BIOMAT Database Logo BIOMAT Database Logo

Synthesis of new chalcone derivatives containing acridinyl moiety with potential antimalarial activity. 2010

V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee-247667, Uttarakhand, India.

A series of novel chalcones bearing acridine moiety attached to the amino group in their ring A have been synthesized through noncatalyzed nucleophilic aromatic substitution reaction between various 3'-aminochalcone or 4'-aminochalcones and 9-chloroacridine. The synthesized chalcone derivatives have been characterized and screened for in vitro antimalarial activity against Plasmodium falciparum NF-54. All the chalcones showed complete inhibition at concentration of 10 microg/mL and above while three compounds showed significant inhibition at concentration of 2 microg/mL. The three most active chalcone derivatives were screened for in vivo activity as well, but no significant inhibition in parasitaemia was observed when given intraperitoneally to Plasmodium yoelii infected mice model.

UI MeSH Term Description Entries
D008297 Male Males
D010961 Plasmodium A genus of protozoa that comprise the malaria parasites of mammals. Four species infect humans (although occasional infections with primate malarias may occur). These are PLASMODIUM FALCIPARUM; PLASMODIUM MALARIAE; PLASMODIUM OVALE, and PLASMODIUM VIVAX. Species causing infection in vertebrates other than man include: PLASMODIUM BERGHEI; PLASMODIUM CHABAUDI; P. vinckei, and PLASMODIUM YOELII in rodents; P. brasilianum, PLASMODIUM CYNOMOLGI; and PLASMODIUM KNOWLESI in monkeys; and PLASMODIUM GALLINACEUM in chickens. Plasmodiums
D002599 Chalcone An aromatic KETONE that forms the core molecule of CHALCONES. Benzalacetophenone,Benzylideneacetophenone,1,3-Diphenyl-2-Propen-1-One,Chalkone,1,3 Diphenyl 2 Propen 1 One
D004912 Erythrocytes Red blood cells. Mature erythrocytes are non-nucleated, biconcave disks containing HEMOGLOBIN whose function is to transport OXYGEN. Blood Cells, Red,Blood Corpuscles, Red,Red Blood Cells,Red Blood Corpuscles,Blood Cell, Red,Blood Corpuscle, Red,Erythrocyte,Red Blood Cell,Red Blood Corpuscle
D005260 Female Females
D000166 Acridines Compounds that include the structure of acridine. Acridine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000962 Antimalarials Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585) Anti-Malarial,Antimalarial,Antimalarial Agent,Antimalarial Drug,Anti-Malarials,Antimalarial Agents,Antimalarial Drugs,Agent, Antimalarial,Agents, Antimalarial,Anti Malarial,Anti Malarials,Drug, Antimalarial,Drugs, Antimalarial
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

Related Publications

V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Synthesis of new chalcone derivatives containing a rhodanine-3-acetic acid moiety with potential anti-bacterial activity.
December 2010, European journal of medicinal chemistry,
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Synthesis and antimalarial activity of sulfonamide chalcone derivatives.
April 2005, Farmaco (Societa chimica italiana : 1989),
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Design, Synthesis, and Biological Activity of Novel Chalcone Derivatives Containing an 1,2,4-Oxadiazole Moiety.
January 2022, Frontiers in chemistry,
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.
May 2005, Journal of medicinal chemistry,
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Synthesis, Antiviral Bioactivity of Novel 4-Thioquinazoline Derivatives Containing Chalcone Moiety.
June 2015, Molecules (Basel, Switzerland),
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
New Chalcone Derivatives Containing 2,4-Dichlorobenzenesulfonamide Moiety with Anticancer and Antioxidant Properties.
December 2023, International journal of molecular sciences,
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Pharmacokinetic evaluation of Chalcone derivatives with antimalarial activity in New Zealand White Rabbits.
July 2021, BMC research notes,
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Design and Synthesis of New Phthalazinone Derivatives Containing Benzyl Moiety with Anticipated Antitumor Activity.
January 2016, Biological & pharmaceutical bulletin,
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Synthesis, characterization, electrochemical studies and antitumor activity of some new chalcone analogues containing ferrocenyl pyrazole moiety.
February 2010, Bioorganic chemistry,
V Tomar, and G Bhattacharjee, and Kamaluddin, and S Rajakumar, and Kumkum Srivastava, and S K Puri
Synthesis and Antifungal Activity of Chalcone Derivatives Containing 1,3,4-thiadiazole.
May 2024, Chemistry & biodiversity,
Copied contents to your clipboard!