HIV-1 infection of the brain and PAF neurotoxicity are implicated in AIDS dementia complex. We previously reported that a trisubstituted piperazine derivative is able to diminish both HIV-1 replication in monocyte-derived macrophages and PAF-induced platelet aggregation. We report in this work new compounds obtained by modifying its piperazine substituents. The structure-activity relationship s...

Celecoxib, a diaryl substituted pyrazole, is practically insoluble in water which precludes its use in parenteral and liquid dosage forms. This study explores the solubility enhancement of celecoxib using hydrotropy and cosolvency solubilization approaches. The equilibrium solubility studies were performed using hydrotropes piperazine, sodium citrate, and urea and cosolvents PEG 200, PEG 400, P...

Various anthelmintics belonging to different pharmacological groups (ivermectin, clorsulon, closantel, netobimin, febantel, praziquantel, niclofolan, bithionol, trichlorfon, levamisole hydrochloride, piperazine citrate and dihydrochloride, nitroscanate), all of proven efficacy against certain helminths, were tested and compared for their in vivo and in vitro activity on a natural infection of O...

The anthelmintic activities of different extracts of aerial parts of Celsia coromandeliane Vahl and Mollugo pentaphylla Linn were evaluated separately on adult Indian earthworm (Pheritima posthuma). It was found that petroleum ether (PECC), chloroform (CCC), ethanol (ECC) extract of C. coromandeliane and petroleum ether (PEMP), benzene (BMP), ethyl acetate (EAMP), ethanol (EMP) extract of M. pe...

Rat liver ATP citrate lyase was inactivated by 2, 3-butanedione and phenylglyoxal. Phenylglyoxal caused the most rapid and complete inactivation of enzyme activity in 4-(2-hydroxyethyl)-1-piperazine-ethanesulphonic acid buffer, pH 8. Inactivation by both butanedione and phenylglyoxal was concentration-dependent and followed pseudo- first-order kinetics. Phenylglyoxal also decreased autophosphor...

Helminths infections are also among the most common infections in human, affecting a large proportion of the world’s population in developing countries and produce a global burden of disease. Pherithema posthuma a helminthes is commonly known as earth-worms, Leucas aspera herb is distributed throughout India. the anthelminthic property of Leucas aspera was evaluated using Pherithema posthuma as...

The present study was aimed to evaluate anthelmintic activity of aqueous and methanolic extract of Trapa natans L.var. bispinosa Roxb fruit peels and root. The plant commonly known as “Water Chestnut” in India and is an annual aquatic floating herb occurring throughout the Indian subcontinent and used traditionally for several medicinal purposes. The effect of this plant was evaluated for anthe...

The human histamine H(4)-receptor (hH(4)R) possesses high constitutive activity and, like the human H(1)-receptor (hH(1)R), is involved in the pathogenesis of type-I allergic reactions. The study aims were to explore the value of dual H(1)/H(4)R antagonists as antiallergy drugs and to address the question of whether H(1)R ligands bind to hH(4)R. In an acute murine asthma model, the H(1)R antago...

In medicinal chemistry nitrogen containing heterocycles are the most important compounds which show various biological activities. The cinnoline are nitrogenous derivatives and found to elicit many pharmacological actions like anti-hypertensive, antithrombotic, antihistamine, antileukemic, CNS activity, anti tumor, antibacterial and antisecretory activity. We planned to synthesis new series of ...