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

Synthesis, Anticancer, and QSAR Studies of 2‐Alkyl(aryl,hetaryl)quinazolin‐4(3H)‐thione's and [1,2,4]Triazolo[1,5‐c]quinazoline‐2‐thione's Thioderivatives

“…Among the main aims of this article was SAR analysis of anticancer activity of the quinazolin‐4(3 H )‐thione's and [1,2,4]triazolo[1,5‐ c ]quinazoline‐2‐thione's S‐ derivatives ( 1 – 44 ). Thus, summary of the already reported and several novel substances’ synthetic routs were selected and presented in this article below (Scheme) .…”

“…Substances 1 and 2 were obtained by treatment of the quinazoline‐4(3 H )‐one ( L ) with 2,4‐bis(4‐methoxyphenyl)‐1,3‐dithia‐2,4‐diphosphatane‐2,4‐disulfide ( Lawesson 's reagent) or P 2 S 5 in dioxane (Scheme) . The corresponding substituted 3 – 24 were obtained by alkylation of 1 by proper halogen derivatives in MeOH with an equivalent amount of MeOK .…”

“…Starting substances ( L , M , N ), 1 – 5 , 7 – 12 , 15 , 16 , 19 – 24 , 43 , 44 , 25 – 37 , 42 , and 40 , 41 were already synthesized and reported. Other starting materials and solvents were obtained from commercially available sources and used without additional purification.…”

Synthesis and Antibacterial Evaluation of New developed 2,3-Dihydroquinazolin-4(1H)-ones

“…Antibacterial activity of quinazolinones is demonstrated via various mechanisms as PBP inhibitors [8], DNA inhibition [9], Mur A inhibitors [10], inhibition of tubulin polymerization [11] and DNA gyrase inhibitors [12]. Also 2,3 disubstituted quinazolinones have been evaluated as new antibacterial agents in many literatures [13][14][15][16] . Substitution at position-2 with either methyl, phenyl or even unsubstituted (I) was found to be favoured for antibacterial activity [14].…”

Application of Azide-Tetrazole Tautomerism and Arylsulfanyl Group Dance in the Synthesis of Thiosubstituted Tetrazoloquinazolines

“…The importance of thioquinazoline derivatives has increased lately. Potential antibacterial, 10,11 antimicrobial, 12 antiviral, 13 antitumor, [14][15][16][17] bronchodilatory 18 activity, and monoamine oxidase inhibitor activity, 19 which is important for the treatment of Parkinson's disease were found among 2-substituted 4(3H)-quinazoline-4-thiones, substituted 2-thioquinazolin-4-one analogues, and unsubstituted or 2-substituted 4-thioquinazolines. Compounds from the 4-thioquinazoline series are also known as agriculture antimicrobials.…”