Four coordination compounds, that include the discrete binuclear complex [Zn(H2O)4(bda4Py)]2(SO4)2 (1), two isomorphous one-dimensional coordination polymers, {[Zn(NO3)2(bda4Py)2]·2H2O}n (2) and {[Cd(NO3)2(bda4Py)2]·2H2O}n (3), and one two-dimensional coordination polymer {[Cd(bda4Py)2(dpa)2]·...
The complexes [Me2(MNAB)SnOSn(MNAB)Me2]2 (2) and [Me2Sn(MNAB)2] (3), where HMNAB is 2-(2-methyl-3-nitroanilino)benzoic acid, (1), have been prepared and structurally characterized by means of vibrational, 1H and 13C NMR spectroscopies. The crystal structure of [Me2(MNAB)SnOSn(MNAB)Me2]2 has been...
The molecular structure of Methyl 2-amino 5-bromobenzoate (M2A5B) was investigated by density functional theory employing Becke’s three parameter hybrid exchange functional with Lee–Yang–Parr (B3LYP) co-relational functional involving 6-311++G(d,p) basis set. Harmonic vibrational wavenumber c...
Bulk single crystal of Methyl 2-amino-5-bromobenzoate (M2A5B) nonlinear optical single crystal of size 60 mm length and 15 mm diameter was successfully grown from solution by Unidirectional growth method of Sankaranarayanan–Ramasamy (SR) for the first time in the literature. The growth conditio...
Good quality single crystal of organic Methyl 2-amino-5-bromobenzoate (M2A5B) was grown using slow evaporation solution growth technique. The grown crystal was confirmed by single crystal X-ray diffraction. The functional groups and vibrational frequencies were identified using FT-IR and FT-Rama...
Triterpenoic acids 1–6 exhibited very low or no cytotoxicity at all, but their corresponding 2,3-di-O-acetyl-piperazinyl amides 13–18 showed low EC50 values for several human tumor cell lines. Their cytotoxicity, however, was also high for the non-malignant mouse fibroblasts NIH 3T3. A signifi...
Based on their biological activity natural products continue to represent optimal lead structures for the development of novel drug candidates. We focused on the syntheses of several derivatives of the triterpene asiatic acid and on the evaluation of their cytotoxic activity in a photometric sul...
We have previously shown differential expression of leucomyosuppressin (LMS) mRNA in apparent endocrine cells in the anterior region of midguts of the cockroach Diploptera punctata, using in situ hybridization. In contrast, other FMRFamide-related peptides, as revealed by immunohistochemistry, h...
The action of leucomyosuppressin (LMS: pGlu-Asp-Val-Asp-His-Val-Phe-Leu-Arg-Phe-NH2) on the glutamate-mediated neuromuscular transmission in the mealworm, Tenebrio molitor, was studied by the microelectrode current-clamp and voltage-clamp techniques. Submicromolar concentrations of LMS reversibl...
1. A neuropeptide that inhibits spontaneous contractions of the isolated cockroach hindgut was purified from head extracts of the cockroach, Leucophaea maderae.2. The inability of aminopeptidase M to degrade the peptide and the presence of glutamic acid in the hydrolysate suggested N-terminal bl...
1. Leucomyosuppressin (LMS) inhibited neurally evoked contractions of the hindgut of the cockroach Leucophaea maderae. The threshold for this inhibition of LMS was in the range of 1 × 10−10 M.2. LMS caused a sharp reduction in both l-glutamate and proctolin induced contractions. Dose-response p...
1. Leucomyosuppressin (LMS) did not inhibit the spontaneous contractions of visceral muscles of the cockroach Leucophaea maderae uniformly as a group but rather showed a selective suppression of activity in the foregut and hindgut. The threshold of LMS inhibition for these organs was 10−11 M for...
The degradation of 2 nmol synthetic leucomyosuppressin (LMS) by enzymes of the hemolymph, midgut lumen and midgut tissues of both Lacanobia oleracea and Spodoptera littoralis was investigated using reversed-phase high-performance liquid chromatography together with matrix assisted laser desorpti...
The feeding pattern of the adult female of Blattella germanica peaks in the middle of the vitellogenic cycle. Following the hypothesis that a factor inhibiting gut peristalsis also inhibits food intake and is involved in the regulation of feeding, we searched for the most powerful myoinhibitory ...
Using HPLC separation, radioimmunoassay, and subsequent bioassay, we have detected the presence of an active peptide, which co-elutes with the insect myoinhibitory peptide leucomyosuppressin, in the brain of the cockroach Diploptera punctata. We have isolated a cDNA encoding the precursor for th...
Myosuppressins are a group of 10-residues FMRFamide-related peptides reported in Dictyoptera, Orthoptera, Lepidoptera and Diptera. Myosuppressins inhibit visceral muscle contractions and, in the cockroach Blattella germanica, inhibit food intake. In B. germanica, the cDNA of leucomyosuppressin (...
Several lines of evidence point to leucomyosuppressin (LMS) and myosuppressin-related peptides as inhibitory modulators of heartbeat frequency in arthropods. Previous studies in Blattella germanica demonstrated that heartbeat frequency decreases after ootheca formation, and remains low during th...
A novel and efficient redox reaction was developed to react 5-amino-1H-pyrazole-4-carbaldehyde with sodium nitrite (NaNO2) in an acidic solution (HCl/MeOH) to generate 5-amino-4-nitrosopyrazole, pyrazole-4-carbaldehyde, or diazenylpyrazole selectively. The results showed that 5-amino-4-nitrosopy...
Hypoxia (inadequate concentrations of dioxygen in tissues) is present in several disease states, including cancer and rheumatoid arthritis. Prodrug systems, which after bioreduction, selectively release active drugs in these tissues may be important in therapy. The 5-nitrothien-2-ylmethyl ester ...
The aim of the present report was to develop and validate simple, sensitive and reliable LC–MS/MS method for quantification of topiramate (TPM) and its main metabolites: 2,3-desisopropylidene TPM, 4,5-desisopropylidene TPM, 10-OH TPM and 9-OH TPM in human plasma samples. The most abundant metab...
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