4-amino methyl pyridine anchored silica gel (4-AMPS) was used as a sorbent in a simple sensitive spectrophotometry determination of Cu (II) in various samples using piperazine dithiocarbamate as a color developing agent (λmax 420 nm) at pH 5.0 ± 0.2. Beer’s law was obeyed over the range of 0.2 -13 μg ml-1. The molar absorptivity and Sandell’s sensitivity were 0.5731 × 105 l mol-1cm-1 and 0.0022...

The serotonin(1A) (5-hydroxytryptamine [5-HT](1A)) receptors are members of a superfamily of seven transmembrane domain receptors that couple to G-proteins. Serotonergic signalling has been shown to play an important role in alcohol intake, preference and dependence. G-protein coupling of the 5-HT(1A) receptor serves as an important determinant for serotonergic signalling. We have studied the e...

Two series of 2-thioxoimidazo[4,5-b]pyridine derivatives have been synthesized from 2,3-diaminopyridine (1) and 5-halogenosubstituted-2,3-diaminopyridines 2, 3. Mannich bases 7 - 12 and 24 - 29, derivatives of 1-arylamino-6-halogeno-2-thioxoimidazo[4,5-b]pyridine were obtained with selected secondary amines: morpholine, piperidine, 2-methoxyphenylpiperazine, pyrimidyn-2-yl-piperazine and formal...

Alcohol and aqueous extracts from the leaves of Argemone mexicana were investigated for their anthelmintic activity against Pheretima posthuma and Ascardia galli. Five concentrations (6.25, 12.5, 25, 50 and 100 mg/ml) of each extracts were studied in activity, which involved the determination of time of paralysis and time of death of the worms. Both the extracts exhibited significant anthelmint...

Sildenafil [SIL (Viagra); Pfizer, New York, NY] is a widely prescribed agent for erectile dysfunction in men older than 65 years. The present study evaluated experimental models to assess age-dependent changes in SIL biotransformation using hepatic microsomes from male rats and mice ranging from 6 weeks to 26 months of age. The role of specific isoforms in the conversion of SIL to its primary c...

The in vitro response of adults (males and females) and free-living stages of Necator americanus one of the human hookworms, to a wide variety of 20 broad and narrow spectrum anthelmintics was tested. Almost all the broad spectrum anthelmintics influenced males, females and free-living stages at different levels and showed good activity with EC50 values varying from about 0.0002 and 0.0007 mg/l...

The in vivo convulsant activities in rats of five representative fluoroquinolones (FQs), norfloxacin, enoxacin, sparfloxacin, fleroxacin, and pefloxacin, were compared. The experimental approach allowed distinction between the drugs' ability to reach the pharmacological receptors at the level of the central nervous system (pharmacokinetic contribution) and their ability to interact with these r...

Drugs that decrease drug-maintained responding at doses that do not decrease other behaviors in animals may be suitable candidates for development as medications to treat drug abuse in humans. The present study examined whether this effect could be obtained with phentermine, a drug that has been reported to decrease cocaine intake in humans. Rhesus monkeys were trained under multiple fixed-rati...

The title compound, C(26)H(36)N(2)O(6), was synthesized from 9α-hy-droxy-parthenolide (9α-hy-droxy-4,8-dimethyl-12-methylen-3,14-dioxa-tricyclo-[9.3.0.0(2,4)]tetra-dec-7-en-13-one), which was isolated from the chloro-form extract of the aerial parts of Anvillea radiata. The mol-ecule is built up from fused five- and ten-membered rings with two additional ep-oxy ring systems and a meth-oxy-pheny...

Design and synthesis of triazole library antifungal agents having piperazine side chains, analogues to fluconazole were documented. The synthesis highlighted utilization of the click chemistry on the basis of the active site of the cytochrome P450 14α-demethylase (CYP51). Their structures were characterized by (1)H-NMR, (13)C-NMR, MS and IR. The influences of piperazine moiety on in vitro antif...