Biological activities antimalarial

Physical form White acicular crystals with bitter taste. Biological activity Antimalarial. 

A.Soluble in water, alcohol and chloroform. Biological activity Antimalarial. 

Aldot condensations between a ketone acting as methylene compound and an aldehyde are termed C laiscn-Schmidt condensations [9]. Therefore. Claisen-Schmidt condensations between acetophenone and bcn/aldchyde derivatives allow u.p-unsaturated ketones called chalconcs (Figure 14) 1110, 182, 256-258]. Chalcones are flavonoids of numerous applications as pesticides, phoioproiector in plastics, solar creams, food additives and many biological activities [Pg.98]

Refer to [8404]. BIOLOGICAL ACTIVITY Antimalarial comparable to that of agrimol [8404]. 

Many quinazolines possessing a wide variety of biological activities are known. The antimalarial activity of febrifugine spurred the preparation and testing of a number of quinazolines, and several... 

Chemistry and biological activity of artemisinin (sesquiterpene y-lactone with oxepane fragment and transannular peroxide bridge) and related antimalari-als 99H(51)1681. 

The large diversity of biological activities including antimalarial, antioxoplasmosis, antileishmaniasis, antishistosomiasis, antitrypanosomiasis, antiviral, antifugal and even anticancer activities displayed by artemisinin and artemisinin derivatives (cf. Ref. 55 for a review) added to the multitude of artemisinin-inspired trioxanes, trioxolanes, tetraoxa-cycloalkanes and peroxide, homodimeric-, trimeric- and even tetrameric artemisinin derivatives recently designed and synthesized is a clear indication that in the future, these compounds will become even more important in the chemotherapy of various diseases, perhaps even above and beyond those mentioned here. 

Quinazolines have become increasingly important as biologically active principles, e.g., as antiseptics or antimalarials. An interesting approach to this class consists of a combination of the aza-Wittig reaction with photochemical processes, as shown in Scheme 76. o-Azidocinnamates (206) are cyclized with the aid of triethyl phosphite to afford 2-alkoxyquinolines... 

Dihydroquinoline derivatives are known to exhibit a wide spectrum of biological activities such as antimalarial, antibacterial, and anti-inflammatory behavior [69-71]. In addition, substrates possessing the dihydroquinoline moiety... 

Bhattacharya AK and Sharma RP (1999) Recent developments on the chemistry and biological activity of artemisinin and related antimalarials - an update. 

The ramifications of the different conformational natures of 166-176 and other similar analogues on biological activity may be a promising area of future exploration. As a preliminary approach, a comparison of the low-energy conformers predicted by molecular mechanics and two-dimensional NMR data are under analysis. A possible correlation with conformational families of these flexible analogues and the antimalarial activity is under examination. 

Further, there does not exist sufficient data regarding the biological activity for each enantiomer in a racemic mixture of artemisinin analogues. To help define the antimalarial contribution made by each enantiomer, a model was developed in which 40 racemates were placed as single (+)-enantiomers in the original database of 202 compounds. By doing this it was implied that the (-)-enantiomers are as active as their counterpart, and an optically pure compound is not necessary for antimalarial activity. These achiral models have been discussed as 199 (2 A/C.3) and 199 Dock. A database without the racemates, or chiral models 160 (2 A/C.3) and 160 Dock, were also included in our study. Finally, adjustment to an achiral model was attempted in which the activities of the racemates in the 199 (2 A/C.3) model were multiplied by 2, or model 199 (2 A/C.3). In each case, data was subjected to the statistical pis analysis (Table 18). Relative antimalarial activities were predicted for two racemic compounds 421 and 422,155 using these datasets as shown in Tables 19 and 20. 

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