Synthesis and Antimicrobial Activity of N-[2-(aryl/substituted aryl)-4-oxo-1,3-thiazolidin-3-yl]pyridine-4-carboxamide

Abstract

ABSTRACT. A series of isonicotinyl hydrazones and their 4-thiazolidinones have been synthesized by condensation of isonicotinic acid hydrazide with various aromatic aldehydes to yield Schiff's bases, followed by the cyclocondensation of Schiff's bases with 2-mercaptoacetic acid to yield their 4-thiazolidinones. The synthesized compounds have been characterized by their elemental, analytical and spectral studies. All these compounds were evaluated for their invitro antimicrobial activity against a spectrum of non-resistant and resistant microbial organisms. These studies proved that compounds 5e,i against B. subtilis; 5e,f,h against B. anthracis; 5g,i against S. aureus showed good activity at lower concentrations. Compounds 5d-5i displayed significant activity against resistant strain of K. pneumonia with minimum inhibitory potency in the concentration range of 2-16 ug/ml.

Design and Synthesis of Arylthiophene-2-Carbaldehydes via Suzuki-Miyaura Reactions and Their Biological Evaluation

“…Compound 2d showed outstanding inhibition against Pseudomonas aeruginosa, with an IC 50 value 29.7 µg/mL, whereas compounds 2a-c, 2e-f, 2h-j exhibited mild to average activity against Pseudomonas aeruginosa. From the screening data, it was observed that electron withdrawing and donating groups on the aryl ring had a substantial influence on the antibacterial activities, confirming earlier reports that on the antibacterial activity of various aryl thiophene derivatives bearing electron donating and electron withdrawing groups [14,16,22]. It was previously claimed that the antibacterial activity of compounds containing electron withdrawing groups was more potent against Gram-negative bacteria.…”

“…Palladium-catalyzed functionalizations of thiophene derivatives have great importance due to the functional group compatibility, relative strength, low toxicity, and greater versatility of organopalladium complexes. Iqbal et al [14], Al-Adiwish et al [15], and Thomas et al [16] reported that the arylthiophene derivatives bearing electron withdrawing substituents showed excellent antibacterial activity against Gram-negative bacteria. Furthermore, Sigmundova et al [17] reported that arylthiophene derivatives with electron donating substituents exhibited potent antibacterial activity against Gram-positive bacteria.…”

Synthesis and antifungal activities of novel nicotinamide derivatives containing 1,3,4-oxadiazole

“…Nicotinamide derivatives, an important class of heterocyclic derivative, has attracted more and more attention in the field of pesticide due to their fungicidal activity [3-5], insecticidal activity [6-9], herbicidal activity [8,10], plant growth regulator activity [11], and bactericidal activity [12-15]. In fungicidal activity regard, some nicotinamide derivatives have been developed and commercialized, an example of such a fungicide is boscalid (Figure 1), which was discovered by BASF and registered in Britain, Germany, and Switzerland in 2004 [16].…”

An Improved Method for the Quaternization of Nicotinamide and Antifungal Activities of Its Derivatives

“…Nicotinamide is a water-soluble B complex vitamin which is naturally present in animal products, whole cereals and legumes [1]. Derivatives of nicotinamide have attracted much attention because of their antimicrobial [2,3,4,5,6], fungicidal [7,8,9,10,11], insecticidal [12,13] and herbicidal activity [14,15,16], plant growth regulator activity [17], cytotoxic properties [18,19], and antiangiogenesis activity [20]. Some nicotinamide derivatives, like boscalid, are used as commercial antifungicides (Figure 1).…”