Synthesis of some new 4(3 H)-quinazolinone-2-carboxaldehyde thiosemicarbazones and their metal complexes and a study on their anticonvulsant, analgesic, cytotoxic and antimicrobial activities – Part-1

• Published in: European journal of medicinal chemistry Vol. 45; no. 8; pp. 3365 - 3373
• Main Authors: Aly, Mohsen M., Mohamed, Yahia A., El-Bayouki, Khairy A.M., Basyouni, Wahid M., Abbas, Samir Y.
• Format: Journal Article
• Language: English
• Published: PARIS Elsevier Masson SAS 01.08.2010; Elsevier
• Subjects: 4(3 H)-Quinazolinones-2-carboxaldehyde; Analgesic; Analgesics; Analgesics - chemical synthesis; Analgesics - chemistry; Analgesics - pharmacology; Analgesics - therapeutic use; Animals; Anti-Infective Agents - chemical synthesis; Anti-Infective Agents - chemistry; Anti-Infective Agents - pharmacology; Anti-Infective Agents - therapeutic use; Antibiotics. Antiinfectious agents. Antiparasitic agents; Anticonvulsant; Anticonvulsants - chemical synthesis; Anticonvulsants - chemistry; Anticonvulsants - pharmacology; Anticonvulsants - therapeutic use; Anticonvulsants. Antiepileptics. Antiparkinson agents; Antineoplastic agents; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Bacteria - drug effects; Biological and medical sciences; Cell Line, Tumor; Chemistry, Medicinal; Cytotoxic and antimicrobial activities; Female; Fungi - drug effects; General aspects; Lethal Dose 50; Life Sciences & Biomedicine; Medical sciences; Mice; Microbial Sensitivity Tests; Neuropharmacology; Organometallic Compounds - chemical synthesis; Organometallic Compounds - chemistry; Organometallic Compounds - pharmacology; Organometallic Compounds - therapeutic use; Pentylenetetrazole - pharmacology; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Rats; Science & Technology; Seizures - chemically induced; Seizures - drug therapy; Thiosemicarbazones; Thiosemicarbazones - chemical synthesis; Thiosemicarbazones - chemistry; Thiosemicarbazones - pharmacology; Thiosemicarbazones - therapeutic use; 4(3 H)-Quinazolinones-2-carboxaldehyde; Anticonvulsant; Analgesic; Cytotoxic and antimicrobial activities; Thiosemicarbazones; ACID; COPPER(II); CRYSTAL-STRUCTURES; 4(3H)-Quinazolinones-2-carboxaldehyde; ZINC(II); ANTITUMOR-ACTIVITY; AGENTS; ANTIFUNGAL; INHIBITORS; DERIVATIVES; Antineoplastic agent; Divalent metal Complexes; Intraperitoneal administration; Zinc II Complexes; Rat; Toxicity; Cytotoxicity; Iodine Organic compounds; Antimicrobial agent; Antifungal agent; Structure activity relation; Copper II Complexes; Chloro complex; Mammary gland; Chemical synthesis; Tumor cell; Thiosemicarbazone; Rodentia; Benzene derivatives; Organic ligand; Transition metal Complexes; Vertebrata; Mammalia; Cell line; Mouse; Animal; Fluorine Organic compounds; Antibacterial agent
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2010.04.020

Novel 3-aryl-4(3 H)-quinazolinone-2-carboxaldehydes, their corresponding Schiff’s base and thiosemicarbazone derivatives were synthesized from the starting 5-iodo anthranilic acid. Copper(II), zinc(II) complexes of some thiosemicarbazone derivatives were also synthesized and characterized. Screening for some selected compounds was carried out to probe their potential anticonvulsant, analgesic, cytotoxic as well as their antimicrobial activities. [Display omitted]