Dextran-etodolac conjugates: synthesis, in vitro and in vivo evaluation.

Etodolac (E), is a non-narcotic analgesic and antiinflammatory drug. A biodegradable polymer dextran has been utilized as a carrier for synthesis of etodolac-dextran conjugates (ED) to improve its aqueous solubility and reduce gastrointestinal side effects. An activated moiety, i.

2-Amino-5-sulfanyl-1,3,4-thiadiazoles: a new series of selective cyclooxygenase-2 inhibitors.

A new series of cyclooxygenase-2 inhibitors with 2-amino-5-sulfanyl-1,3,4-thiadiazole as the central scaffold unit has been synthesized. The newly synthesized compounds were characterized by analytical and spectral methods. Compounds were screened for cyclooxygenase inhibitory activity by the colorimetric COX (ovine) inhibitor screening assay, anti-inflammatory activity by the carrageenean induced rat paw oedema test and analgesic activity by the tail flick method.

Ketorolac-dextran conjugates: synthesis, in vitro and in vivo evaluation.

Ketorolac is a non-steroidal anti-inflammatory drug. Dextran conjugates of ketorolac (KD) were synthesized and characterized to improve ketorolac aqueous solubility and reduce gastrointestinal side effects. An N-acylimidazole derivative of ketorolac (KAI) was condensed with a model carrier polymer, dextran of different molecular masses (40000, 60000, 110000 and 200000).

Structure-activity relationship study of some triazolinone based compounds with antagonistic balanced activity on angiotensin II receptor subtypes AT1 and AT2. A three-dimensional quantitative structure-activity relationship investigation.

Angiotensin II (AII) receptor antagonists have attracted much attention as anti-hypertensive agents in recent times following the discovery of side effects associated with angiotensin converting enzyme (ACE) inhibitors. Various lead structures of the compounds of this category are reported in the literature. Studying the structure-activity relationships (SAR) for such compounds has been a fascination for scientists and efforts have been made to identify the essential physico-chemical requirements for the angiotensin type 1 (AT1) receptor selective, angiotensin type 2 (AT2) receptor selective and some AT,/ AT2 balanced antagonistic activity compounds.