Quinazoline derivatives with antitubercular activity

Possible inhibition of hydroxy methyl glutaryl CoA reductase activity by nicotinic acid and ergosterol: as targeting for hypocholesterolemic action

“…The lowering of LDL-C was higher and is feasible as a range of food products are commercially available for consumption. LDL-c lowering effect contributes to beneficial effects in reducing the risk of cardiovascular diseases 14 . The decrease in the LDL-c level due to consumption of plant stanols in high doses (about 9 g) is of similar magnitude to that achieved by drugs lowering cholesterol via partly blocking cholesterol absorption 15 .…”

2-Alkyl(aryl)-quinazolin-4(3H)-thiones, 2-R-(quinazolin-4(3H)-ylthio)carboxylic acids and amides: synthesis, molecular docking, antimicrobial and anticancer properties

“…Alkylation of 2-R-quinazolin-4(3H)-thiones (1.2) by the halogenoalkanes in an alkaline medium with the presence of tetrabutylammonium bromide leads to the corresponding S-derivatives (1.4) (Scheme 1) 23 . When isothiocyanates were used as electrophiles to react with ortho-bromophenyl isocyanides (1.5), appropriate cyclic 2-Rquinazolin-4(3H)-thiones (1.7) were formed in high yields (Scheme 2) 24 .…”

“…Given the constant and increasing threat of drug resistance, we were particularly interested in antimicrobial properties of quinazoline-4(3H)-thione's derivatives. It was found that 4-(S-butylthio)quinazoline was more active than isoniazide, against atypical strains of mycobacteria, when investigated for antitubercular activity against Mycobacterium tuberculosis, M. kansasii, M. fortuitum, M. avium and M. intracellulare 8 . The 4-ethylthio-6-fluoroquinazoline had potent antifungal activities against practically all the tested fungi (Gibberella zeae, Fusarium oxysporum, Cardamine mandshurica, Rhizoctonia solani, Thanatephorus cucumeris, Phytophthora infestans, Sclerotinia sclerotiorum, Botrytis cinerea, Colletotrichum gloeosporioides) and showed a broad-spectrum bioactivity 9 .…”

Synthesis and Antimicrobial Evaluation of Some Tricyclic Substituted benzo[h]quinazolines, benzo[h]quinolines and naphthaleno[d]thiazoles

“…Quinazoline nucleus is one of fused heterocyclic ring systems that possesses a wide array of biological activities. These pharmacological activities include DNA binding 4 , antitumor [5][6][7] , benzodiazepine and GABA receptor ligand activity 8 , antiviral 9,10 , antibacterial 11 , antituberculosis 12,13 and cellular phosphorylation and tyrosine kinase inhibition 14 . Many marketed drugs comprise quinazoline nucleus in their structures such as; , treatment of lupus 25 , treatment of neurodegenerative diseases 26 , antitubercular 27,28 , antiprotozoal 29,30 and anticancer 31,32 .…”