Resistance carboxamides

Kraus et al.75 78) in Israel fabricated new aromatic phosphoric amide-carboxamide copolymers, which gave membranes high thermal stability, flame resistance, and salt rejection. Thus a copolymer was prepared from N,N -bis(3-aminophenyl)-N"-phenylphosphoric triamide 25, m-phenylenediamine and isophthaloyl chloride in... 

The resistance of the furoxan ring to chemical attack allows derivatives to be prepared via the reactions of the substituents (Section 4.22.3.4). Carboxylic acids are available by permanganate oxidation of methyl derivatives or by hydrolysis of the corresponding esters reaction with ammonia affords carboxamides. Acylfuroxans provide a source of hydroxyalkyl compounds by reduction, and oximes, for example, via nucleophilic addition. Acylation and oxidation of aminofuroxans allows the amide and nitro derivatives to be prepared. Nucleophilic displacements of nitro substituents can take place, but can be somewhat hazardous on account of the explosive nature of these compounds. Alkoxy derivatives are formed with sodium alkoxide, while reaction with thiolate anions yields sulfides, from which sulfones can be synthesized by peracid oxidation. Nitrofuroxans have also been reduced to... 

The liquid range of HMPA is 7.2-235°C its dielectric constant is 30 (20" C). HMPA solvates cations strongly, whereas anions are less solvated. Unlike carboxamides, such as DMF, it is not attacked by aqueous alkali at t < SO C, and it is very resistant toward nucleophilic attack [377] but forms peroxides under the influence of light and oxygen [376]. 

BLM is also metabolized by bleomycin hydrolase, which is an enzyme catalyzing the hydrolysis of the (3-amino-alanine carboxamide (upper left of structure). The carboxylic acid obtained shows decreased DNA affinity. Several hydrolase-resistant BLMs, where the carboxamide nitrogen carries a 3-(a-methyl-benzylamino) propylamine group, exhibited lower pulmonary toxicity. 

Dimethylformamide diethylacetal converted 2-benzylaminopyrazine-3-carboxamide to l-benzylpteridin-4-one (see 10) in good yield after 1 hr of refluxing, although this pyrazine had resisted the more common cyclizing agents.230... 

One of the unique features of BLM is its lack of significant hepatic, renal, and bone marrow toxicities, undesired effects of many anticancer drugs. Two drawbacks are the tumor resistance and the BLM-induced pulmonary toxicity. Both effects are related to the level of BLM hydrolase, a protease that binds to DNA and inactivates BLM by hydrolyzing the /3-alanine carboxamide moiety (14, 15). Cells with high levels of BLM hydrolase are resistant to bleomycin, whereas lungs are sensitive to BLM-induced tissue injuries because of low levels of this enzyme. The structure of this protease, which binds DNA and is conserved from bacteria to humans, has been solved (16). 

Extensive studies of structural-activity relationships of carboxamides have been made, particularly in regard to the molecular designs that inhibit carboxin resistant mutants of Ustilago maydis ( l5 These Investigations have shown that... 

Carboxamides Highly Active Against Carboxin-Resistant Succinic Dehydrogenase Complexes from Carboxin-Selected Mutants of Ustilago maydis and Aspergillus nidulans, Pestic. Biochem. Physiol, 1978, 9,165. 

Synonyms Alkali resistant dark red Cl 12355 Cl pigment red 23 3-Flydroxy-4-[(2-methoxy-5-nitrophenyl) azo]-3 -nitro-2-naphthanilide 3-Flydroxy-4-((2-methoxy-5-nitrophenyl)azo)-N-(3-nitrophenyl)-2-naph-thalene carboxamide 1 -(2-Methoxy-5-nitrophenylazo)-2-hydroxy-3-(3-nitrophenylcarbamoyl) naphthalene 2-Naphthalenecarboxamide Naphthol red B Empirical C24FI17N5O7... 

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