Synthesis and biological activity of some new furan quaternary salts.

A series of new N-(5-substituted 2-furfuryl)-N,N-dimethyl-N-aryloxyalkyl quaternary ammonium salts relating to general structure IV has been synthesized by reacting 5-substituted 2-(N,N-dimethylaminomethyl)furans IIa-d with appropriate aryloxyalkyl bromides III. The resulting compounds are tested for in vitro antimicrobial activity. A simpler synthesis of 5-nitro-2-(N,N-dimethylaminomethyl)furan (IId) involving the reduction of N,N-dimethyl-5-nitro-2-furamide (Ib) with diborane is described. A new compound, 5-bromo-2-(N,N-dimethylaminomethyl)furnan (IIc), is prepared in a similar way. Many of these compounds (22, 28, 34, 37-42, 44, and 45) indicate high activity against Staphylococcus aureus, Streptococcus faecalis, Klebsiella pneumoniae, and Pseudomonas aeruginosa and are more active than nitrofurantoin, Compounds 22, 34 and 41 exhibit the highest in vitro antibacterial activity in the series. Some of these quaternary salts (22, 25, 37, 37-41, and 60) possess appreciable activity against Mycobacterium tuberculosis H37Rv. None of these compounds show significant antifungal activity. Eight compounds (18, 21, 22, 26-28, 32, and 34) have high in vitro antibacterial activity were inactive when tested for anthelmintic activity in rats against Nippostrongylus brasiliensis and Hymenolepis nana.

Antimicrobial agents: synthesis and antimicrobial activity of new aryloxyalkyl esters of p-hydroxybenzoic acid.

Several new aryloxyalkyl esters of p-hydroxybenzoic acid were synthesized and screened for in vitro antimicrobial activity. Although a few compounds showed low antifungal activity, many possessed appreciable in vitro antibacterial activity. However, none of these compounds was active against Mycobacterium tuberculosis (H37Rv).

Effect of bezafibrate & nicotinic acid on triton induced hyperlipidemias in CFY rats.

The two mechanisms of action of bezafibrate and nicotinic acid and their combination were evaluated in normal rats and triton treated rats. Bezafibrate was effective hypolipidemic agent in normal rats, but addition of nicotinic acid has certainly improved the effectiveness further which could be of clinical significance. In triton treated rats bezafibrate and nicotinic acid used individually and together had prophylactic hypolipidemic action. However, in their therapeutic effectiveness, bezafibrate reduced triglycerides (65.4%) and nicotinic acid, cholesterol (39.3%). But when treated together they showed marked acceleration in the removal of cholesterol as well as triglycerides. It is therefore concluded that a combination of bezafibrate and nicotinic acid may be beneficial in the treatment of hyperlipoproteinemias, both prophylactically and therapeutically.

Pre-clinical toxicity of IDPH-791: a new centrally acting muscle relaxant in rats.

IDPH-791, a novel centrally acting muscle relaxant, in doses up to 500 mg/kg (po) for 14 days did not result in any appreciable adverse effect on body weight gain, food or water consumption including biochemical and haematologica parameters in rats. Variations observed in the biochemistry and haematology were either comparable to controls or were within normal limits.

Metabolic behaviour of aflatoxin producing strain and non-toxigenic strain of Aspergillus flavus to different sources of nitrogen and glucose concentration.

The effect of different nitrogen sources and varying glucose concentration on aflatoxin production by a toxigenic and non-toxigenic strain of Aspergillus flavus was studied. Greatest production (3.8 ppm) of aflatoxin B1 was produced in a synthetic medium when casamino acids were supplied as the nitrogen source. Optimum sugar concentration for aflatoxin B1 production ranged between 3 and 10 g/100 ml. There was no appreciable difference in the metabolic behaviour between toxigenic and non-toxigenic strains of A. flavus when dry mycelial weight, total proteins, non-protein nitrogen and reducing sugar were the criteria.

Effect of probucol on triton induced hyperlipidemias in CFY rats.

The two phases of triton test have been used to find out the effect of probucol to evaluate whether it is effective cholesterol lowering agent prophylactically or therapeutically. Probucol is shown to be a better accelerator for lipid clearance in triton hyperlipidemia than clofibrate. The clearance rate of VLDL is more than that of LDL. In the first phase of triton test probucol has more effect on cholesterol synthesis than triglycerides while in the second phase of triton test probucol has more effect as a clearing agent on triglycerides than on cholesterol.

St-93 hyperglycemia in Wistar rats.

The alpha 2-adrenoceptor agonist St-93 was evaluated for its effect on blood glucose levels in Wistar rats. A dose-dependent increase in blood glucose was observed in rats after intraperitoneal administration of St-93. The hyperglycemic effect of St-93 was not altered by prazosin and propranolol, whereas idazoxan significantly inhibited this effect. Pretreatment with reserpine did not affect the hyperglycemic effect of St-93. There was no significant increase in the blood glucose values with St-93 in streptozotocin-diabetic rats. It may be concluded that the hyperglycemia induced by St-93 is mediated through alpha 2-adrenoceptors, possibly located on pancreatic beta-cells.