Investigation of Antimicrobial Activities of Indole-3-Aldehyde Hydrazide/Hydrazone Derivatives

Abstract

Background: Indoles and hydrazone-type compounds constitute an important class of compounds for new drug development in order to discover an effective compound against multi-drug-resistant microbial infections. Methods: A series of indole-3-aldehyde and 5-bromoindole-3-aldehyde hydrazide and hydrazones was evaluated for their in vitro antimicrobial activities using the 2-fold serial dilution technique against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Escherichia coli, Bacillus subtilis and Candida albicans. The minimum inhibitory concentration (MIC) was determined for test compounds and for the reference standards sultamicillin, ampicillin, fluconazole and ciprofloxacin. Results: Compounds possessed a broad spectrum of activity having MIC values of 6.25–100 mg/ml against the tested microorganisms. Compounds 1a–1j, in particular, displayed better activity against MSRA and significant activity against S. aureus relative to ampicillin. Unexpectedly, indole nicotinic acid hydrazides showed no significant activity while indole anisic acid hydrazides displayed better activity. Conclusion: The results may be instructive to researchers attempting to gain more understanding of the antimicrobial activity of indole hydrazide/hydrazone-type compounds.

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“…Gurkok et al [82] investigated antimicrobial activities of Indole-3-Aldehyde hydrazide/hydrazone derivatives (26) and (27). Küçükgüzel et al [84] synthesized diflunisal hydrazide-hydrazone derivatives.…”

Indoles as anticancer agents

“…They are a very important category of compounds that play a key role in cell physiology and are probable intermediates for numerous biological reactions. Indole derivatives correspond to scores of important modules of therapeutic agents in medicinal chemistry such as anti-cancer [22] , anti-oxidant [23] , anti-rheumatoidal [24] , anti-HIV [25,26] , anti-microbial [27][28][29] , anti-inflamatory [30] , analgesic [31] , antipyretic [32] , anti-convulsant [33,34] , anthelmintic cardiovascular [35] , selective COX-2(cyclooxygenase-2) inhibitory activities [36][37][38][39] (which is an enzyme accountable for inflammation and pain) and DNA binding ability [40] . Furthermore, countless essential indole derivatives are used in disease management, for example, the non-steroidal anti-inflammatory drug indomethacin (Indocin ® ), the beta blocker pindolol (Viskin ® ) for management of high blood pressure (hypertension), the psychedelic, dimethyltryptamine (DMT) [41] and…”

Synthesis and Antitumor Evaluation of Novel 5-Bromo Indole-Aryl Keto Hydrazide-Hydrazone Analogues

“…Previously indole-hydrazide-hydrazone derivatives shows antimicrobial [11][12][13][14][15][16][17], antifungal [18], anticonvulsant [19], anti-inflammatory, antiplatelet [20][21][22][23][24] and antituberculosis activities [25][26][27][28]. But these series of indole fused aryl aldehydes analogues shows potent antitumor [29][30][31][32][33] activity on anticancer [34][35][36] human cell lines.…”