ABSTRACT. The versatile scaffold, N'-(2-cyanoacetyl)-2-hydroxybenzohydrazide (3) was utilized in the production of new pyridine, chromene and thiazole derivatives as antimicrobial antioxidant agents. synthetic strategy involves treatment precursor 3 with various arylidene-malononitrile 3-aryl-2-cyanoacrylate compounds to furnish substituted pyridines 5 7. interaction salicylaldehyde and/or phen...

Chatterjee (8) and Rees and Waters (~ I ) suggested the value of examination of acid phosphatase activity in experimental and human leprosy. Hence certain we)) known anti mycobacterial agents like isonicotin ic acid hydrazide ( isoniazid, INH ), 2-ethylisothionicotinamide ( E t h ion a m ide , Trescatyl, 1314TH, Thioamid ), 4, 4'-diaminodiph en yl sulfon e ( DDS ), l(p-N,_ dimethylaminophenyl) ...

The interaction of Cu2+ with isonicotinic acid hydrazide (INH) and some of its derivatives has been investigated by means of electron spin resonance, nuclear magnetic resonance, and optical absorption studies. It could be shown that an interaction exists between the metal ions and the hydrazine side chain in addition to the very weak interaction with the ring nitrogen. The results obtained indi...

The stability constants and related thermodynamic functions characterizing the formation of divalent Ni, Cu, Zn, Cd and Hg complexes with oand p-aminobenzoic acid hydrazide were determined potentiometrically at different temperatures. The formations of the complexes are endothermic processes. The formed bonds are mainly electrostatic. Conductometric titration was carried out to determine the st...

Isonicotinic acid hydrazide (INH) is a frontline antituberculosis agent. Once taken up by Mycobacterium tuberculosis, INH requires activation by the catalase-peroxidase KatG, converting INH from its prodrug form into a range of bactericidal reactive species. Here we used 15N-labeled INH together with electron paramagnetic resonance spin trapping techniques to demonstrate that nitric oxide (NO*)...

The 1,3,4-oxadiazole is an aromatic heterocycle valued for its low-lipophilicity in drug development. Substituents at the 2and/or 5-positions can modulate the heterocycle's electronic and hydrogen bondaccepting capability, while exploiting its use as a carbonyl bioisostere. A new approach to 1,3,4oxadiazoles is described wherein a-bromo nitroalkanes are coupled to acyl hydrazides to deliver the...

Activation of the pro-drug isoniazid (INH) as an anti-tubercular drug in Mycobacterium tuberculosis involves its conversion to isonicotinyl-NAD, a reaction that requires the catalase-peroxidase KatG. This report shows that the reaction proceeds in the absence of KatG at a slow rate in a mixture of INH, NAD(+), Mn(2+), and O(2), and that the inclusion of KatG increases the rate by >7 times. Supe...

Following reports on the effectiveness of isonicotinic acid hydrazide in the treatment of tuberculosis,’ a clinical trial was instituted at the San Angel Sanatorium in Mexico City. Beginning in March 1952, a series of 13 hospitalized and 12 ambulatory patients were started on therapy with Rlmifon* and the results evaluated at the end of a 90-day period. The hospitalized patients selected for st...