Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.

A series of 1H-1,2,3-triazolyl piperazino oxazolidinone analogs with optionally varied glycinyl substitutions were synthesized and their antibacterial activity assessed against a panel of susceptible and resistant Gram-positive and selected Gram-negative bacteria including clinical isolates. The N-aroyl- and N-heteroaroyl-glycinyl (MIC: 0.06-4 μg/ml) derivatives were more potent than the N-acylglycinyl (2-8 μg/ml) derivatives against all Gram-positive bacteria tested.

Effects of varied substituents on the antibacterial activity of triazolylmethyl oxazolidinones.

A number of 1,2,3-triazolylmethyl piperazino oxazolidinone derivatives with optionally varied substituents at the 4N-piperazine position were synthesized and their antibacterial activity evaluated against a panel of susceptible and resistant Gram-positive and selected Gram-negative bacteria. Substitution with 5-membered heteroaroyl and dinitrobenzoyl moieties potentiated activity against staphylococci and enterococci strains. Furthermore, the compounds having dinitrobenzoyl 7n, 7o, and 5-nitrofuroyl 7t substitutions were four- to eightfold more potent than linezolid against M.

Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones.

The antibacterial activities of a series of triazolyl oxazolidinones against Mycobacterium tuberculosis strain in vitro and in vivo in a mice model are presented. Most active compounds were noncytotoxic against VERO cells with acceptable selectivity indexes (SI) as measures of compound tolerability. Structure activity relationships (SARs) revealed that analogs with alkylcarbonyl (IC(90): < 0.

The effect of systematic structural modifications on the antibacterial activity of novel oxazolidinones.

A novel series of tetraethylene glycol (TEG) triazolyl and squaramide containing oxazolidinones were synthesized and tested for their antibacterial activity against a selected panel of Gram-positive and Gram-negative bacteria. The 4-TEG-triazolyl derivatives were prepared by 'click reaction'. The introduction of the TEG and squaramide groups did not favor antibacterial activity.

Assessment of the stability of novel antibacterial triazolyl oxazolidinones using a stability-indicating high-performance liquid chromatography method.

Objectives: To evaluate the stability of 12 triazolyl oxazolidinone (TOZ) derivatives in simulated gastric and intestinal fluids as well as in human plasma at 37 ± 1°C.

Materials And Methods: A stability-indicating high-performance liquid chromatography (HPLC) procedure with a C(8) column (250 × 40 mm, 5 μm particle size) and a mobile phase of acetonitrile/H(2)O (50/50 v/v) at 1.0 ml/min was used.

Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.

A series of 5-(4-methyl-1,2,3-triazole)methyl oxazolidinones were synthesized and tested for their antibacterial activity against a panel of Gram-positive and Gram-negative clinical isolates in comparison with linezolid and vancomycin. Most of the compounds demonstrated strong to moderate in vitro antibacterial activity against susceptible and resistant Gram-positive pathogenic bacteria. Antibacterial activity varied with substitutions at the phenyl C4 position with bulky alkylcarbonyl and alkoxycarbonyl substitutions on the piperazine N4 being detrimental to antibacterial activity.