Synthesis and antimycobacterial activity of N′-(aryl-methylene)-N-(pyrazine-2-carbonyl/substituted benzyl)-isonicotinohydrazide

Abstract

A new series of antimycobacterial agents 2a-j, 3a-d, 6b-f,j, and 7b,f was designed, synthesized and evaluated for antimycobacterial activity against different mycobacterium species i.e. M. tuberculosis, M. avium, and M. intracellulare in an agar dilution method. Some of these compounds (2e, 3a-d) were highly potent with in vitro activity against M. tuberculosis H 37 Rv and clinical isolates (sensitive strains), equivalent to that of Isoniazid.

Supported-amine-catalyzed cascade synthesis of spiro-thiazolone-tetrahydrothiophenes: assessing HSA binding activity

“…5 As a consequence, several methods have been reported to synthesize sulfur-containing heterocyclic compounds. 6,7 In 2006, Jørgensen and coworkers introduced a pioneering method, utilizing enamine catalysis, to synthesize functionalized optically active THTs (Scheme 1a). 7 a Guo et al devised a method using Lewis acid catalysis (Scheme 1b).…”

Synthesis of hybrid compounds by benzylation of acylhydrazones with 3,5-di-tert-butyl-4-hydroxybenzyl acetate

“…17 Amides are very weak nucleophiles, and their alkylation is generally performed in the presence of strong bases. 18 The alkylation and acylation of acylhydrazones, in particular, isoniazid hydrazones, in the presence of sodium hydride under prolonged refl ux in toluene were also described 19 (Scheme 2).…”