Novel Fluoroquinolones With Pinane Moiety: Synthesis and Antimicrobial Activity.

Here, we report a synthesis of fluoroquinolones carrying a monoterpene moiety at the C7 position of aromatic structure. The minimal inhibitory concentrations of fluoroquinolone fused with trans-3-hydroxy-cis-myrtanylamine 18 against Staphylococcus aureus (MSSA isolates) were two- to eightfold lower compared to moxifloxacin, although fourfold higher against MRSA isolates. The fluoroquinolone fused with (-)-nopylamine 16 was four- to eightfold less active on MSSA compared to moxifloxacin, while had similar activity on MRSA.

A novel terpene-BODIPY conjugates based fluorescent probes: Synthesis, spectral properties, stability, penetration efficiency into bacterial, fungal and mammalian cells.

The design of fluorescent probes based on biocompatible luminophores for medical diagnostics is one of the rapidly developing areas worldwide. Here, we report the synthesis of a novel BODIPYs containing a propanoic acid residue at the α-position of one of the pyrrole rings conjugated to (+)-myrtenol or thiotherpenoid. Both conjugates are quite photostable (t ∼ 40 h) and exhibit high fluorescence efficiency (φ ∼ 77-90 %).

Unraveling the Mechanism of Platelet Aggregation Suppression by Monoterpenoids.

Platelet aggregation causes various diseases and therefore challenges the development of novel antiaggregatory drugs. In this study, we report the possible mechanism of platelet aggregation suppression by newly synthesized myrtenol-derived monoterpenoids carrying different heteroatoms (sulphur, oxygen, or nitrogen). Despite all tested compounds suppressed the platelet aggregation in vitro, the most significant effect was observed for the S-containing compounds.

Deep Insights into Heavy Oil Upgrading Using Supercritical Water by a Comprehensive Analysis of GC, GC-MS, NMR, and SEM-EDX with the Aid of EPR as a Complementary Technical Analysis.

Upgrading of heavy oil in supercritical water (SCW) was analyzed by a comprehensive analysis of GC, GC-MS, NMR, and SEM-EDX with the aid of electron paramagnetic resonance (EPR) as a complementary technical analysis. The significant changes in the physical properties and chemical compositions reveal the effectiveness of heavy oil upgrading by SCW. Especially, changes of intensities of conventional EPR signals from free radicals (FRs) and paramagnetic vanadyl complexes (VO) with SCW treatment were noticed, and they were explained, respectively, to understand sulfur removal mechanism (by FR intensity and environment destruction) and metal removal mechanism (by VO complexes' transformation).

Stereodynamics of some pyridoxine derivatives.

The conformational properties of three pyridoxine derivatives were studied by H dynamic NMR spectroscopy. Conformational exchange caused by a rotation of 2-nytrophenyl group around one single C-C bond, of 2,4-dinitrophenyl substituent around two single C-O bonds, and twist-twist transformations of the seven-membered ketal cycle was observed by NMR experiments at low temperatures. Meanwhile, the conformational exchange of the acetal ring remains fast in the NMR timescale even at 198 K.

Dynamic NMR study of dinitrophenyl derivatives of seven-membered cyclic ketals of pyridoxine.

Two pyridoxine derivatives containing a dinitrophenyl moiety were investigated by (1)H NMR spectroscopy. Conformational dynamics in solution were studied for each compound using dynamic NMR experiments. It was shown that both compounds studied are involved into two conformational exchange processes.

Structure of pravastatin and its complex with sodium dodecyl sulfate micelles studied by NMR spectroscopy.

The aim of this work was to study the mechanisms of interaction between pravastatin and cell membranes using model membranes (sodium dodecyl sulfate micelles) by nuclear magnetic resonance spectroscopy methods. On the basis of the nuclear magnetic resonance experiments, it was established that pravastatin can form intermolecular complexes with sodium dodecyl sulfate micelles by the interaction of its hydrophilic groups with the polar surface of the micelle. Conformational features of pravastatin molecule were also studied.

Dynamic NMR study of cyclic derivatives of pyridoxine.

A series of pyridoxine derivatives was investigated by (1) H and 2D nuclear overhauser enhancement spectroscopy (NOESY) NMR. The free energies of activation for the pyridyl-oxygen rotation of the 2,4-dinitrophenyl ether of the seven-membered acetals of pyridoxine were measured by dynamic NMR. A conformational exchange between the chair and twist forms of the seven-membered acetal ring was confirmed by dynamic NMR and STO3G computations.

[Anaphylactic contraction is a property of many but not all skeletal muscles].

The authors studied the ability for anaphylactic contraction in vitro of musculus plantaris, diaphragmatic muscle and musculus soleus of guinea pig. The muscles of double sensitized pigs were denervated and 4 weeks after the nerve cut the muscles' specimens were studied for anaphylactic contraction. The addition of the resolving dose of the specific antigen to incubation medium resulted in anaphylactic contraction of the diaphragmatic muscle and musculus soleus.

[Effects of the respiratory epithelium on the tracheal smooth muscle in guinea pigs].

We studied the influence of respiratory epithelium on tracheal smooth muscle tone of guinea pigs. Mechanical removal of the epithelium induced an increase of the contractile response to histamine. In preparation of smooth muscle previously contracted by histamine, isoproterenol induced dose--dependent relaxation, the level of which was significantly greater in tracheal smooth muscle with epithelium than without it.

[Immunologic criteria of the evaluation of the severity of the condition of patients with mechanical jaundice].

Examination of 62 patients with mechanical jaundice has established a pronounced disproportion in the ratio of the amount of "general" T-, "active" T- and "theophylline-sensitive" T-lymphocytes which suggests the critical state of the patient especially if it persists in the early postoperative period. The dynamics of the content of serum immunoglobulin A reflects the degree of resolution of hypertension in bile ducts while the clinical value of this test is not high enough due to its being very time-taking.

[Experimental study of the allergenic and modulating properties of RNAses].

It was shown with the immediate type hypersensitivity (ITH) test and the delayed type hypersensitivity (DTH) test that pancreatic RNase and RNases from Bacillus sp. had rather pronounced allergenic properties which were similar in both the tests. The modulating properties of the RNases with respect to sensitization in accordance with ITH or DTH were also investigated.

[Characteristics of thyrotoxicosis in men].

The clinical and laboratory data were examined in 227 men presenting with thyrotoxicosis and compared with the data obtained during examination of 100 thyrotoxic women. In men, thyrotoxicosis ran a far graver course than in women, showing a rapid progress. Early manifestations of the disease consisted in the impairment of cardiovascular and nervous system functions.

[Redistribution of populations of T- and B-lymphocytes among lymphoid organs in response to hydrocortisone].

Single injection of hydrocortisone to guinea-pigs provoked a remarkable transitory T-lymphocytopenia with transition of T- lymphocytes into the bone marrow during the early stages. On the contrary, the content of B-lymphocytes in the peripheral blood gradually rose and exceeded the normal level twice as much by the end of the first day. Histological analysis did not reveal any signs of massive destruction of lymphocytes.

[Effect of testosterone propionate on the lymphoid system and antibody-producing capacity in golden hamsters].

The effect of testosterone-propionate on the lymphoid tissue and humoral immunological response to SRBC was studied in 224 golden hamsters of both sex. The hormone was injected intramuscularly in a dose of 1 and 5 mg every other day (a total of 10 injections). Testosterone caused thymus atrophy, hypoplasia of the spleen, reduction of the absolute B lymphocyte count in the bone marrow, forming cell count and a fall of the serum hemolysin titre in the immunized animals.