This work was supported by the Foundation for Science and Technology (FCT), Portugal (projects PTDC/QUI-QUI/113687/2009 and PEst-C/QUI/UI0081/2013). A.G. (SFRH/BD/43531/2008) and M.J.M. (SFRH/BD/61262/2009) thank FCT for grants.

/pdf/chromone-a-valid-scaffold-in-medicinal-chemistry-4qd4v5m5z2.pdf

Chromone: A Valid Scaffold in Medicinal Chemistry

Chromones as a privileged scaffold in drug discovery: a review.

Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Compounds, compositions, and methods

Drugs for treating tuberculosis (TB) have been available for over half a century, and yet the incidence of disease worldwide continues to rise year by year. In 2002, the last year for which statistics are available, it is estimated that 24,000 people developed active disease and close to 5,000

New Small-Molecule Synthetic Antimycobacterials

Benzotriazole: An overview on its versatile biological behavior

The synthesis of the biologically active novel systems derived from reaction of 3-formylchromones with three types of amino derivatives, 6-R2-2-aminobenzothiazoles, 6-amino-2-R3-thiobenzothiazoles and hydrazide derivatives (derived from cyanoacetic, isonicotine, salicylic and gallic acids) was carried out. The structures of the prepared compounds have been proved by elemental analysis, 1H NMR and IR spectra. Antimicrobial activity was studied against the following microorganisms — bacteria G+ (Staphylococcus aureus 29 58 , Bacillus subtilis 18 66 ), G− (Escherichia coli 326 71 , Pseudomonas aeruginosa); yeasts; Candida albicans, Saccharomyces cerevisiae; moulds; Microsporum gypseum, Aspergillus niger, Scopulariopsis brevicaulis; and against typical and atypical mycobacteria: Mycobacterium tuberculosis (H37Rv), Mycobacterium kansasii (PFG 8), Mycobacterium avium (My 80 72 ), Mycobacterium fortuitum (1021). The hereditary bleaching effect on the plastid system of Euglena gracilis, a unique phenomenon of the biological activity of chromone derivatives, is reported. The bleaching test on E. gracilis is used for detecting extranuclear mutations.

Synthesis, antimicrobial activity and bleaching effect of some reaction products of 4-oxo-4H-benzopyran-3-carboxaldehydes with aminobenzothiazoles and hydrazides

Condensation 4-oxo-4H-chromene-3-carboxaldehydes (1a,b) with acid hydrazine-carbodithioic acid and/or thiocarbohydrazide afforded hydrazonecarbodithioic acid 2, monothiocarbohydrazone 3a,b and bisthiocarbohydrazone 4, respectively. Heterocyclization of 2–4 via reaction with oxygen, sulfur and/or halogen reagents in different media yielded pyridazinethione 5; 1,3-thiazoles 7; pyrazoles 9–12; 1,2,4-thiadiazoles 8,13,14, and 23; 1,2,4-triazolethiones 15–17; 1,2,4-triazinethiones 18–22; imidazolethione 24 and pyrimidinethione 25 derivatives. Antifungal activity was screened for some the new synthesized compounds. Formulations of all products have been deduced by elemental analysis and spectral data (IR, 1H NMR and Mass spectroscopy).

Synthesis of Bioactive 4-Oxo-4H-Chromenes Bearing Heterocyclic Systems from Hydrazonecarbodithioic Acid and Thiocarbohydrazone

The aldol synthesis of benzimidazole, benzothiazole and benzothiazolium salt derivatives of chromones is described. The structures of the compounds have been proved by elemental analysis and 1H NMR spectra. The antimycobacterial activity of some of the prepared compounds have been tested in vitro against Mycobacterium tuberculosis (H37Rv) and Mycobacterium fortuitum (1021).

Synthesis and antimycobacterial activity of some new 3-heterocyclic substituted chromones.

A facile route to phenyl, phenylsulfanyl and phenylselanyl substituted pyrano[3,2-c]chromenes

The synthesis of eight hydroxy- and 2-oxopyranochromone-3-carboxaldehydes 3, 5 and their reactions with 2-hydroxyaniline, 2,4-dinitrophenylhydrazine and 2-benzothiazolylhydrazine were investigated. Products were confirmed by IR, NMR spectral and elemental analysis data. The semi-empirical AM1 quantum-chemical method has been used to study optimal geometries and heats of formation of synthesized 3-formylchromones.

http://www.isuct.ru/khimia/molecules/papers/30600149.pdf

Hafez M. El-Shaaer

Papers

Synthesis, antimicrobial activity and bleaching effect of some reaction products of 4-oxo-4H-benzopyran-3-carboxaldehydes with aminobenzothiazoles and hydrazides

Synthesis of Bioactive 4-Oxo-4H-Chromenes Bearing Heterocyclic Systems from Hydrazonecarbodithioic Acid and Thiocarbohydrazone

Synthesis and antimycobacterial activity of some new 3-heterocyclic substituted chromones.

A facile route to phenyl, phenylsulfanyl and phenylselanyl substituted pyrano[3,2-c]chromenes

Synthesis and Reactions of New 4-Oxo-4H-benzopyran-3-carboxaldehydes Containing Hydroxy Groups or 2-Oxopyran Cycles