Document Detail

Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities.
MedLine Citation:
PMID:  23534411     Owner:  NLM     Status:  MEDLINE    
Fifty analogues of batzelladine K were synthesized and evaluated for in vitro antimalarial (Plasmodium falciparum), antileishmanial (Leishmania donovani), antimicrobial (panel of bacteria and fungi), antiviral (HIV-1) activities. Analogues 14h and 20l exhibited potential antimalarial activity against chloroquine-sensitive D6 strain with IC(50) 1.25 and 0.88 μM and chloroquine-resistant W2 strain with IC(50) 1.64 and 1.07 μM, respectively. Analogues 12c and 14c having nonyl substitution showed the most potent antileishmanial activity with IC(50) 2.39 and 2.78 μM and IC(90) 11.27 and 12.76 μM, respectively. Three analogues 12c, 14c, and 14i were the most active against various pathogenic bacteria and fungi with IC(50) < 3.02 μM and MIC/MBC/MFC <6 μM. Analogue 20l having pentyl and methyl substituents on tricycle showed promising activities against all pathogens. However, none was found active against HIV-1. Our study demonstrated that the tricyclic guanidine compounds provide new structural class for broad spectrum activity.
Nafees Ahmed; Keyur G Brahmbhatt; Shabana I Khan; Melissa Jacob; Babu L Tekwani; Sudeep Sabde; Debashis Mitra; Inder P Singh; Ikhlas A Khan; Kamlesh K Bhutani
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.    
Journal Detail:
Title:  Chemical biology & drug design     Volume:  81     ISSN:  1747-0285     ISO Abbreviation:  Chem Biol Drug Des     Publication Date:  2013 Apr 
Date Detail:
Created Date:  2013-03-28     Completed Date:  2013-09-24     Revised Date:  2014-04-02    
Medline Journal Info:
Nlm Unique ID:  101262549     Medline TA:  Chem Biol Drug Des     Country:  England    
Other Details:
Languages:  eng     Pagination:  491-8     Citation Subset:  IM    
Copyright Information:
© 2012 John Wiley & Sons A/S.
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MeSH Terms
Anti-Bacterial Agents / chemical synthesis*,  chemistry,  pharmacology
Anti-HIV Agents / chemical synthesis*,  chemistry,  toxicity
Antifungal Agents / chemical synthesis*,  chemistry,  pharmacology
Antimalarials / chemical synthesis*,  chemistry,  pharmacology
Aspergillus fumigatus / drug effects
Candida / drug effects
Cell Survival / drug effects
Cercopithecus aethiops
Cryptococcus neoformans / drug effects
Guanidine / chemistry*,  pharmacology,  toxicity
Guanidines / chemical synthesis*,  pharmacology,  toxicity
HIV-1 / drug effects
Leishmania donovani / drug effects
Microbial Sensitivity Tests
Plasmodium falciparum / drug effects
Structure-Activity Relationship
Vero Cells
Grant Support
Reg. No./Substance:
0/Anti-Bacterial Agents; 0/Anti-HIV Agents; 0/Antifungal Agents; 0/Antimalarials; 0/Guanidines; 0/batzelladine K; JU58VJ6Y3B/Guanidine

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