins, but possessing a longer duration of effect. Replacement of the C13--C14 trans double bond by a cis double bond or an ethylene linkage causes a substantial diminishment of this activity.

Change + Communication = Challenge [L] (Magagment of New Drug Development)

AbstractTo adapt to the challenges of rapidly changing global regulatory, technical and economic environments, pharmaceutical R&D organizations are combining classical project management principles and drug development teams.Several recent drug development successes in the Medical Research Division of American Cyanamid are the direct result of the clear definition of global project objectives, goals and strategies (project management) and a global team structure (development teams) to support the management of these projects.