Alcohols antibacterial activity

Namely, allyl alcohol is successively treated with diethylzinc, (R,R) dipropyl tartrate, and 4-methoxybenzohydroximinoyl chloride (163) to afford the enantiomeric isoxazoline alcohol 166, which under the Jones oxidation conditions affords the corresponding carboxylic acid derivative (167). Treatment of compound 167 with hydroxylamine-O-triflate followed by tri-fluoroacetic acid gives rise to the desired enantiomeric 165 in high excess enantiomeric yield. The synthesis of other isosteric analogues of 165 was reported in the same paper. None of the isosteric analogues exhibits LpxC inhibitory and antibacterial activities [103]. 

PHARMACOLOGICAL ACTIVITIES AND CLINICAL TRIALS Antibacterial activity. Alcohol extract of black tea, assayed on Salmonella typhi and Salmonella paratyphi A, was active on all strains of Salmonella paratyphi A, and only 42.19% of Salmonella typhi strains were inhibited hy the extract ". Ffot water extract of the dried entire plant and the tannin fraction, on agar plate, were active on Escherichia coli. Pseudomonas aeruginosa, and Staphylococcus aureus. ... 

Triclosan cannot only be applied as an emulsion, but it also has demonstrated antibacterial and antiinflammatory efficacy in eczema therapy when used as an antiseptic wash.28,30 Likewise, 10% povidone-iodine solution as a disinfectant showed excellent antibacterial activity together with improvement of clinical severity.79 As a 1% solution, chlorhexidine digluconate has shown superior effectiveness to triclosan in vitro, but may be only suitable for therapeutic use in intertriginous areas or as part of wet wrap dressings in the treatment of AD when used as an alcoholic solution.26,80... 

It has been reported that a combination of chlorobutanol and phenylethanol, both at 0.5% w/v concentration, has shown greater antibacterial activity than either compound alone. An advantage of the use of this combination is that chlorobutanol dissolves in the alcohol the resulting liquid can then be dissolved in an aqueous pharmaceutical preparation without the application of heat. 

The first work in this area was the synthesis of lO-oxa-lO-deazaAMT (IV.52), which was reported as early as 1954 by Fairbum and co-workers [107]. The key building block in this synthesis was the a-ketoaldehyde diethyl acetal, (IV.54), which on reaction with 2,4,5,6-tetraaminopyrimidine at pH 3.0 (90 °C for 2 h) and subsequent vigorous treatment with HCl (100 °C, 15 min) afforded the diester (IV.53) in low yield. Compound (IV.54) was prepared from diethyl V-(4-hydroxybenzoyl)-L-glutamate by reaction with 2,3-epoxy-1,1-diethoxypropane followed by oxidation of the resultant secondary alcohol with chromic acid. Alkaline hydrolysis of (IV.53) yielded (IV.52). The product was assumed to be 6- rather than 7-substituted on the basis that the 5-amino group in 2,4,5,6-tetraaminopyrimidine is the most nucleophilic and therefore most likely to react with the keto group in (IV.54). Antibacterial activity against S. faecium was observed. 

The initial selection of adjuvants to crinitol was based largely on the above mentioned structure-activity relationship study. Thus, the hydroxy group at C-9 in crinitol seems to be essential to its antibacterial activity. The allylic C-9 hydroxy group is easily oxidized, a possibility which might detoxify crinitol in bacterial systems. Because crinitol possesses two allylic alcohol groups in its molecule (at C-1 and C-9), we combined it with several antioxidants which have been used as food and cosmetic additives. Thus two natural antioxidants, vitamins C and E, and two synthetic antioxidants, BHA and BHT, were chosen for the experiment. While the synthetic antioxidants exhibited antimicrobial activity against all the test bacteria (30), natural antioxidants did not show any activity up to 800... 

I. Kubo, H. Muroi and A. Kubo, Antibacterial activity of long-chain alcohols against Streptococcus mutans, J. Agric. Food Chem., 41 (1993), 2447-2450. 

Allicin not only shows antibacterial activity, but also antifungal [63], antiprotozoal [87], anti-parasitic [88] and antiviral activities [89]. It has recently been shown to inhibit the ability of Entamoeba histolytica trophozoites to destroy monolayers of baby hamster kidney cells [90]. Cysteine proteinases, an imporatant contributor to amebic virulence, as well as alcohol dehydrogenase, are strongly inhibited by allicin [90]. 

An example of the application of the DARC-PELCO approach is given in eq. 199 (PC = phenol coefficient) [421], which describes the antibacterial activities of linear and branched alcohols (54) however, the result is trivial, because the compounds... 

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