INTRODUCTION Angiotensin-converting enzyme (ACE) inhibitors represent a significant group of drugs primarily used in the treatment of hypertension and congestive heart failure. OBJECTIVE Selected ACE inhibitors (enalapril, quinapril, fosinopril, lisinopril, cilazapril) were studied in order to establish a fast and easy estimation method of their plasma protein binding degree based on their li...

A series of 18 N-alkyl substituted 3-aminopyrazine-2-carboxamides was prepared in this work according to previously experimentally set and proven conditions using microwave assisted synthesis methodology. This approach for the aminodehalogenation reaction was chosen due to higher yields and shorter reaction times compared to organic reactions with conventional heating. Antimycobacterial, antiba...

OBJECTIVE To determine whether adverse effects such as elevated intraocular pressure and cataracts, which are lower with dexamethasone when compared with fluocinolone acetonide or triamcinolone acetonide, may be explained in part by the differences in drug lipophilicity and partitioning of these drugs into the trabecular meshwork and lens. METHODS The n-octanol/phosphate-buffered saline (pH 7...

Abstract Photodynamic therapy involves the concomitant action of three components, light with an appropriate wavelength, molecular oxygen, and a molecule, able to absorb electromagnetic radiation, called photosensitizer (PS). A fundamental aspect is bioavailability PS that directly related some physicochemical properties itself as it should feature certain degree lipophilicity easily cross cell...

We successively introduce new catalytic centers through click reaction into MOFs and modify their environment by addition of lipophilic groups. The resulting bifunctionalized MOF provides an optimized balance between basicity and lipophilicity and shows outstanding performance for the transesterification reaction.

The presented review article deals with various conjugates of arabinosylcytosine (araC). This powerful drug that is routinely used in therapy of hematological malignancies has some shortcomings, which limit its use and therapeutic effects. These are low lipophilicity, low stability to degrading enzymes and need for biological activation through phosphorylation. Conjugating araC to another molec...

Five cationic platinum(II) complexes of general formula, [Pt(NH(3))(2)(β-diketonate)]X are reported, where X is a noncoordinating anion and β-diketonate = acetylacetonate (acac), 1,1,1,-trifluoroacetylacetonate (tfac), benzoylacetonate (bzac), 4,4,4-trifluorobenzoylacetonate (tfbz), or dibenzoylmethide (dbm), corresponding, respectively, to complexes 1-5. The log P values and the stabilities of...

Small molecule synthetic anion transporters may have potential application as therapeutic agents for the treatment of diseases including cystic fibrosis and cancer. Understanding the factors that can dictate the anion transport activity of such transporters is a crucial step towards their application in biological systems. In this study a series of acylthiourea anion transporters were synthesis...

The lipophilicity of various mu-selective opioids was determined by measuring their distribution between n-octanol and Tris.HCl buffer, pH 7.4, by a procedure requiring submicromolar concentrations (submilligram amounts) of the compounds. After partitioning at 25 degrees C, the concentrations of opioids in the aqueous phase was quantified by their displacement of bound [3H]Tyr-Ala-Gly-(Me)Phe-G...

Through the studies on structure-activity relationships o f 5-acyl-3-(l-aminoalkylidene)4-hydroxy-2 H-pyran-2,6(3 H)-dione derivatives in photosystem II (PS II) inhibition, overall lipophilicity o f the molecule was found to be a major determinant for the activity. In the sub­ stituted N-benzyl derivatives, not only the lipophilicity but also the electronic and steric char­ acters o f the subst...