Biomedical subjects
Publications and source records attributed to Andrew Watson.
A series of fused pyrimidine based inhibitors of PDE7 have been derived from an earlier screening lead 1. The synthesis, structure-activity relationships (SAR) and selectivity against several other PDE family members are described.
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A series of purine based inhibitors of PDE7 has been derived from screening lead 1a. The synthesis, structure-activity relationships (SAR), and selectivity against several other PDE family members are described.
In a continuing effort to discover novel chemotypes as potent and selective PDE5 inhibitors for the treatment of male erectile dysfunction (ED), we have found that 4-benzylaminoquinoline derivatives are very potent and selective PDE5 inhibitors. Some compounds in this series had PDE5 IC(50)'s as low as 50 pM. While an electron withdrawing group at the C6-position of the quinoline substantially improved PDE5 potency, an ethyl group at the C8-position not only improved the PDE5 potency but also the isozyme selectivity. Substitutents at the C3-position can incorporate a variety of different groups. The synthesis and primary structure-activity relationship of this new series of potent PDE5 inhibitors are described.
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Explore the source record for details and available documents.
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The aim of this study was to evaluate systematically the role of pharmacological agents used as adjuvants during infertility surgery to prevent or reduce postoperative adhesion formation and improve pregnancy rates. Meta-analyses were performed of the ten randomized controlled trials identified that evaluated the use of pharmacological adjuvants at infertility surgery. The administration of steroids, dextran 70, noxytioline, heparin, or promethazine have all been investigated for their adjuvant role in preventing adhesion formation during pelvic surgery for infertility. Outcome measures were taken as: pregnancy rates after infertility surgery; number of patients with absent, improved or deteriorated adhesions at second look laparoscopy (dichotomous outcomes); and changes in adhesion score from initial surgery to second look laparoscopy (ordinal outcome). None of the pharmacological adjuncts investigated in a randomized controlled fashion was shown to improve postoperative pregnancy rates. There was some evidence that steroids reduced the incidence or severity of postoperative adhesion formation; there was little evidence to support the use of dextran. The routine use of pharmacological adjuncts during infertility surgery cannot be recommended on the basis of the available evidence derived from randomized controlled trials. Dextran appears to offer no advantage. The evidence with regard to steroids is far from conclusive but tentatively indicates that they may be beneficial.