BACKGROUND Cutaneous leishmaniasis (CL) is treated with parenteral drugs for decades with decreasing rate cures. Miltefosine is an oral medication with anti-leishmania activity and may increase the cure rates and improve compliance. METHODOLOGY/PRINCIPAL FINDINGS This study is a randomized, open-label, controlled clinical trial aimed to evaluate the efficacy and safety of miltefosine versus p...

A set of compounds (n = 30), including traditional cytochrome P450 substrates and compounds from AstraZeneca's compound library, was used in an experimental evaluation of an optimal design approach (ODA) for the estimation of enzyme kinetic parameters (CL(int), V(max), and K(m)). A depletion method previously shown to provide reliable results, the multiple depletion curves method (MDCM), was us...

Novel p-tolylimido rhenium(V) complexes trans-(Cl,Cl)-[Re(p-NC6H4CH3)Cl2(py-2-COO)(PPh3)]·MeCN (1a), trans-(Cl,Cl)-[Re(p-NC6H4CH3)Cl2(py-2-COO)(PPh3)] (1b), trans-(Br,Br)-[Re(p-NC6H4CH3)Br2(py-2-COO)(PPh3)] (2), cis-(Cl,Cl)-[Re(p-NC6H4CH3)Cl2(py-2-COO)(PPh3)] (3), cis-(Br,Br)-[Re(p-NC6H4CH3)Br2(py-2-COO)(PPh3)]·H2O (4), trans-(Cl,Cl)-[Re(p-NC6H4CH3)Cl2(OMe)] (5) and trans-(Br,Br)-[Re(p-NC6H4CH3...

Ca(2+)-activated Cl(-) currents (I(Cl,Ca)) were examined using fluorescence confocal microscopy to monitor intracellular Ca(2+) liberation evoked by flash photolysis of caged inositol 1,4, 5-trisphosphate (InsP(3)) in voltage-clamped Xenopus oocytes. Currents at +40 mV exhibited a steep dependence on InsP(3) concentration ([InsP(3)]), whereas currents at -140 mV exhibited a higher threshold and...

The structures of 1,2,4-triazolium chloride (C2H4N3)Cl and its derivative with antimony trichloride (C2H4N3)2[SbCl5] ÿ (C2H4N3)Cl containing unsubstituted 1,2,4-triazolium cations were determined. (C2H4N3)Cl crystallizes in the monoclinic system, space group P21/n with the unit cell dimensions at 86 K: a = 9.425(2), b = 8.557(2), c = 11.158(2) Å, þ = 95.87(3); V = 895.2(3) Å3,Z= 8,dc = 1.566,dm...

The aim of the current study was to evaluate the accuracy of allometric scaling methods for drugs metabolized by UDP-glucuronosyltransferases (UGTs), such as ketoprofen, imipramine, lorazepam, levofloxacin, zidovudine, diclofenac, furosemide, raloxifene, gemfibrozil, mycophenolic acid, indomethacin, and telmisartan. Human plasma clearance (CL) predictions were conducted from preclinical in vivo...

CL/Fpop and V/Fpop represent the typical oral clearance value and apparent volume of distribution value for the adult population, and weightpop represents a typical weight for the adult population. CL/F for an infant was also allowed to mature to an allometrically scaled adult value according to age (months) to reach the population value CL/Fpop, hence kmat is a first-order rate constant that d...

in published high performance liquid chromatographic (hplc) methods for analysis of topiramate (tpm) in pharmaceutical dosage forms and raw materials refractive index detector (rid) has been used which is not available in many laboratories and has low sensitivity. we described a new, sensitive and simple hplc method for determination of topiramate in pharmaceutical forms and in-virto dissolutio...

Ferrocenyl platinum(ii) complexes (), viz. [Pt(Fc-tpy)Cl]Cl (), [Pt(Fc-tpy)(NPC)]Cl (, HNPC = N-propargyl carbazole) and [Pt(Fc-bpa)Cl]Cl (), were prepared, characterized and their anti-proliferative properties in visible light in human keratinocyte (HaCaT) cell lines have been studied. [Pt(Ph-tpy)Cl]Cl () was prepared and used as a control. Complexes and , structurally characterized by X-ray c...