A Ru/Zn synergism in extraction of ruthenium by calixarene phosphine oxides

Diesters on the basis of 16-hydroxyisosteviol and dicarboxylic acids, exhibiting anti-tubercular activity, transport Fe(III) through liquid chloroform membrane which models a cell membrane. It is revealed that fluxes and anti-tubercular activity increase, as the length of the chain (spacer) between two ent-beyran skeletons of diesters increases. Computations on the level DFT/PBE explain the dependence of complexes stability on a structure of diterpenoid ligands. The structures of three diesters were established by single crystal X-ray analysis.     

Design,synthesis and biological evaluation of 5-(2-(4-(substituted benzo[d]isoxazol-3-yl)piperazin-1-yl)acetyl)indolin-2-one and 5-(2-(4-substitutedpiperazin-1-yl)acetyl)indolin-2-one analogues as novel anti-tubercular agents

A series of thirty-six novel 5-(2-(4-(benzo[d]isoxazol-3-yl)piperazin-1-yl)acetyl)indolin-2-one and 5-(2-(4-substitutedpiperazin-1-yl)acetyl)indolin-2-one analogues were synthesized, characterized and screened for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain. These compounds exhibited minimum inhibitory concentration between 1.56 and 50 μg/mL. Among these derivatives, compounds 10c, 10d, 10j, 10o and 10v (MIC 6.25 μg/mL) displayed moderate activity, while compounds 10e, 10l, 10q, 10w,10x, 12d, 12e and 12i (MIC 3.12 μg/mL) showed good anti-tubercular activity and compounds 10f, 10k, 10p, 10r, 12f, 12j and 12k (MIC 1.56 μg/mL) exhibited excellent anti-tubercular activity. In addition, MTT assay was accomplished on the active analogues of the series against mouse macrophage (RAW 264.7) cells to evaluate the cytotoxic effect of the newly synthesized compounds and selectivity index of the compounds was determined.     

[Et3NH][HSO4]-mediated efficient synthesis of novel xanthene derivatives and their biological evaluation

A series of novel 2-chloro quinoline incorporated xanthene derivatives were synthesized by using various 2-chloro 3-formyl quinoline, dimedone and triethylammonium hydrogen sulfate [Et₃NH][HSO₄] as a catalyst as well solvent to give good to excellent yields. All the xanthene compounds were investigated for their in vitro antimycobacterial activity against M. tuberculosis H37Ra (MTB) and M. bovis BCG strains. Among the synthesized compounds 3a, 3c, 3d, 3e, 3g, 3h and 3k were highly potent against both the strains. Most of the active compounds were non-cytotoxic against THP-1, HCT-116, A549 and MCF-7 cell lines. Most active compounds were having higher selectively index which suggested that these compound were highly potent.     

Synthetic utility of sydnones to couple pharmacologically important heterocycles for antitubercular activity

In the present investigation we have utilized the 3-arylsydnones 1a–c to couple two biodynamic moieties in amide derivatives 7–10. The 3-arylsydnones were brominated to 4-bromo-3-arylsydnones 2a–c which further were reacted with benzotriazole/benzothiazolin-2-thione/morpholine/diphenylamine to the corresponding final compounds. The structures of the amide derivatives were confirmed by the spectral (IR, ¹H NMR and Mass) and analytical data. Further, these were subjected to the antitubercular activity against Mycobacterium tuberculae (H37Rv). The morpholine 7a–c and benzotriazole 8a–c derivatives have exhibited good inhibition.     

Benzothiazines in synthesis. Formal synthesis of erogorgiaene

A benzothiazine, readily available in enantiomerically pure form via a completely selective, intramolecular addition of a sulfoximine-stabilized carbanion to an α,β-unsaturated ester, could be converted to a precursor to erogorgiaene in good overall yield.     

L-Proline catalyzed one-pot multi-component synthesis of 2-（1,3-diphenyl-1H-pyrazol-4-yl）quinazolin-4（3H）-one derivatives and their biological studies

A new series of quinazolin-4（3H）-one derivatives containing a（1 3-diphenyl-1H-pyrazol-4-yl） core with substituents at the 2-position and aromatic or heteroaromatic substituents at the 3-position were synthesized using an L-proline catalyzed one-pot multi-component reaction approach.All the synthesized compounds were characterized and screened for their antimicrobial,antifungal and anti-tubercular activities.     

Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives

In the present investigation, a series of 2(4-pyridyl)-5[(aryl/heteroarylamino)-1-oxoethyl]thio-1,3,4-oxadiazole were synthesized using isonicotinohydrazide and substituted aryl/heteroaryl amines using pyridine as solvent. Newly synthesized compounds were tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. Among the synthesized compounds, compounds 2(4-pyridyl)-5((2-nitrophenylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5e), 2(4-pyridyl)-5((4-nitrophenylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5g) and 2(4-pyridyl)-5((2-pyrrolylamino)-1-oxoethyl)thio-1,3,4-oxadiazole (5k) produced highest efficacy and exhibited >90% inhibition at a concentration of 0.0077, 0.0052 and 0.0089 μM, respectively. All the new compounds were pharmacologically evaluated for their in vitro Antimicrobial activity.     

Potential anti-tubercular agents: Hexahydro-3-phenyl indazol-2-yl(pyridin-4-yl)methanones from anti-tubercular drug isoniazid and bis(substituted-benzylidene)cycloalkanones

A series of indazol-2-yl(pyridin-4-yl)methanones,4 were acquired from 2,6-bisbenzylidene cyclohexanones,3 and anti-tubercular drug(isoniazid),and their anti-tubercular impacts were screened.Among the test compounds used against Mycobacterium tuberculosis H37 Ra cell line in the microplate alamar blue assay,the compounds 4g-j revealed moderate anti-tubercular activity with MIC 12.5 μg/mL,comparable to standard drugs(streptomycin,MIC,6.25 u.g/mL,pyrazinamide,isoniazid and ciprofloxacin with MICs of 3.125 μg/mL).     

Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids: Design,synthesis and in vitro anti-mycobacterial activity evaluation

A series of novel benzofuran-isatin-hydroxylimine/-thiosemicarbazide hybrids were designed, synthesized and evaluated for their in vitro anti-TB activities against drug-sensitive MTB H₃₇Rv and MDR-TB isolates as well as cytotoxicity. All benzofuran-isatin-hydroxylimine/-thiosemicarbazide hybrids exhibited considerable in vitro anti-mycobacterial activities against the tested three MTB strains, and all of them also showed acceptable cytotoxicity. The most active hybrid 7f was >4.8 and >51 folds more potent than the first line anti-TB agents RIF and INH against both drug-sensitive MTB H₃₇Rv and MDR-TB isolates, respectively. The results demonstrated the potential utility of benzofuran-isatin-hydroxylimine/-thiosemicarbazide hybrids as anti-TB agents.