Rational design of novel diaryl ether-linked benzimidazole derivatives as potent and selective BACE1 inhibitors.

Due to the large size and high flexibility of the catalytic active site of BACE1 enzyme, the development of nonpeptide inhibitors with optimal pharmacological properties is still highly demanding. In this work, we have discovered 2-aminobenzimidazole-containg ether scaffolds having potent and selective inhibitory potentials against BACE1 enzyme. We have synthesized novel 29 compounds and optimization of aryl linker region resulted in highly potent BACE1 inhibitory activities with EC values of 0.

Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.

Synthesis, SAR study and BACE1 inhibitory activity of (3S,4S)-4-aminopyrrolidine-3-ol derivatives (2) were described. The compound 7c exhibited more inhibition activity than 11a (IC50: 0.05μM vs 0.

Hepatoprotective activity of Phyllanthus reticulatus.

Two partially purified organic fractions designated by PR1 and PR2 of the fat free ethanol (95%) extract of aerial parts of Phyllanthus reticulatus were tested for the hepatoprotective activity in rats against CCl(4)-induced liver damage. The rats receiving the fractions showed promising hepatoprotective activity as evident from significant changes of pentobarbital-induced sleeping time, changes in serum levels of sGPT, sGOT, sALP and bilirubin and also from histopathological changes as compared to CCl(4)-intoxicated rats.

Anti-inflammatory activity of indanyltetrazole derivatives.

A number of indanyl tetrazolederivatives namely 5-(6'-chloroindan-1'-yl)tetrazole (CIT), 5-(6'-bromoindan-1'-yl)tetrazole (BIT), 5-(6'-chloroindan-1'-yl)methyltetrazole (CIMT), 5-(6'-bromoindan-1'-yl)methyl-tetrazole (BIMT) were evaluated for the anti-inflammatory activity in carragennan induced rat paw edema in Swiss albino Wister rats for 24-hour period at the dose of 100 mg/kg of body weight by intraperitoneal route where phenylbutazone (PBZ) was used as the standard. All of these compounds exhibited inhibition on rat paw edema with peak actions observed following 3 hours after administration. Moreover, compounds CIMT and BIMT were further evaluated at dose of 50 mg/kg of body weight.

Report: in vitro dissolution studies of different brands of sustained release diclofenac sodium matrix tablet available in Bangladesh.

Commercially available national thirteen brands and three international brands of diclofenac sodium sustained release matrix tablets were studied in simulated gastric medium (pH 1.2) for 2 hours time period and simulated intestinal medium (pH 6.8) for 10 hours time period using USP reference dissolution apparatus.