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Disclosed are compounds of the general formula: wherein R1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R is hydrogen, R or R4 where R is an organic residue attached to the azetidine ring through a carbon atom therein and R4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula wherein R5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof. The compounds have antimicrobial and/or beta-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals

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Pyridazine – Wikipedia,
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N,N’-Diacyldiaza-18-crown-6 ethers were obtained by the acylation of diaza-18-crown-6 with amino acids.The enantioselectivity coefficients were determined for the chiral compound in relation to the L and D isomers of valine.The obtained compounds represent a promising class of enantioselective complexones.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. HPLC of Formula: C10H7ClN2, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 20375-65-9, name is 3-Phenyl-6-chloropyridazine. In an article,Which mentioned a new discovery about 20375-65-9

Biocatalytic methods for peptide synthesis are of high value due to the rapidly increasing approval of peptide-based therapeutics and the need to develop new analogs. Guinea pig liver transglutaminase (gTG2) catalyzes the cross-linking of peptides and proteins via the formation of gamma-glutamyl-epsilon-lysyl isopeptide bonds. In this study, we investigate gTG2-catalyzed peptide bond formation between various amino acid-derived donor and acceptor substrates. Using LC-MS analysis, we demonstrate that gTG2 forms Gly-Xaa and d-Ala-Gly dipeptide products, confirming that its natural transamidation activity can be co-opted for peptide synthesis. An aromatic ester of Gly was the most efficient acyl-donor substrate tested; aromatic esters of d-Ala and l-Ala showed 50-fold lower reactivity or no reactivity, respectively. A computational strategy combining computational protein design algorithms and molecular dynamics simulations was developed to model the binding modes of donor substrates in the gTG2 active site. We show that the inability of gTG2 to efficiently catalyze peptide synthesis from donors containing alanine results from the narrow substrate binding tunnel, which prevents bulkier donors from adopting a catalytically productive binding mode. Our observations pave the way to future protein engineering efforts to expand the substrate scope of gTG2 in peptide synthesis, which may lead to useful biocatalysts for the synthesis of desirable bioactive molecules.

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Pyridazine – Wikipedia,
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Oxidative rearrangement of allylic selenides in the presence of various amine nucleophiles provides synthetic access to a variety of allylic amine derivatives.The stereochemical outcome of these reactions has been investigated, and is consistent with a <2,3>-sigmatropic rearrangement mechanism.Several D-alpha-amino acids and racemic beta,gamma-unsaturated alpha-amino acids were prepared in this manner.A variant of this process employing an achiral allylic selenide and chiral amide afforded protected allylic amines in low diastereoisomeric excess.

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Screening of a combinatorial CTV-based artificial, synthetic receptor library 1 {1-13, 1-13, 1-13} for binding of a variety d-Ala-d-Ala and d-Ala-d-Lac containing ligands (6-11) was carried out in phosphate buffer (0.1 N, pH=7.0). After screening and Edman sequencing, synthetic receptors were found containing amino acid sequences, which are either characteristic for binding dye labeled d-Ala-d-Ala or d-Ala-d-Lac containing ligands. For example, receptors capable of binding d-Ala-d-Ala containing ligands 6, 7, 9 and 11 contained – almost in all cases – at least one basic amino acid residue – predominantly Lys – in their arms. This was really a striking difference with the arms of the receptors capable of binding d-Ala-d-Lac containing ligands 8 and 10, which usually contained a significant number of polar amino acids (Gln and Ser), especially in ligand 8, but hardly any basic amino acids. Use of different (fluorescent) dye labels showed that the label has a profound, albeit not decisive, influence on the binding by the receptor. A hit from the screening of the CTV-library with FITC-peptidoglycan (6) was selected for resynthesis and validation. Graphical Abstract.

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The synthesis of a series of stevastelin analogues with modification of the susbstituent at the C-2 position of the stearic acid chain (compounds 28 and 31), variation of the amino acids (compounds 41, 42, 73, and 78), or lacking the lipidic chain (compound 91) is described. The replacement of L-valine and L-threonine with other amino acids proceeded without difficulties for the synthesis of analogues 41 and 42; however, the substitution of L-serine with simple amino acids, such as glycine or L-alanine, proved to be elusive, which was adscribed to factors of conformational flexibility. Finally, the substitution with L-valine or L-threonine proceeded without difficulties to provide the analogues 73 and 78 respectively.

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Pyridazine – Wikipedia,
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As a key intermediate for the synthesis of sulfazecin derivatives, 3-amino-3-methoxy-2-azetidinone (24 or 26) was synthesized from penicillins, and various new compounds, including sulfazecin, were synthesized by acylation and sulfonation of 24 or 26. Some of these compounds (33, 36) showed higher antibacterial activity than the corresponding 3-demethoxy derivatives against a beta-lactamase-producing strain of Escherichia coli.

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For the first time the synthesis of covalently linked very water-soluble chiral perylenediimides (PDIs) is presented. The PDIs carry the amino acids alanine or lysine as imide substituents, respectively, which are coupled to Newkometype dendrimers acting as hydrophilic groups. The tert-butylprotected precursors 5 as well as its water-soluble free acid compounds 6 were investigated by absorption, fluorescence and circular dichroism (CD) spectroscopy. Except for the sterically most crowded 2nd generation alanine compounds 5f and 6f all chiral dyes show bisignate CD effects which indicate helical aggregation. The 1st generation alanine compound 6b shows the greatest CD effects in buffer solution and its aggregation behaviour was also directly proven by the use of cryogenic transmission electron microscopy. Furthermore, the formation of chiral superstructures of 6b was found to be pH- and concentration-dependent.

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Pyridazine – Wikipedia,
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Selective 4-N-acylation of fortimicin B (2) has been accomplished by 4-N-acylation of 1,2′,6′-tri-N-benzyloxycarbonylfortimicin B (4) followed by hydrogenolysis of the N-protecting benzyloxycarbonyl groups. In this manner, fortimicin B was converted into fortimicin A (1), and a series of 4-N-acylfortimicins B (3) was prepared for antibacterial assay. The key intermediate, 1,2′,6′-tri-N-benzyloxycarbonylfortimicin B, was prepared either directly from fortimicin B or by converting fortimicin A into 1,2′,6′,2”-tetra-N-benzyloxycarbonylfortimicin A (6a), followed by selective hydrolysis of the 4-N-(N-benzyloxycarbonyl)glycyl group of the latter.

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The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R1 and R2 each independently represent a hydrogen atom, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like; R5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms.

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Pyridazine – Wikipedia,
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