Syntheses of New Unsymmetrical 2,5‐Disubstituted‐1,3,4‐oxadiazoles and 1,2,4‐Triazolo[3,4‐b]‐1,3,4‐thiadiazoles Bearing Thieno[2,3‐c]pyrazolo Moiety

New series of (thieno[2,3‐c]pyrazolo‐5‐yl)‐[1,2,4]triazolo[3,4‐b][1,3,4]thiadiazoles 10a , 10b , 10c and (thieno[2,3‐c]pyrazol‐5‐yl)‐1,3,4‐oxadiazol‐3(2H)‐yl)ethanones 6a , 6b , 6c has been synthesized from thieno[2,3‐c]pyrazole‐5‐carbohydrazide 3 by multistep reaction sequence. (5‐Aryl‐1,3,4‐oxadiazol‐2‐yl)‐1H‐thieno[2,3‐c]pyrazoles 4a , 4b , 4c were also synthesized from thieno[2,3‐c]pyrazole‐5‐carbohydrazide 3 by cyclization with various aromatic carboxylic acids. The hydrazide 3 was obtained by reaction of thieno[2,3‐c]pyrazole‐5‐carboxylate 2 with hydrazine hydrate in good yield, and compound 2 was obtained by the reaction of 5‐chloro‐3‐methyl‐1‐phenyl‐1H‐pyrazole‐4‐carbaldehyde 1 and 2‐ethyl thioglycolate in presence of sodium alcoholate in good yield.     

New Synthesis and Reactions of Ethyl 5‐amino‐4‐cyano‐1‐phenyl‐1H‐pyrazole‐3‐carboxylate

Synthesis of ethyl 5‐amino‐4‐cyano‐1‐phenyl‐1H‐pyrazole‐3‐carboxylate 5 has been achieved via abnormal Beckmann rearrangement of o‐chloroaldehyde 1 . Reaction of o‐aminocarbonitrile 5 with concentrated H₂SO₄ furnished expected o‐aminocarboxamide pyrazole 6 . Key intermediates o‐aminocarbonitrile 5 and o‐aminocarboxamide 6 were successfully utilized for the synthesis of pyrazolopyrimidine derivatives. The replacement of Cl in o‐chlorocarbonitrile 3 with secondary amine furnished new synthon 13 , which was further used for the synthesis of polysubstituted heterocycles. The obtained new products were well characterized by IR, ¹H and ¹³C NMR, and mass spectra.     

A novel piezoelectric immunosensor for the detection of malarial Plasmodium falciparum histidine rich protein-2 antigen

A novel piezoelectric (PZ) immunosensor for the direct detection of malarial Plasmodium falciparum histidine rich protein-2 (PfHRP-2) antigen was developed. The mixed self-assembled monolayers (SAMs) of thioctic acid and 1-dodecanethiol were formed on gold surface of quartz crystal. Cyclic voltammetry, electrochemical impedance spectroscopy and surface Raman spectroscopy techniques were used to characterize the mixed SAMs. The rabbit anti-PfHRP-2 antibodies were coupled on mixed SAM modified gold surface of quartz crystal via NHS/EDC activation method. The PZ immunosensor was applied to detect PfHRP-2 in the linear range of 15-60 ng/ml with a detection limit of 12 ng/ml. It was also found that even after 14 days of storage, 50% of the activity still remained. Clinical human serum samples were tested with this method, and the results were in agreement with those obtained from commercially available ICT kit (NOW^® Malaria).     

Assessment of Physical Process Conditions for Enhanced Production of Novel Glutaminase-Free L-Asparaginase from <Emphasis Type="BoldItalic">Pectobacterium carotovorum</Emphasis> MTCC 1428

Statistically based experimental design was applied to maximize the production of glutaminase-free L-asparaginase from Pectobacterium carotovorum MTCC 1428. The effect of physical process parameters (initial pH of the medium, temperature, rpm of the shaking incubator, and inoculum size) on the production of L-asparaginase from P. carotovorum MTCC 1428 was studied using central composite design technique. The individual optimum levels of initial pH of the medium, temperature, rpm of shaking incubator, and inoculum size were found to be 6.90, 29.8 °C, 157 rpm, and 2.61% (v/v), respectively, for the production of L-asparaginase. After physical process parameters optimization, the production and productivity of L-asparaginase was enhanced by 26.39% (specific activity) and 10.19%, respectively. Maximization of L-asparaginase production was achieved at 12 h under optimal levels of physical process parameters in shake flask level.     

Control of structure formation in phase-separating systems

In this paper, we study the evolution of phase-separating binary mixtures which are subjected to alternate cooling and heating cycles. An initially homogeneous mixture is rapidly quenched to a temperature T(1)T(c). These cycles are repeated to create a domain morphology with multiple length scales, i.e., the structure factor is characterized by multiple peaks. For phase separation in d = 2 systems, we present numerical and analytical results for the emergence and growth of this multiple-scale morphology.     

Effect of ethanolic extract of Rubia peregrina L. (Rubiaceae) on monoamine-mediated behaviour

In the traditional system of medicine in Sardinia, Rubia peregrina (RP) is reported as an aphrodisiac herb. Since aphrodisiacs may also have dopaminergic activity, and there can be a reciprocal relationship between dopaminergic and serotonergic functions in the central nervous system, the aim here was to study the effect of the ethanolic extract of the aerial parts of R. peregrina on monoamine-mediated behaviour. The RP (100 and 200?mg?kg(-1) intraperitoneally) significantly inhibited haloperidol (1?mg?kg(-1) i.p.) induced catalepsy in mice (p?相似文献   

Branching on hyperplane methods for mixed integer linear and convex programming using adjoint lattices

We present branching-on-hyperplane methods for solving mixed integer linear and mixed integer convex programs. In particular, we formulate the problem of finding a good branching hyperplane using a novel concept of adjoint lattice. We also reformulate the problem of rounding a continuous solution to a mixed integer solution. A worst case complexity of a Lenstra-type algorithm is established using an approximate log-barrier center to obtain an ellipsoidal rounding of the feasible set. The results for the mixed integer convex programming also establish a complexity result for the mixed integer second order cone programming and mixed integer semidefinite programming feasibility problems as a special case. Our results motivate an alternative reformulation technique and a branching heuristic using a generalized (e.g., ellipsoidal) norm reduced basis available at the root node.     

Rice and Rice‐Shapiro Theorems for transfinite correction grammars

Hay and, then, Johnson extended the classic Rice and Rice‐Shapiro Theorems for computably enumerable sets, to analogs for all the higher levels in the finite Ershov Hierarchy. The present paper extends their work (with some motivations presented) to analogs in the transfinite Ershov Hierarchy. Some of the transfinite cases are done for all transfinite notations in Kleene's important system of notations, $\mathcal {O}$. Other cases are done for all transfinite notations in a very natural, proper subsystem $\mathcal {O}_{\mathrm{Cantor}}$ of $\mathcal {O}$, where $\mathcal {O}_{\mathrm{Cantor}}$ has at least one notation for each constructive ordinal. In these latter cases it is open as to what happens for the entire set of transfinite notations in $(\mathcal {O} -\mathcal {O}_{\mathrm{Cantor}})$.