griseofulvin and Tuberculosis

A series of novel morpholinoquinoline based conjugates with pyrazoline moiety were synthesized under microwave irradiation. The newly synthesized compounds were screened for their preliminary in vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi, antituberculosis activity against Mycobacterium tuberculosis H37Rv and antimalarial activity against Plasmodium falciparum. Most of them exhibited significant antibacterial activity as compared to the first line drugs. Compounds 6a and 9d were found to possess excellent antibacterial activity potency as compared to ampicillin (286 μM), chloramphenicol (154 μM) and ciprofloxacin (150 μM). In antifungal screening, against Candida albicans, compounds 6c, 7c, 8a, 8b, 8c and 9b showed significant activity as compared to griseofulvin (1147 μM). Compounds 8b, 6b, 9d, 6a, 9b, 7b and 8a displayed brilliant activity against P. falciparum strain as compared to chloroquine (IC50 0.062 μM) as well as quinine (IC50 0.826 μM). Compounds 6d, 7b, 8b, 9c and 9d exhibited superior antitubercular activity. Among them 8b was found to be equipotent to rifampicin with 95% inhibition. The cytotoxicity of the synthesized compounds was tested using bioassay of Schizosaccharomyces pombe cells at cellular level.

Topics: Anti-Infective Agents; Antimalarials; Antitubercular Agents; Bacteria; Bacterial Infections; Fungi; Humans; Malaria, Falciparum; Microbial Sensitivity Tests; Mycobacterium tuberculosis; Mycoses; Plasmodium falciparum; Pyrazoles; Quinolines; Structure-Activity Relationship; Tuberculosis

Twenty four biquinolone-isoniazid hybrids were designed based on molecular hybridization technique and synthesized via multicomponent cyclocondensation (MCC) approach. All the newly synthesized compounds were screened for their antimicrobial and antitubercular activities. The brine shrimp bioassay was carried out to study the cytotoxicity of the synthesized compounds. Hybrids 7f (MIC = 25 μg/mL); 7a, 7e and 7m (MIC = 50 μg/mL); 7g, 7h and 7k (MIC = 62.5 μg/mL) exhibited excellent antimicrobial activity as compared with standard drugs. Hybrids 7l and 7j displayed 99% inhibition against Mycobacterium tuberculosis bacteria with better LC50 values 35.39 and 34.59 μg/mL, respectively. These results indicate that the synthesized compounds can act as leads for the development of newer antimicrobial and antitubercular compounds.

Topics: Animals; Anti-Bacterial Agents; Antifungal Agents; Antitubercular Agents; Artemia; Bacteria; Dose-Response Relationship, Drug; Drug Design; Fungi; Isoniazid; Microbial Sensitivity Tests; Molecular Structure; Motor Activity; Quinolones; Structure-Activity Relationship; Tuberculosis

A new series of fluorinated pyrazoles, 4a-e, were synthesized in good to excellent overall yields (65-82%) from the corresponding chalcones, 3a-e, by ultrasonic irradiation. The newly synthesized compounds were characterized and screened for their in vitro anti-bacterial, anti-fungal, and anti-tubercular activities against Mycobacterium tuberculosis H(37)Rv.

Topics: Anti-Infective Agents; Antitubercular Agents; Bacteria; Bacterial Infections; Fungi; Green Chemistry Technology; Halogenation; Humans; Microbial Sensitivity Tests; Mycobacterium tuberculosis; Mycoses; Pyrazoles; Tuberculosis