Stereochemistry–activity relationship of orally active tetralin S1P agonist prodrugs

نویسندگان
چکیده

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Oxime derivatives of PD217015 and PD148903. Orally active anti-Parkinson cascade prodrugs

A series of oxime ether and oxime ester derivatives of the potential anti-Parkinson prodrug PD148903 (2.3) were synthesized and evaluated in pharmacological models. Oximes 4.3 (hydroxyl-oxime) and 4.4 (methoxyl-oxime) were inactive in vitro but in the Ungerstedt rat model for Parkinson’s disease 4.3 and 4.4 produced a pronounced and long lasting effect at 1.0 mg kg po. Enantiomerically pure (–)...

متن کامل

Prodrugs of bisthiazolium salts are orally potent antimalarials.

We created neutral antimalarial prodrugs that deliver bisthiazolium compounds with antimalarial activity in the nanomolar range. These drugs primarily affect early intraerythrocytic stages through rapid, nonreversible cytotoxicity. The compounds are suitable for both parenteral and oral use and plasma promotes rapid conversion of the prodrug into the drug. We demonstrate that very low doses off...

متن کامل

Identification of an orally active small-molecule PTHR1 agonist for the treatment of hypoparathyroidism

Parathyroid hormone (PTH) is essential for calcium homeostasis and its action is mediated by the PTH type 1 receptor (PTHR1), a class B G-protein-coupled receptor. Hypoparathyroidism and osteoporosis can be treated with PTH injections; however, no orally effective PTH analogue is available. Here we show that PCO371 is a novel, orally active small molecule that acts as a full agonist of PTHR1. P...

متن کامل

Antinociceptive activity of the S1P-receptor agonist FTY720

FTY720 is a novel immunosuppressive drug that inhibits the egress of lymphocytes from secondary lymphoid tissues and thymus. In its phosphorylated form FTY720 is a potent S1P receptor agonist. Recently it was also shown that FTY720 can reduce prostaglandin synthesis through the direct inhibition of the cytosolic phospholipase A2 (cPLA2). Since prostaglandins are important mediators of nocicepti...

متن کامل

Development of a Peptide-Derived Orally-Active Kappa-Opioid Receptor Agonist Targeting Peripheral Pain

Kappa-opioid agonists are particularly efficacious in the treatment of peripheral pain but suffer from central nervous system (CNS)-mediated effects that limit their development. One promising kappa-agonist is the peptidic compound CR665. Although not orally available, CR665 given i.v. exhibits high peripheral to CNS selectivity and benefits patients with visceral and neuropathic pain. In this ...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters

سال: 2010

ISSN: 0960-894X

DOI: 10.1016/j.bmcl.2010.02.006