Reaction of carbonyl-stabilized allyl sulfoxonium ylides with michael acceptors

Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/33983/1/0000255.pd

New synthetic methods: a general and efficient approach to ring-fused cycloheptadienes

Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/33984/1/0000256.pd

Antituberculosis Activity of Brotowali (Tinospora Crispa) Extract and Fractions Against Mycobacterium Tuberculosis Using Microplate Alamar Blue Assay Method

Tuberculosis (TB), in which caused by pathogenic bacteria, Mycobacterium tuberculosis, has become the major causes of death among all of infectious diseases. The increasing incidence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) has created a need to discover a new antituberculosis drug candidate. The aim of this study was to screen extract and fractions of Tinospora crispa for activity against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA) method. T. crispa extract was prepared by maceration in ethanol (96%) and antituberculosis activity was carried out using MABA method. The result of this study showed that ethanolic extract of T. crispa exhibit antituberculosis activity with minimum inhibition concentration of 12.5 mg/ml

Antituberculosis Activity of Brotowali (Tinospora crispa) Extract and Fractions against Mycobacterium tuberculosis using Microplate Alamar Blue Assay Method

Tuberculosis (TB), in which caused by pathogenic bacteria, Mycobacterium tuberculosis, has become the major causes of death among all of infectious diseases. The increasing incidence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) has created a need to discover a new antituberculosis drug candidate. The aim of this study was to screen extract and fractions of Tinospora crispa for activity against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA) method. T. crispa extract was prepared by maceration in ethanol (96%) and antituberculosis activity was carried out using MABA method. The result of this study showed that ethanolic extract of T. crispa exhibit antituberculosis activity with minimum inhibition concentration of 12.5 mg/ml

EVALUATION OF BENZYLIDENE-ACETONE ANALOGUES OF CURCUMIN AS ANTITUBERCULOSIS

 Objective: The objective of this research is to evaluate the effect of benzylideneacetone analog of curcumin against Mycobacterium tuberculosis (MTB) H37Rv.Method: The activity of benzylideneacetone analog of curcumin is evaluated using mycobacteria growth indicator tube (MGIT) method and microplate alamar blue assay (MABA) method. The compound of minimum inhibitory concentration (MIC) is defined as the minimum concentration of drugs which really inhibit the growth of MTB.Result: The MIC compound of 1,5-bis(3,4-dichlorophenyl)-1,4-pentadiene-3-one (C9) and 1,5-bis(3-chlorophenyl)-1,4-pentadiene-3-one (C10) can inhibit the bacteria of MTB at the concentration of 500 μg/ml using MGIT method. Based on MABA method, it can be obtained similar MIC value of C9 compound and C10 compound that are 187.5 μg/ml.Conclusion: C9 and C10 have antituberculosis activity. Benzylideneacetone analog of curcumin which has chlor moiety has a better activity in inhibiting MTB, but it still needs further research to make it become a potent antituberculosis drug

Antituberculosis Activity of Brotowali (Tinospora crispa) Extract and Fractions against Mycobacterium tuberculosis using Microplate Alamar Blue Assay Method

Tuberculosis (TB), in which caused by pathogenic bacteria, Mycobacterium tuberculosis, has become the major causes of death among all of infectious diseases. The increasing incidence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) has created a need to discover a new antituberculosis drug candidate. The aim of this study was to screen extract and fractions of Tinospora crispa for activity against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA) method. T. crispa extract was prepared by maceration in ethanol (96%) and antituberculosis activity was carried out using MABA method. The result of this study showed that ethanolic extract of T. crispa exhibit antituberculosis activity with minimum inhibition concentration of 12.5 mg/ml

A Novel Antimycobacterial Compound Acts as an Intracellular Iron Chelator

Efficient iron acquisition is crucial for the pathogenesis of Mycobacterium tuberculosis. Mycobacterial iron uptake and metabolism are therefore attractive targets for antitubercular drug development. Resistance mutations against a novel pyrazolopyrimidinone compound (PZP) that is active against M. tuberculosis have been identified within the gene cluster encoding the ESX-3 type VII secretion system. ESX-3 is required for mycobacterial iron acquisition through the mycobactin siderophore pathway, which could indicate that PZP restricts mycobacterial growth by targeting ESX-3 and thus iron uptake. Surprisingly, we show that ESX-3 is not the cellular target of the compound. We demonstrate that PZP indeed targets iron metabolism; however, we found that instead of inhibiting uptake of iron, PZP acts as an iron chelator, and we present evidence that the compound restricts mycobacterial growth by chelating intrabacterial iron. Thus, we have unraveled the unexpected mechanism of a novel antimycobacterial compound

Identification of a small molecule with activity against drug-resistant and persistent tuberculosis

A cell-based phenotypic screen for inhibitors of biofilm formation in mycobacteria identified the small molecule TCA1, which has bactericidal activity against both drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb) and sterilizes Mtb in vitro combined with rifampicin or isoniazid. In addition, TCA1 has bactericidal activity against nonreplicating Mtb in vitro and is efficacious in acute and chronic Mtb infection mouse models both alone and combined with rifampicin or isoniazid. Transcriptional analysis revealed that TCA1 down-regulates genes known to be involved in Mtb persistence. Genetic and affinity-based methods identified decaprenyl-phosphoryl-beta-D-ribofuranose oxidoreductase DprE1 and MoeW, enzymes involved in cell wall and molybdenum cofactor biosynthesis, respectively, as targets responsible for the activity of TCA1. These in vitro and in vivo results indicate that this compound functions by a unique mechanism and suggest that TCA1 may lead to the development of a class of antituberculosis agents

Synthetic Uses Of Carbonyl - Stabilized Sulfoxonium-allylides.

PhDOrganic chemistryUniversity of Michigan, Horace H. Rackham School of Graduate Studieshttp://deepblue.lib.umich.edu/bitstream/2027.42/191094/2/7510193.pd