Novel chalcones and 1,3,5‐triphenyl‐2‐pyrazoline derivatives as antibacterial agents

Abstract

The authors Ponnurengam Malliappan Sivakumar, Suresh Ganesan and Prabhawathi Veluchamy wishes to dedicate this work to their guide Prof MD on the occassion of his birthdayNovel sixteen chalcones and thirteen 1,3,5-triphenyl-2-pyrazolines were synthesized and characterized using FT-IR, HR-Mass, NMR ( C CoSY) and XRD. These compounds were evaluated for their antibacterial activity against six micro-organisms, namely Bacillus subtilis NCIM 2718, Staphylococcus aureus NCIM 5021, Salmonella typhi NCIM 2501, Enterobacter aerogenes NCIM 5139, Pseudomonas aeruginosa NCIM 5029, and Proteus vulgaris NCIM 2813 by twofold dilution method using resazurin as the indicator dye. In the case of chalcones, compounds with hydroxyl and bromo substitutions in the B-ring favor activity and benzyloxy substitution irrespective of its position in the A-ring. In the case of 1,3,5-triphenyl-2-pyrazolines, chloro substitution in the A-ring favors activity. Hydrophilic ⁄ lipophilic balance of the compounds plays a major role in their antibacterial activity.

Licochalcone A exerts antitumor activity in bladder cancer cell lines and mice models

“…It was observed that licochalcone A suppressed the growth of all the three tested bladder cancer cell lines in a dose-dependent manner (Figure 1). ERK 1/2 has been reported to be involved in drug resistance [11][12][13][14][15][16][17]. …”

“…They exhibit anti-inflammatory [9], anti-invasive [10], anti-tumour [11] and antibacterial [12] properties. Chalcone treatment causes induction of apoptosis and alters mitochondrial membrane potential in various types of cancers [13].…”

Ultrasonics Promoted Synthesis of 5-(Pyrazol-4-yl)-4,5-Dihydropyrazoles Derivatives

“…Cyclization of chalcones, leading to pyridine, pyrimidine and pyrazoline derivatives, has been a developing field within the realm of heterocyclic chemistry for the past several years, because of their ready accessibility and the broad spectrum of biological activity of the products [38][39][40][41][42][43][44]. These observations led us to synthesize chalcones and its corresponding pyrazoline, exploring simple procedures.…”

Chalcones: A Solubility Study at Different Temperatures

“…Many of these have been used as important intermediates in organic synthesis [1,2]. The compounds with the backbone of chalcones have been reported to possess various biological activities such as antimicrobial [3][4][5], antiinflammatory [6,7], antifungal [8,9], antioxidant [10,11], antileishmanial [12], antimalarial [13,14], antituberculosis [15,16], analgesic [17], anti HIV [18], antioxidant [19], antitumor [20,21] and neuro protective [22] activities.…”