Font Size: a A A

Study On The Screening And Preparation For Nitazoxanide_pleuromutilin And Other Hybrid Anti-TB Drugs

Posted on:2017-01-20Degree:MasterType:Thesis
Country:ChinaCandidate:J ZhangFull Text:PDF
GTID:2311330512462412Subject:Pharmaceutical Engineering
Abstract/Summary:PDF Full Text Request
Antibioticisthe breakthrough result in the history of human medicine.It is a powerful weapon that people resist the disease and saved thousands of lives.With the widespread use of antibiotics,resistant accompanying gradually into the people’s vision.The misuse of antibiotics has been accelerating the development of resistant bacteriaundoubtedly.At present,the situation has been very severe resistant,its traditional role of antibiotics has been minimal.Human life has also been a serious security threat.The TB is a very ancient infectious disease andhas high mortality rate.While some anti-TB drugs have controlled tuberculosis on the 20 th century,the global TB epidemic is on the risein recent years.Especially the emergence of drug resistance and MDR-TB made the global TB epidemic very severe.Now the Clinical first-line anti-TB and second-line anti-TB drugs are increasingly unsatisfactory.The traditional anti-TB drugs have failed to meet the clinical needs.Therefore,in today’s situation is more severe,new anti-TB drugs have been developed it is imperative!Pleuromutilin was firstly isolated from two natural Higher Basidiomycetes Pleurotus multilus(Fr.)Sacc.And P.passecke-rianus Pilat.It is an eight-membered ring double mushrooms compoundwitha rigid 5-6-8 posts tricyclic structure carbon skeleton.It can effectively suppress staphylococcus,streptococcus and Gram-positive bacteria and other microorganismsandtreat disease mycoplasma infection.Pleurotus truncated element and bacterial ribosomes,effectively prevent the truncated ear carotenoid compounds hydrophobic part of C14 side chain extends into the bacterial ribosomes,and selective inhibition of bacterial protein synthesis.Related research reports that pleuromutilin antibacterial activity is than many derivatives pleuromutilin stronger,while the broader antibacterial spectrum.The product has the efficacy of anti-multidrug-resistant tuberculosis.We should thoroughly study Pleuromutilin.Rifamycinis antibiotic compounds from the Streptomyces Mediterranean.Rifamycin compounds have a wide antibacterial spectrum.It caneffectively kill Mycobacterium tuberculosis,and some non-tuberculous mycobacteria(including Mycobacterium leprae,etc.),aerobic gram-positive bacteria(including Bacillus anthracis,Staphylococcus aureus enzyme,methicillin-resistant strains,etc.),the needoxygen Gram-negative bacteria(including Neisseria gonorrhoeae,Neisseria meningitidis,Haemophilus influenzae,etc.).The antibacterial mechanismis thatit can be firmly combined with bacterial RNA polymerase β subunit,blocking bacterial RNA synthesis andbacterial RNA transcription process,that stop the synthesis of DNA and protein eventually.Since the discovery of rifampicin,it has a good effect of tuberculosis.Currently,the rifamycins already on the market are mainly rifampicin,rifadin,rifapentine,rifabutin.rifamycin class of drugs is one of themain anti-TB drugs now in clinical.In this paper,with antibacterial activity,a very wide spectrum antibiotic pleuromutilin,nitazoxanide,metronidazole,rifampicin and isoniazid drug molecules as the study subject and with the drug molecule to put together,a new concept for the heterozygous as the guiding ideology,we devised better efficacy,safety and reliability of the new hybrid antibiotic molecular structure for nitazoxanide_pleuromutilins,pleuromutilin_metronidazole and HYD.Following the principle of a simple process and readily available starting materials andreasonable cost,we designed and synthesized route of new molecular structure and obtained samples tested,they showed good antibacterial activity.
Keywords/Search Tags:Pleuromutilin, rifamycin, heterozygous drugs, TB, antibacterial activity
PDF Full Text Request
Related items