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Acid Hydrazide (acid + hydrazide)
Kinds of Acid Hydrazide Selected AbstractsSynthesis, Stereochemistry and Biological Activity of Some Novel Long Alkyl Chain Substituted Thiazolidin-4-ones and Thiazan-4-one from 10-Undecenoic Acid Hydrazide.CHEMINFORM, Issue 26 2005V. P. Mujeebur Rahman Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis and Antimicrobial Activity of Some New Hydrazones of 4-Fluorobenzoic Acid Hydrazide and 3-Acetyl-2,5-disubstituted-1,3,4-oxadiazolines.CHEMINFORM, Issue 50 2002Sevim Rollas Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis, structure, and antibacterial evaluation of new N -substituted-3-amino- 5-oxo-4-phenyl-2,5-dihydro-1H -pyrazole-1-carbothioamidesHETEROATOM CHEMISTRY, Issue 4 2010Monika Pitucha Novel N -substituted-3-amino-5-oxo-4-phenyl-2,5-dihydro-1H -pyrazole-1-carbothioamide derivatives were synthesized by means of two methods. First is the cyclization reaction of 1-(cyanophenyl)acetyl-4-substituted thiosemicarbazide, and the second one is reaction of cyanophenyl acetic acid hydrazide with isothiocyanate. Structures of new compounds were confirmed by elemental analysis, 1H NMR, and X-ray diffraction analysis. Biological evaluation showed that some of them possess promising antibacterial activities. © 2010 Wiley Periodicals, Inc. Heteroatom Chem 21:215,221, 2010; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20598 [source] Tuberculosis verrucosa cutis: antitubercular therapy, a well-conceived diagnostic criterionINTERNATIONAL JOURNAL OF DERMATOLOGY, Issue 3 2005Virendra N. Sehgal MD A 39-year-old housewife sustained inadvertent trauma to the right index finger about 6 years ago, whilst stitching clothes. A couple of weeks later, the site of trauma became hard and gritty. Ever since, it has progressed slowly, without any appreciable outward sign. It was not associated with any discomfort/pain. Consequent on an opinion from a surgeon, it was decided to operate on the right index finger. During the operation, under local anesthesia, a hard and gritty material was removed. The material was subjected to histopathologic study. Several stitches were applied to the wound. It failed to respond to antimicrobial therapy over a 4-week period, prompting the patient to seek another opinion. Examination of the skin surface revealed a plaque with an irregular configuration on and around the distal interphalangeal joint of the right index finger. It was erythematous and pigmented. The top of the plaque was irregular and had alternating elevations and depressions (Fig. 1). Diascopy was negative for apple jelly nodule. A bacillus Calmette,Guérin (BCG) vaccination scar was identified on the left deltoid. There was no regional lymphadenopathy or systemic abnormality. Mantoux test with intradermal injection of 0.1 mL SPAN's tuberculin (purified protein derivative/5 tuberculin units/0.1 mL) (Span Diagnostic Ltd., Murat, India) was negative after 72 h. Investigations, including total and differential leukocyte count, erythrocyte sedimentation rate, serum biochemistry, and renal and liver function tests, were within the normal range, as was a chest X-ray. Figure 1. Tuberculosis verrucosa cutis before (a) and after (b) antitubercular therapy (ATT) Hematoxylin and eosin-stained sections prepared from the biopsy taken from the lesion revealed noteworthy changes in the epidermis and the dermis. The former was marked by the presence of hyperkeratosis, acanthosis, and papillomatosis, whilst the latter contained tubercle granulomas. Each of the granulomas was well formed and consisted of large numbers of lymphocytes, histiocytes, and foreign body (Langerhans') giant cells (Fig. 2). Caseation necrosis and acid-fast bacilli could not be demonstrated. The preceding revelations were fairly conducive to the diagnosis. Accordingly, antitubercular therapy (ATT), comprising 450 mg of rifampicin, 300 mg of isonicotinic acid hydrazide, and 800 mg of ethambutol, was recommended for oral administration each day for 60 days. The outcome of the treatment was satisfactory, resulting in perceptible regression of the skin lesion (Fig. 1b). The patient was advised to continue the treatment for another 30 days, after which 450 mg of rifampicin and 300 mg of isonicotinic acid hydrazide were to be continued for another 6 months. Figure 2. Tuberculosis verrucosa cutis depicting well-formed tubercle(s) comprising lymphocytes, histiocytes, neutrophils, and a few giant cells (hematoxylin and eosin, × 100) [source] Utilization of 2-benzo[b]furan carboxylic acid hydrazide in the synthesis of 1,3,4-oxadiazole derivativesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 4 2009Yu-Xia Da In this study, the synthesis of series of 2-benzo[b]furan-substituted 1,3,4-oxadiazole derivatives using readily available 2-benzo[b]furan carboxylic acid hydrazide as starting material has been investigated. J. Heterocyclic Chem., (2009). [source] Hydrophobic ion pairing of isoniazid using a prodrug approachJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 6 2002Huiyu Zhou Abstract Inhalation therapy for infectious lung diseases, such as tuberculosis, is currently being explored, with microspheres being used to target alveolar macrophages. One method of drug encapsulation into polymeric microspheres to form hydrophobic ion-paired (HIP) complexes, and then coprecipitate the complex and polymer using supercritical fluid methodology. For the potent antituberculosis drug, isoniazid (isonicotinic acid hydrazide, INH), to be used in this fashion, it was modified into an ionizable form suitable for HIP. The charged prodrug, sodium isoniazid methanesulfonate (Na,INHMS), was then ion paired with hydrophobic cations, such as alkyltrimethylammonium or tetraalkylammonium. The logarithms of the apparent partition coefficients (log P,) of various HIP complexes of INHMS display a roughly linear relationship with the numbers of carbon atoms in the organic counterions. The water solubility of the tetraheptylammonium,INHMS complex is about 220-fold lower than that of Na,INHMS, while the solubility in dichloromethane exceeds 10 mg/mL, which is sufficient for microencapsulation of the drug into poly(lactide) microspheres. The actual logarithm of the dichloromethane/water partition coefficient (log P) for tetraheptylammonium,INHMS is 1.55, compared to a value of ,,1.8 for the sodium salt of INHMS. The dissolution kinetics of the tetraheptylammonium,INHMS complex in 0.9% aqueous solutions of NaCl was also investigated. Dissolution of tetraheptylammonium,INHMS exhibited a first-order time constant of about 0.28 min,1, followed by a slower reverse ion exchange process to form Na,INHMS. The half-life of this HIP complex is on the order of 30 min, making the enhanced transport of the drug across biological barriers possible. This work represents the first use of a prodrug approach to introduce functionality that would allow HIP complex formation for a neutral molecule. © 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:1502,1511, 2002 [source] The emitting species formed by the oxidation of hydrazides with hypohalites or N-halosuccinimidesLUMINESCENCE: THE JOURNAL OF BIOLOGICAL AND CHEMICAL LUMINESCENCE, Issue 4 2004Paul S. Francis Abstract The chemiluminescence accompanying the oxidation of salicylic hydrazide (2-hydroxybenzoic acid hydrazide) with hypochlorite, hypobromite, N-chlorosuccinimide, N-bromosuccinimide or hydrogen peroxide with cobalt(II) matched the photoluminescence emission of salicylic acid. In a related reaction, the oxidation of a mixture of isoniazid and ammonia, a synergistic effect was observed. The chemiluminescence spectrum for this reaction matches that accompanying the oxidation of the hydrazide, rather than the oxidation of ammonia. These results were used to assess mechanisms proposed by previous authors. Copyright © 2004 John Wiley & Sons, Ltd. [source] Synthesis and Antibacterial Activity of a New Series of 3-[3-(Substituted Phenyl)-1-Isonicotinoyl-1H -Pyrazol-5-yl]-2H -Chromen-2-one DerivativesARCHIV DER PHARMAZIE, Issue 6 2009Prashant Aragade Abstract A novel series of 3-[3-(substituted phenyl)-1-isonicotinoyl-1H -pyrazol-5-yl]-2H -chromen-2-one derivatives 4a,k have been synthesized by the reaction of 3-[2,3-dibromo-3-(substituted phenyl) propanoyl]-2H -chromen-2-one 3a,k and isonicotinic acid hydrazide in the presence of triethylamine in absolute ethanol, characterized by spectral data and screened for their in-vitro antibacterial activity against Gram-positive and Gram-negative bacteria. Among the series, compounds 4e, 4i, and 4k displayed an encouraging antibacterial activity profile as compared to the reference drug ampicillin against tested bacterial strains. [source] Immunomodulatory and Anticancer Activities of Some Novel 2-Substituted-6-bromo-3-methylthiazolo[3,2- a]benzimidazole DerivativesARCHIV DER PHARMAZIE, Issue 4 2009Hatem A. Abdel-Aziz Abstract Ethyl 6-bromo-3-methyl-1,3-thiazolo[3,2- a]benzimidazole-2-carboxylate 2 was prepared by the ambient temperature bromination of ethyl 3-methyl-1,3-thiazolo[3,2- a]benzimidazole-2-carboxylate 1. The acid hydrazide 4 was obtained by the reaction of ester 2 with hydrazine hydrate. Treatment of compound 4 with benzaldehyde or 2-thiophenaldehyde yielded the corresponding hydrazones 6a and 6b, respectively, while the reaction of acid hydrazide 4 with ethoxymethylene malononitrile (7a) or with ethyl ethoxymethylene cyanoacetate (7b) in refluxing ethanol afforded pyrazole derivatives 9a and 9b, respectively. Taken together, from the biological investigations compounds 9a and 9b were the most significant inhibitors of LPS-stimulated NO generation from Raw murine macrophage 264.7, and, as another result, compounds 2 and 4 had a weak radical scavenging activity against DPPH radicals. Moreover, 2, 4, and 9a had a concomitant strong cytotoxicity against both colon carcinoma cells (HCT-116) and hepatocellular carcinoma cells (Hep-G2) while 9b showed specific cytotoxicity only against colon carcinoma cells. [source] Liposomes as tools to study drug diffusion and toxin-induced leaksBIOCHEMISTRY AND MOLECULAR BIOLOGY EDUCATION, Issue 2 2002Florence Levillain Multilayered vesicles made of egg-phosphatidylcholine and of phosphatidic acid were used to teach in a 4-h session of practical work with a low cost spectrophotometer how to determine osmolarity inside multilayered vesicles and to show, by using two anti-tuberculous drugs (isonicotinic acid hydrazide, p -aminosalicylate), that a small and non-ionized molecule diffused freely through phospholipid vesicles, whereas a charged one did not. In addition, the permeabilizing effect of melittin, a membrane-targeted bee-venom toxin, was tested. [source] Tricarbonyl Rhenium(I) and Technetium(I) Complexes with Hydrazones Derived from 4,5-Diazafluoren-9-one and 1,10-Phenanthroline-5,6-dioneEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 29 2010Paula Barbazán Abstract Tricarbonylrhenium(I) and -technetium(I) halide (halide = Cl and Br) complexes of ligands derived from 4,5-diazafluoren-9-one (df) and 1,10-phenanthroline-5,6-dione (phen) derivatives of benzoic and 2-hydroxybenzoic acid hydrazides have been prepared. The complexes have been characterized by elemental analysis, MS, IR, 1H NMR and absorption and emission UV/Vis spectroscopic methods. The metal centres (ReI and TcI) are coordinated through the nitrogen imine atoms and establish five-membered chelate rings, whereas the hydrazone groups stand uncoordinated. The 1H NMR spectra suggest the same behaviour in solution on the basis of only marginal variations in the chemical shifts of the hydrazine protons. [source] Synthesis of thiadiazoles, triazoles and oxadiazoles from sulfonyl acetic acids via a common routeJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 1 2005Venkatapuram Padmavathi A new class of five membered heterocycles, thiadiazoles, triazoles and oxadiazoles were prepared from sulfonyl acetic acids via acid hydrazides. [source] Design and Synthesis of 2-Phenoxynicotinic Acid Hydrazides as Anti-inflammatory and Analgesic AgentsARCHIV DER PHARMAZIE, Issue 9 2010Alireza Moradi Abstract A series of 2-phenoxynicotinic acid hydrazides were synthesized and evaluated for their analgesic and anti-inflammatory activities. Several compounds having an unsubstituted phenyl/4-pyridyl or C-4 methoxy substituent on the terminal phenyl ring showed moderate to high analgesic or anti-inflammatory activity in comparison to mefenamic acid as the reference drug. The compounds with highest anti-inflammatory activity were subjected to in vitro COX-1/COX-2 inhibition assays and showed moderate to good COX-1 and weak COX-2 inhibition activities. [source] | ||||||||||