A new polythiophene derivative, poly-2,3-bis(4-tert-butylphenyl)-5,8-bis(4-hexylthiophen-2-yl)quinoxaline (PHTQ) was synthesized by both chemical and electrochemical polymerization and its electrochemical properties were reported. The monomer was electrochemically polymerized in the presence of ...
Soluble 4-tert-butylphenyl substituted derivatives of 2,2′:6′,2″-terpyridine, 2,2′:6′,2″:6″,2″′-quaterpyridine, 2,2′:6′,2″:6″,2″′:6″′,2″″-quinquepyridine and 2,2′:6′,2″:6″,2″′:6″′,2″″:6″″,2″″′-sexipyridine have been prepared. The ligands and their metal complexe...
Comparative anticestodal efficacies of single dose oral treatments with the powdered fruit of Mallotus philippinensis called Kamala (125, 250 and 375 mg/kg BW), its water or methanol extracts (equivalent to 375 mg/kg) and the total glycosides (25, 50 and 100 mg/kg) were determined in naturally c...
Single dose oral treatments of kamala, the dried, powdered fruit of Mallotus philippinensis (250, 375, 500 and 750 mg kg−1 liveweight), were compared with a single dose of fenbendazole (Panacur®) (10 mg kg−1 liveweight, as recommended by the manufacturer) to determine the relative effectiveness ...
The present study was designed to investigate the adverse effects of indigenous Kamala seed etheral extract on various reproductive parameters of female rats. Animals were treated with various doses (50, 75 and 100 mg/kg body weight, (bw)) of seed extract through gavage for 30 days. Treatment wi...
The availability of forage resources during the dry season is often a critical factor in determining the distribution and movement of large herbivores. It has long been suspected that the Kamala tree (Mallotus philippinensis) can serve as an indicator of the distribution for Asian elephants duri...
Reaction of 6-aryl-3-trichloromethyl-1,2,4-triazines with 1-morpholinocyclopentene affords 4-aryl-1-dichloromethyl- 6,7-dihydro-5H-cyclopenta[c]pyridines.
3-Chloro-3-chlorosulfenylchroman-4-ones are efficiently obtained from chroman-4-ones by treatment with thionyl chloride. Direct oxidation affords 3,3-dichlorochroman-4-ones, whilst conversion to the sulfenamides prior to oxidation provides a facile route to 3-chlorochroman-4-ones.
The reaction of the α-sulfinyl carbanion of dichloromethyl p-tolyl sulfoxide with a variety of α,β-unsaturated carbonyl compounds gave highly substituted cyclopropanes (up to five substituents) in good to high yields with high stereoselectivity.
While gem-dichloromethyl groups can be directly synthesized by the mono-dechlorination of the corresponding trichloromethyl groups, the suppression control of the over-reduction to form chloromethyl or methyl functionalities is quite difficult. We have established the efficient and widely applic...
A highly sensitive method for the determination of 3-chloro-4-dichloromethyl-5-hydroxy-2(5H)-franone (MX) in water by gas chromatography with electron-capture detection is described. MX was derivatized with 2,2,3,3,3-pentafluoropropanol and the product was easily decomposed by UV irradiation. Th...
Here anhydrous and hydrated multi-component organic acid-base salts of 2,6-diaminopyridine have been prepared with the organic acids as trichloroacetic acid, 3,5-dinitrobenzoic acid, 5-nitrosalicylic acid, 3,5-dihydroxybenzoic acid, 5-sulfosalicylic acid, m-phthalic acid, naphthalene-1,5-disulfo...
Our previous study showed that nicardipine and its structural analog, methyl 2-(N-benzyl-N-methylamino)ethyl-2,6-dimethyl-4-(2-isopropyl-pyrazolo[l,5-a]pyridine-3-yl)-l,4-dihydro-pyridine-3,5-dicarboxylate (AHC-52), which is devoid of calcium channel blocking activity, were equally effective in ...
Delavirdine is a novel non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1-infected patients. A simple and rapid high-performance liquid chromatographic method for the quantification of delavirdine in human plasma suitable for drug monitoring in patients is described. Sampl...
The objective of the study was to investigate the safety and antiviral effect of three delavirdine dose regimens or placebo in combination with zidovudine in patients who were already taking zidovudine. Eighty-nine symptomatic HIV-1 seropositive individuals with CD4+ cell counts between 50 and 3...
This study was performed to determine delavirdine protein-binding characteristics as well as those of its N-dealkylated metabolite (N-DLV). Initial studies of 36 μM delavirdine and 30 μM N-DLV in solutions of plasma, albumin 4 g%, alpha-1-acid glycoprotein (AAG) 100 mg% or immune globulin (IVI...
In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[(1-methyl-ethyl)amino]-2-pyridinyl}-4-{[5-(4-{5[(1E)-2-(hydroxyphenyl)ethenyl]-1,3-benzenedioyl-carbonylbutanoyl}amino)-1H-indol-2-yl]carbonyl}-piperazine was synthesized by linking the del...
Delavirdine is a newly developed anti-HIV-1 drug for AIDS therapy. This study describes a sensitive high-performance liquid chromatographic method for the determination of delavirdine in 50 μl of plasma. Samples were deproteinized with 150 μl of a solution of internal standard (cisapride 10 μ...
The oxidative metabolism of delavirdine, a non-nucleoside inhibitor of HIV-1 reverse transcriptase, is mediated in part by cytochrome P450 3A. The influence of rifabutin, an inducer of certain human cytochrome P450 isozymes, on the steady-state pharmacokinetics of delavirdine was investigated in...
Delavirdine mesylate is a non-nucleoside inhibitor of the reverse transcriptase enzyme found in human immunodeficiency virus type 1 and is indicated for treatment of this infection. Several solid-state forms of delavirdine mesylate have been identified and characterized. Crystallization of delav...
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