Montmorillonite K10-catalyzed synthesis of N-fused imino-1,2,4-thiadiazolo isoquinoline derivatives

A novel synthesis of N-fused imino-1,2,4-thiadiazolo derivatives is described. This approach involves the inexpensive, nontoxic, recoverable, and easy to handle montmorillonite K10 that catalyzes the coupling of 3-aminoisoquinolines and phenylisothiocyanates to afford the N-fused imino-1,2,4-thiadiazolo isoquinoline motifs in exemplary yields. The main attractions of this synthetic strategy were simple procedure and excellent yields.     

Simultaneous Occurrence of Nanospheres and Nanofibers Self-Assembled from Achiral Tripeptides

The achiral tripeptide Boc-Aib-MABA-Aib-OMe has the ability to co-exist as nanospheres and as a network of nanofibers in methanol. Furthermore, AFM and TEM images show the presence of bulges in the network of nanofibers. Interestingly, the formation of nanofibers is seen to emerge from the outer boundary of the spherical structures. Some of the nanofibers curl up at the tip and later result in the formation of hollow nanospheres with thick boundaries. The presence of β-turn-like structures with hydrogen bonding is observed using FT-IR studies. The presence of hydrogen bonding is also demonstrated by using NMR studies.     

UPLC–MS/MS method validation of ciprofloxacin in human urine: Application to biodegradability study in microbial fuel cell

To enable the reliable quantification of ciprofloxacin in human urine, a sensitive and selective assay based on liquid chromatography–tandem mass spectrometry was developed. The chromatographic separation of the ciprofloxacin was carried out on a Zorbex Eclipse C₁₈ column using methanol and ammonium acetate as a mobile phase by the gradient elution method. The developed assay covered a wide range of concentrations (1.56–100 ng/mL) with a lower limit of detection of 0.76 ng/mL. Quantification was performed using the multiple reaction monitoring transitions 331.8/231 for ciprofloxacin and 362/318 for ofloxacin (internal standard). This assay was validated for linearity, accuracy, precision and recovery. The validated method was then applied to the biodegradability of ciprofloxacin (99%) from human urine in the microbial fuel cell.     

Chemoselective and Site-Selective Lysine-Directed Lysine Modification Enables Single-Site Labeling of Native Proteins

The necessity for precision labeling of proteins emerged during the efforts to understand and regulate their structure and function. It demands selective attachment of tags such as affinity probes, fluorophores, and potent cytotoxins. Here, we report a method that enables single-site labeling of a high-frequency Lys residue in the native proteins. At first, the enabling reagent forms stabilized imines with multiple solvent-accessible Lys residues chemoselectively. These linchpins create the opportunity to regulate the position of a second Lys-selective electrophile connected by a spacer. Consequently, it enables the irreversible single-site labeling of a Lys residue independent of its place in the reactivity order. The user-friendly protocol involves a series of steps to deconvolute and address chemoselectivity, site-selectivity, and modularity. Also, it delivers ordered immobilization and analytically pure probe-tagged proteins. Besides, the methodology provides access to antibody-drug conjugate (ADC), which exhibits highly selective anti-proliferative activity towards HER-2 expressing SKBR-3 breast cancer cells.     

Discovery of a Novel Mycobacterial F-ATP Synthase Inhibitor and its Potency in Combination with Diarylquinolines

The F₁F_O-ATP synthase is required for growth and viability of Mycobacterium tuberculosis and is a validated clinical target. A mycobacterium-specific loop of the enzyme's rotary γ subunit plays a role in the coupling of ATP synthesis within the enzyme complex. We report the discovery of a novel antimycobacterial, termed GaMF1, that targets this γ subunit loop. Biochemical and NMR studies show that GaMF1 inhibits ATP synthase activity by binding to the loop. GaMF1 is bactericidal and is active against multidrug- as well as bedaquiline-resistant strains. Chemistry efforts on the scaffold revealed a dynamic structure activity relationship and delivered analogues with nanomolar potencies. Combining GaMF1 with bedaquiline or novel diarylquinoline analogues showed potentiation without inducing genotoxicity or phenotypic changes in a human embryonic stem cell reporter assay. These results suggest that GaMF1 presents an attractive lead for the discovery of a novel class of anti-tuberculosis F-ATP synthase inhibitors.     

Surface Modified Long Period Fiber Grating Sensor for Rapid Detection of Aspergillus Niger Fungal Spores

We present development of a compact and label-free sensor based on the surface modification of copper vapor laser fabricated long period fiber gratings for detection of airborne Aspergillus niger (A. niger) fungal spores. Surface of sensors were functionalized with monoclonal glucose oxidases IgG1 for target-specific covalent binding. In process of functionalization and binding of 10³ cfu/ml of pathogenic A. niger fungal spores, notable shorter wave transition in resonance wavelength from 1562.93 nm to 1555.97 nm, and significant reduction in peak loss from 61.72 dB to 57.48 dB were recorded. The implementation was cost effective and yielded instantaneous results.     

Infrared and raman studies of some naphthols

Vibrational spectra of α-naphthol,β-naphthol andβ-naphthol-OD have been recorded in the solid and solution phases. A number of bands, common to all the three compounds, have been correlated with earlier naphthalene assignments and an attempt has been made to identify certain frequencies with vibrational modes that are centred in the substituentsOH andOD. TheC _s symmetry is assumed for each molecule.