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Start Over Author "Lolans K" Journal bioorganic medicinal chemistry letters
3 results on '"Lolans K"'

1. Quinazolinone fungal efflux pump inhibitors. Part 3: (N-methyl)piperazine variants and pharmacokinetic optimization.

Author

Watkins WJ, Chong L, Cho A, Hilgenkamp R, Ludwikow M, Garizi N, Iqbal N, Barnard J, Singh R, Madsen D, Lolans K, Lomovskaya O, Oza U, Kumaraswamy P, Blecken A, Bai S, Loury DJ, Griffith DC, and Dudley MN

Subjects
Animals, Antifungal Agents blood, Antifungal Agents chemistry, Antifungal Agents pharmacokinetics, Candida albicans drug effects, Hepatocytes metabolism, Male, Membrane Transport Proteins metabolism, Molecular Structure, Piperazine, Quinazolinones blood, Quinazolinones pharmacokinetics, Rats, Rats, Sprague-Dawley, Structure-Activity Relationship, Antifungal Agents pharmacology, Membrane Transport Proteins drug effects, Piperazines chemistry, Quinazolinones pharmacology, Serum chemistry
Abstract

Further structure-activity relationships of a novel series of fungal efflux pump inhibitors with respect to potentiation of the activity of fluconazole against strains of C. albicans and C. glabrata over-expressing ABC-type efflux pumps are systematically explored. Rat protein binding and pharmacokinetics of selected analogues are reported.

Published
2007
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2. Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivatives.

Author

Watkins WJ, Lemoine RC, Chong L, Cho A, Renau TE, Kuo B, Wong V, Ludwikow M, Garizi N, Iqbal N, Barnard J, Jankowska R, Singh R, Madsen D, Lolans K, Lomovskaya O, Oza U, and Dudley MN

Subjects
Antifungal Agents chemistry, Antifungal Agents pharmacology, Candida enzymology, Candida albicans drug effects, Candida albicans enzymology, Candida glabrata drug effects, Candida glabrata enzymology, Drug Resistance, Fungal, Drug Synergism, Fluconazole chemistry, Fluconazole pharmacology, Fungal Proteins antagonists & inhibitors, Humans, Microbial Sensitivity Tests, Piperazines chemistry, Piperazines pharmacology, Quinazolines chemistry, Quinazolines pharmacology, Stereoisomerism, Structure-Activity Relationship, Antifungal Agents chemical synthesis, Candida drug effects, Membrane Transport Modulators, Membrane Transport Proteins antagonists & inhibitors, Piperazines chemical synthesis, Quinazolines chemical synthesis
Abstract

Structure-activity relationships of a novel series of fungal efflux pump inhibitors with respect to potentiation of the activity of fluconazole against strains of Candida albicans and Candida glabrata over-expressing ABC-type efflux pumps are systematically explored.

Published
2004
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3. Quinazolinone-based fungal efflux pump inhibitors. Part 1: Discovery of an (N-methylpiperazine)-containing derivative with activity in clinically relevant Candida spp.

Author

Lemoine RC, Glinka TW, Watkins WJ, Cho A, Yang J, Iqbal N, Singh R, Madsen D, Lolans K, Lomovskaya O, Oza U, and Dudley MN

Subjects
Antifungal Agents pharmacology, Candida enzymology, Drug Resistance, Fungal, Drug Synergism, Fluconazole chemistry, Fluconazole pharmacology, Humans, In Vitro Techniques, Models, Molecular, Piperazines chemistry, Piperazines pharmacology, Quinazolines chemistry, Quinazolines pharmacology, Solubility, Stereoisomerism, Structure-Activity Relationship, ATP-Binding Cassette Transporters antagonists & inhibitors, Antifungal Agents chemical synthesis, Candida drug effects, Fungal Proteins antagonists & inhibitors, Membrane Transport Modulators, Membrane Transport Proteins antagonists & inhibitors, Piperazines chemical synthesis, Quinazolines chemical synthesis
Abstract

The discovery of a series of quinazolinone-based fungal efflux pump inhibitors by high-throughput screening for potentiation of fluconazole in C. albicans is described. Attempts to improve the aqueous solubility of screening hits led to the discovery of an analog with greatly improved physical properties and activity against clinically-relevant Candida spp.

Published
2004
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