908563-71-3Relevant academic research and scientific papers
Synthesis, antimicrobial evaluation, and molecular docking studies of novel chromone based 1,2,3-triazoles
Dofe, Vidya S.,Sarkate, Aniket P.,Lokwani, Deepak K.,Kathwate, Santosh H.,Gill, Charansingh H.
, p. 15 - 28 (2017)
Abstract: In Search of novel antimicrobial agents with improved potency, we designed and synthesized a series of 3-((1-benzyl-1H-1,2,3-triazol-4-yl)methoxy)-2-(4-fluorophenyl)-4H-chromen-4-ones 5a–f using click chemistry. The structures of synthesized com
Functionalization of the chalcone scaffold for the discovery of novel lead compounds targeting fungal infections
Bonvicini, Francesca,Gentilomi, Giovanna A.,Bressan, Francesca,Gobbi, Silvia,Rampa, Angela,Bisi, Alessandra,Belluti, Federica
, (2019/02/01)
The occurrence of invasive fungal infections represents a substantial threat to human health that is particularly serious in immunocompromised patients. The limited number of antifungal agents, devoid of unwanted toxic effects, has resulted in an increased demand for new drugs. Herein, the chalcone framework was functionalized to develop new antifungal agents able to interfere with cell growth and with the infection process. Thus, a small library of chalcone-based analogues was evaluated in vitro against C. albicans ATCC 10231 and a number of compounds strongly inhibited yeast growth at non-cytotoxic concentrations. Among these, 5 and 7 interfered with the expression of two key virulence factors in C. albicans pathogenesis, namely, hyphae and biofilm formation, while 28 emerged as a potent and broad spectrum antifungal agent, enabling the inhibition of the tested Candida spp. and non-Candida species. Indeed, these compounds combine two modes of action by selectively interfering with growth and, as an added value, weakening microbial virulence. Overall, these compounds could be regarded as promising antifungal candidates worthy of deeper investigation. They also provide a chemical platform through which to perform an optimization process, addressed at improving potency and correcting liabilities.
Ultrasound-assisted synthesis and antimicrobial activity of tetrazole-based pyrazole and pyrimidine derivatives
Dofe, Vidya S.,Sarkate, Aniket P.,Shaikh, Zarina M.,Gill, Charansingh H.
, p. 59 - 65 (2018/01/18)
New tetrazole-based pyrazole and pyrimidine derivatives were synthesized by an ultrasound irradiation method. All compounds were characterized by infrared spectroscopy (IR), 1H nuclear magnetic resonance (NMR), 13C NMR, mass spectrometry (MS) and elemental analysis and assessed in vitro for their efficacy as antimicrobial agents against four bacteria (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa) and two fungi (Candida albicans, Aspergillus Niger). Compounds 8a, 8e, 9a, 9b and 9e show potent activity against the tested strains compared to the reference drugs chloramphenicol and clotrimazole.
Synthesis of chromones and pyrazolines as antimicrobial & antifungal agents
Ghotekar,Mandhane,Joshi,Bhagat,Gill
experimental part, p. 341 - 344 (2012/01/02)
A series of chromones and pyrazolines have been synthesized and evaluated for their antimicrobial and antifungal activity against Gram+ve and Gram-ve microorganisms. 2-Hydroxy acetophenone on treatment with substituted aldehydes gave the corresponding cha
A two step synthesis of BzR/GABAergic active flavones via a Wacker-related oxidation
Lorenz, Michael,Shahjahan Kabir,Cook, James M.
experimental part, p. 1095 - 1098 (2010/04/05)
A general route for the synthesis of biologically important flavones is reported via a two step sequence employing a catalytic Wacker-Cook oxidation4b as the key step.
Synthesis of some biologically important fluorinated 3-chlorochromones and 1,5 - Benzothiazepines as antimicrobial and antifungal agents
Ghotekarab,Joshia,Mandhane,Bhagata,Gill
scheme or table, p. 1267 - 1270 (2010/12/25)
A series of synthetic 3-chlorochromones and 1,5-benzo-thiazepines have been synthesized and evaluated for their antimicrobial and antifungal activity against Gram +ve and Gram -ve microorganisms. In these series the chemical transformation of chalcones to
