Synthesis of Some Antibacterial Compounds from 4‐Hydroxycoumarin.

Abstract

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Quinolin-6-Amines: Synthesis and Biological Evaluation

“…Biological evaluation results revealed that 2-{(chloromethoxy)methyl}thio-N-(4-methoxyphenyl) [1,2,4] triazolo[1,5-a]quinolin-6-amine i.e. 4f displayed significant biological activity.…”

“…4f displayed significant biological activity. Screening data explored that 2-{(chloromethoxy)methyl}thio-N-(4-methoxyphenyl) [1,2,4]triazolo[1,5-a]quinolin-6-amine showed broad antibacterial as well as antifungal spectrum in comparison to used standard drugs.…”

“…2-{(chloromethoxy)methyl}thio-N-(4-aminophenyl) [1,2,4]triazolo [1,5-a]quinolin-6-amine also showed moderate insecticidal as well as anthelmintic activity. On the basis of SAR, it is elicited that 2-{(chloromethoxy)methyl}thio-N-(4-methoxyphenyl) [1,2,4] triazolo[1,5-a] quinolin-6-amine, bearing 4-methoxy substitution caused better efficacy against the all used pathogens while on the other hand derivative 4h i.e. 2-{(chloromethoxy)methyl}thio-N-(4-aminophenyl) [1,2,4]tria zolo[1,5-a]quinolin-6-amine bearing 4-amino group resulted into better insecticidal as well as anthelmintic activity.…”

“…compound 2. The latter was anilated by the reaction of different substituted aromatic amines to afford 6-(substituted phenylamino)(1,2,4-triazolo)(1,5-a)quinoline-2-thiol; 3a-h. Condensation reaction of compounds 3a-h with bis(chloromethyl) ether produced target derivatives, 2-[(chloro methoxy)methylthio-N-substitutedphenyl]- (1,2,4) triazolo (1,5-a)quinolin-6-amine; 4a-h. …”

“…Due to its sweet odor, it was frequently used in perfumes since 1882. Coumarin and its derivatives extensively used as building block in heterocyclic synthetic chemistry for their versatile biological activities including antibacterial [2][3][4][5] antifungal [6][7][8][9][10], herbicidal [11], antitumor [12][13], anti-HIV [14], anticoagulant [15], anticonvulsant [16][17], anti-inflammatory [18][19], antimalarial [20] activities. In addition, these compounds are used as additives in food and cosmetics [21], dyes for tuning lasers [22][23][24][25].…”