Antimycobacterial activity

During the most active period of investigation of sulfanilamide derivatives, 1935—1944, for systemic bacterial infections, the antimycobacterial activity of 4,4 -dianainodiphenylsulfone [80-08-8] (DDS, dapsone) was discovered (14). Although neither this compound nor its derivatives proved to be clinically usehil for human tuberculosis, it did evolve into the most important type of compound for leprosy (15). The diacetyl derivative has also... 

Pereira CG, Leal PF, Sato DN and Meireles MAA. 2005. Antioxidant and antimycobacterial activities of Tabernaemontana catharinensis extracts obtained by Supercritical CO2 +cosolvent. J Med Food 8(4) 533—538. 

The answer is b. (Hardmanr p 1158.) Isoniazid inhibits cell-wall synthesis in mycobacteria. Increasing vitamin B6 levels prevents complications associated with this inhibition, including peripheral neuritis, insomnia, restlessness, muscle twitching, urinary retention, convulsions, and psychosis, without affecting the antimycobacterial activity of INH. 

Bosi S, Da Ros T, Castellano S, Banfi E, Prato M (2000) Antimycobacterial activity of ionic fullerene derivatives. Bioorg. Med. Chem. Lett. 10 1043-1045. 

More recent investigations on the antimycobacterial activity of pamamycin-607 (lb) on 25 independent M. tuberculosis clinical isolates (either susceptible, mono-, or multiresistant to the first line antituberculous drugs) established minimum inhibitory concentrations MICjoo in the range of 1.5-2.0 pg/ml, while the MICjoo of lb for a bioluminescent laboratory strain of M. tuberculosis (H37Rv) was determined as 0.55 pg/ml [3a]. Parallel studies on the effect of lb on the cell cycle distribution of human (HL-60) cells by flow cytometry indicated no... 

Leon-Rivera I, Miron-Lopez G, Molina-Salinas GM, Herrera-Ruiz M, Estrada-Soto S, Gutierrez M, Alonso-Cortes D, Navarrete-Vasquez G, Rios M, Said-Femandez S (2008) Tyrianthinic Acids from Ipomoea tyrianthina and Their Antimycobacterial Activity, Cytotoxicity and Effects on the Central Nervous System. J Nat Prod 71 1686... 

Antimalarial activity. The dried leaf was inactive on Plasmodium falciparum D-6 and W-2, ICjf, greater than 1000 nmols " h Antimycobacterial activity. Essential oil, on agar plate, was active on AntimycO bacterium smegmatis, MIC 0.1 mg/mL 5 Anti-nematodal activity. Water extract of the dried leaf at variable concentrations produced strong activity on Meloidogyne incognita. ... 

Antimycobacterial activity. Ethanol (95%) and water extracts of the entire plant, on agar plate, were inactive on Mycobacterium tuberculosis ° Leaf juice, on agar plate, produced weak activity on Mycobacterium tuberculosis, MIC less than 1 20 L Anti-nematodal activity. Methanol ex-tract of the fruit, at a concentration of 1 mg/ mL, was active, and the water extract, at a concentration of 10 mg/mL, produced weak activity on Toxacara canis . 

Two naturally occurring 1,3-oxazine derivatives with a unique, 2-chlorinated tetrahydro-l,3-oxazine structure were reported as metabolites isolated from extracts of the endophytic fungus Geotrichum sp. AL4 <2007MI1520>. Halogenated 3-(4-alkylphenyl)-l,3-benzoxazine-2,4(3//)-diones were found to exhibit antimycobacterial activity <2007AP264>. 

Encamacion-DimayugaR, Ramirez MR, Luna-Herrera J (2003) Aerothionin, aBromotyro-sine Derivative with Antimycobacterial Activity from the Marine Sponge Aplysina gerardogreeni (Demospongia). Pharm Biol 41 384... 

Kdnig GM, Wright AD, Franzblau SG (2000) Assessment of Antimycobacterial Activity of a Series of Mainly Marine Derived Natural Products. Planta Med 66 337... 

The plants with the highest antimycobacterial activity include ... 

Plant species from a wide range of families have been shown to have significant in vitro antimycobacterial activities, and a number of active plant-derived compounds belonging to various chemical classes have been isolated. 

Crude extracts prepared from different parts of Turkish T. baccata have also been evaluated for their antimycobacterial activity. A CHCI3 fraction of the heartwood and ethanol extract of the leaves exhibited a minimum inhibitory concentration value (MIC) against Mycobacterium tuberculosis H37Ra strain of 200 pg/mL [102]. 

Pytela O, Klimesova V (2011) Effect of substitution on the antimycobacterial activity of 2-(substituted benzyl)sulfanyl benzimidazoles, benzoxazoles, and benzothiazoles-a quantitative structure-activity relationship study. Chem Pharm Bull 59 179-184... 

Banfi E, Scialino G, Zampieri D et al (2006) Antifungal and antimycobacterial activity of new imidazole and triazole derivatives. A combined experimental and computational approach. J Antimicrob Chemother 58 76-84... 

S. pyrocinia produces [118] an antifungal antibiotic pyrrolnitrin (140) active against mycobacteria. The antimycobacterial activity can be well correlated with the presence of the halogen and nitro group in the aromatic ring. 

Stille coupling between suitable 6-chloropurines and aryl(tributyl)tin afforded 6-arylpurines with a variety of substituents in the 9-position which were screened for antimycobacterial activity <02JMCI383>. The Stille cross-coupling reactions of 1,4- and l,3-bis(trialkylstannyl)benzenes with 9-benzyl-6-chloropurine gave 1,4- and l,3-bis(purin-6-yl)benzenes and 4-(purin-9-yl)benzenes <02T7431>. 

This section covers the preparation and reactions of nuclear or extranuclear pyrazinecarboxylic esters, pyrazinecarboximidates, and the like. Pyrazinecarboxylic esters exhibit antimycobacterial activities akin to those of pyrazinecarboxamides 651 the structure-activity relationship of such esters has been studied.656... 

High level compound purity is essential for a hit to become a genuine lead. For example, the terpene, ursolic acid, has shown inconsistent biological activity across a number of diverse assays. Recently, purity-activity studies of its antimycobacterial activity were performed using ursolic acid samples of varying purity. Ursolic acid showed enhanced antimycobacterial activity when impure.43... 

Molnar, Beladii, and Foldes [69] studied antimycobacterial activity of five phenothiazine derivatives including chlorpromazine, levomeprazine, promazine, promethazine, and diethazine. The growth of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium butyricum was found to be inhibited by chlorpromazine at practically identical concentrations. The minimum inhibitory concentrations for Mycobacterium tuberculosis were chlorpromazine and levomeprazine 10 xg/ml diethazine and promethazine 20 xg/ml whilst chlorpromazine sulphoxide was ineffective even at 100 xg/ml. Chlorpromazine and promethazine exerted a measurable bactericidal activity on Mycobacterium tuberculosis at 50 xg/ml total destruction of the organism and loss of acid fastness in part of the cells were shown at 300 xg/ml. Preliminary studies in mouse experiments revealed that phenothiazine derivatives were ineffective. 

Gasparova, R., Lacova, M., and EL-Shaaer, H.M. 1997. Synthesis and antimycobacterial activity of some new 3-heterocyclic substituted chromones. II Farmaco, 52 251-53. 

Applications of MCR-Derived Heterocycles in Drug Discovery Table 16 Antimycobacterial activities of spiro pyrrolidines... 

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