Heterocyclic isosters of antimycobacterial salicylanilides.

A series of 64 derivatives of substituted heterocyclic analogues of salicylanilides was synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii. For the QSAR study, the combination of Free-Wilson approach with Hansch approach was used.

Antimycobacterial N-pyridinylsalicylamides, isosters of salicylamides.

The series of derivatives of substituted N-pyridinylsalicylamides were synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium avium and two strains of Mycobacterium kansasii. In the quantitative structure activity relationships analysis (QSAR), the Free-Wilson and Hansch approaches were used but the analysis was not significant.

A new group of potential antituberculotics: hydrochlorides of piperidinylalkyl esters of alkoxy-substituted phenylcarbamic acids.

A group of 31 of alkoxy-substituted phenylcarbamic acids with the alkoxy group in ortho, meta or para position, and methyl or ethoxymethyl attached to the ethylene moiety in position 1, including both basic ethyl esters and derivatives branched on ethylene, were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, M. kansasii, and M. avium.

[Advances in the development of antitubercular agents containing no heterocyclic compounds in the pharmacophore. Part 2. Other derivatives except carboxylic acids].

This paper is the 21st communication in the series of review papers on the development of antituberculotics and the 10th communication summarizing the papers on the development of antituberculotics in recent 15 years. The first seven communications were devoted to heterocyclic compounds, the eighth one to the compounds containing an alkylsulfanyl group in the pharmacophore. The present paper sums up information concerning the compounds not containing a heterocycle in the pharmacophore which are not derivatives of carboxylic acids either.

Antimycobacterial activity of piperidinylpropyl esters of alkoxy-substituted phenylcarbamic acids.

A series of 17 hydrochlorides of piperidinylpropyl esters of alkoxy-substituted phenylcarbamic acids with the alkoxy group in position 2, 3 or 4 on the phenyl ring, and basic substituents attached to the moiety in position 3, were evaluated for in vitro antimycobacterial activity against the strains of Mycobacterium tuberculosis, M. kansasii and M. avium.