Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols.

Full Abstract

In the present article, we examined the antileishmanial, antimalarial, antibacterial, and antifungal activities of several newly synthesized O-alkylated phloroglucinol compounds (11-19) which are analogues of the naturally occurring antimalarial compound 1. Analogues 12 and 16 exhibited antileishmanial activity against, Leishmania donovani promastigotes with IC(50)s of 5.3 and 4.2microg/mL, respectively. Naturally occurring monomeric formylated acylphloroglucinol compounds, grandinol (2), jensenone (3), and their analogues (29-37), were also synthesized and evaluated for antileishmanial, antimalarial, antibacterial, and antifungal activities. Amongst these, both grandinol and jensenone showed mild to moderate antibacterial, antifungal, and antileishmanial activities. Jensenone (3) was effective against Candida albicans with an IC(50) of 5.5microg/mL but was ineffective against Cryptococcus neoformans and methicillin-resistant Staphylococcus aureus. Among the analogues, 34 was the most active against C. albicans and C. neoformans with IC(50)s of 2.0 and 2.5microg/mL, respectively, and was fungicidal toward Candida albicans.

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Author information

Author/s: Bharate, Sandip B (SB); Khan, Shabana I (SI); Yunus, Nafees A M (NA); Chauthe, Siddheshwar K (SK); Jacob, Melissa R (MR); Tekwani, Babu L (BL); Khan, Ikhlas A (IA); Singh, Inder Pal (IP);

Affiliation: Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S. Nagar, Punjab 160062, India.

Journal and publication information

Publication Type: Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.

Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem), published in England. (Language: eng)

Reference: 2007-Jan; vol 15 (issue 1) : pp 87-96

Dates: Created 2006/11/20; Completed 2007/02/20;

PMID: 17070063, status: MEDLINE (last retrieval date: 12/26/2008)

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MeSH headings (categories)

This article was linked to the MESH Headings shown below.

Animals
Anti-Bacterial Agents - chemical synthesis; chemistry; pharmacology
Antifungal Agents - chemical synthesis; chemistry; pharmacology
Antiprotozoal Agents - chemical synthesis; chemistry; pharmacology
Candida albicans - drug effects
Cell Proliferation - drug effects
Cell Survival - drug effects
Cercopithecus aethiops
Cryptococcus neoformans - drug effects
Epithelial Cells - drug effects

Epithelial Cells - drug effects
Leishmania donovani - drug effects
Microbial Sensitivity Tests
Molecular Structure
Parasitic Sensitivity Tests
Phloroglucinol - analogs & derivatives; chemistry; pharmacology
Staphylococcus aureus - drug effects
Stereoisomerism
Structure-Activity Relationship
Vero Cells

Associated Chemicals: Anti-Bacterial Agents (0) ; Antifungal Agents (0) ; Antiprotozoal Agents (0) ; Phloroglucinol (108-73-6)

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