Isonicotinic hydrazide

Isomorphic monomers, 19 762 Isoniazid, 25 798 Isonicotinic hydrazide, 21 103 Isonitrile complexes, platinum, 19 656 Isonitrile-nitrile rearrangement, 21 149 Isononanoic acid, physical properties, 5 35t Isononyl alcohol, properties of commercial, 2 12t... 

Although many antibiotics are effective to some extent in arresting the progress of tuberculosis, none is uniformly successful. One of the most effective is isonicotinic hydrazide (73), available from methyl isonicotinate by reaction with hydrazine (B-75MI20903). Extensive clinical use of this agent showed the drug to possess an additional antidepressant effect and led to the development of iproniazid (74), an established antidepressant (53JOC994). 

Certain activated hydrazides [235], such as isonicotinic hydrazide, are reduced to the amides ... 

Pyridine derivatives are precursors of many chemical products of medicinal, agricultural, and industrial importance. Pyridine itself is used not only as a solvent, but also as a starting material for pharmaceuticals, herbicides, insecticides, and fungicides. a-Picoline is a precursor for 2-vinylpyridine which is used in the production of an adhesive for textile tire cord. The major use of y-picoline is in the production of isonicotinic hydrazide, an antituberculosis agent. / -Picoline and 2-methyl-5-ethylpyridine are important intermediates in the production of two members of the vitamin B family, nicotinamide, and nicotinic acid (also known as vitamin B3). All this shows there is a substantial need for the production of picolines. The following text describes a novel route to a-picoline which might in the future lead to new processes. 

Pyridine-4-carboxylic acid hydrazide (isonicotinic hydrazide) (C H70N3)... 

Nicotinic acid pyridine 3-carboxylic acid, 123.11, m.p. 234-237°C, first obtained in 1867 from the oxidation of nicotine. It is biologically important as a member of the vitamin Bj complex (see Vitamins). Isonicotinic hydrazide (INH), iff, 137.14, m.p. 163 °C, is an antitubeteulosis agent, which shows antivitamin properties against both nicotinic acid and vitamin B. ... 

The enzyme leading to the modification of p40 does not use NADP directly. The substrate is free phospho ADP-ribose produced by a glycohydrolase present in the microsomal preparation. Addition of isonicotinate hydrazide, an inhibitor of NADP glycohydrolase, prevented incorporation from NADP while incorporation fi om phospho ADP-ribose was hardly affected (Table 1). Also, reduction to NADPH, which is not a substrate for the glycohydrolase, eliminated incorporation into the acceptor polypeptide. Non-enzymatic attachment of labeled phospho ADP-ribose (6) was excluded by the inefficiency of free ADP-ribose to serve as a precursor (Fig. 1, inset), and by denaturation experiments (Table 1) Thermic treatment as well as short exposure to alkali or acid at 0° completely eliminated incorporation (8). 

This normally requires the functioning ot a series of enzyme systems within the cell. The formation of succinyl CoA requires a citric acid cycle as shown by Shemin s tracer studies with succinate-1,4-C and succinate-2,3-C this was also shown by inhibition studies with malonate, trans-aconitate, fluoroacetate, or arsenite (35). Coupled to the citric acid cycle is an electron transfer system to O as shown by inhibition by CO and anaerobiosis. Inhibition by dinitrophenol su ests that oxidative phosphorylation is required, although dinitrophenol may inhibit 5-AL synthetase more directly (36). For AL synthesis, pyridoxal-P is required as shown by Schulman and Richert (37) on vitamin B -dehcient chicks and by inhibitors of pyridoxal-P, e.g., deoxypyridoxine, isonicotinic hydrazide, etc. (35). 

If standard doses of INH (isonicotinic hydrazide, isoniazid) with respect to body weight are administered to a randomly selected population, the plasma concentration of the drug a few hours later will show a bi- or trimodal distribution depending on the precision of the method used for INH determination. The decrease in INH-plasma levels is individually constant Variation is smaUer in identical than in dizygotic twins. All the drug is excreted in the urine as unchanged isoniazid. acetyl isoniazid, isonicotinic add and minor amounts of other metabolites. The percentage of inactive acetyl-INH in urine varies from 14-70% in relation to... 

Human chorionic gonadotropin Hexose diphosphate Human menopausal gonadotropin Hexose monophosphate Interstitial cell-stimulating hormone Inosine diphosphate Inosine monophosphate Isonicotinic hydrazide Isoelectric point Inosine triphosphate a-Ketoglutaric acid (oxoglutarate)... 

Pharmaceuticals. The tuberculostatic dmg isoniazid [54-85-3] (60), the hydrazide of 4-pyridinecarboxyhc acid, was one of the eadiest hydrazine-based dmgs introduced in the United States. It is made by the reaction of hydrazine and an isonicotinic acid ester (219). 

Dipping solution Dissolve 1 g isonicotinic acid hydrazide (4-pyridinecarboxylic acid hydrazide, isoniazide) in 100 ml ethanol and add 500 gl trifluoroacetic acid [1] or 1 ml glacial acetic acid. 

Spray solution Dissolve 0.8 g isonicotinic acid hydrazide in 200 ml methanol and add 1 ml hydrochloric acid (25%) [6] or glacial acetic acid [2]. 

Isonicotinic acid hydrazide forms fluorescent hydrazones with ketosteroids. 

Hydrazides of isonicotinic acid have been used as antidepressant agents by virtue of their monoamine oxidase-inhibiting activity the pyridine ring has been shown to be replaceable by an... 

Therapeutic Function Antitubercular Chemical Name 4-pyridinecarboxylic acid hydrazide Common Name Isonicotinic acid hydrazide Structural Formula ... 

Methyl acrylate, 28.0 g (0.4 mol) was added dropwise during one hour to a solution containing 54.8 g (0.4 mol) of isonicotinic acid hydrazide (isoniazid) and 10 ml of glacial acetic acid in 400 ml of tertiary butyl alcohol. The resulting solution then was heated for 18 hours on a steam bath. Concentration of the reaction mixture to 100 ml yielded 13.0 g of unreacted isonicotinic acid hydrazide. The filtrate was concentrated to a thick syrup which was triturated... 

Diethyidithiocarbamate a,a1-Dipyridyl Diphenylthiocarbazone 8-Hydroxyquinoline Isonicotinic add hydrazide... 

Isonicotinic acid hydrazide reagent 318 Isoprenaiine 395,396 Isoprenoid compounds 44 Isopulegol 59 Isoquercitrin 279, 280, 323 Isoquinoline alkaloids 46, 66, 262 Isorhamnetin 323 Isothiazolones, microbiocidal 45 Isothiocyanates 75 Isotopes, j8-radiation-emitting 41 -, detection limits 41 Itaconic acid 61... 

---