Synthesis, characterization and assessment of antioxidant and antibacterial potential of dihydroquinoline-3-carboxylic acid and their metal derivatives.

Metal complexes of drug are used to inhibit growth of pathogenic microorganisms and reduces drug resistance. Moxifloxacin is a dihydroquinoline-3-carboxylic acid 4th generation fluoroquinolone antibiotic that has tendency to bind with metal ions. In current study four moxifloxacin-metal complexes i.e. Moxifloxacin-sliver (Moxi-Ag), Moxifloxacin-rhodium (Moxi-Rh), Moxifloxacin-titanium (Moxi-Ti) and Moxifloxacin-rubidium (Moxi-Rb) have been synthesized and evaluated for antibacterial activities against resistant microorganisms along with antioxidant effects. The structure elucidation was carried out using FTIR, 1H- NMR and UV-Vis spectroscopy. Agar well diffusion method and DPPH (1, 1- dipheny1-2-picrylhydrazyl) methods were used to study the antibacterial and antioxidant activity respectively. Both 1H NMR and FTIR spectra clearly showed that Moxi-metal complexes are formed due to change in their carboxyl stretching band in IR, H-2 and H-5 peak position in 1H NMR. All the Moxi-metal complexes showed distinguished antibacterial effects against both Gram-negative and Gram-positive bacteria as compared to drug which was found resistant against many microorganisms. Moxi-Rb and Moxi-Ag metal complexes showed higher antioxidant activity (IC50 values range from 8.26 - 9.19 µg/ml) than Moxi-Ti and Moxi-Rh metal complexes (IC50 range from 11.23 - 14.65 µg/ml).

Comparative effectiveness of individualized longer and standardized shorter regimens in the treatment of multidrug resistant tuberculosis in a high burden country.

Objective: To compare the effectiveness of second line injectables containing shorter (duration 9-12 months) and longer treatment regimens (LTR, duration ≥ 20 months) among multidrug-resistant tuberculosis (MDR-TB) patients with no documented resistance and history of treatment with any second-line anti-TB drug (SLD) for ≥ 1 month. Methods: This was an observational cohort study of MDR-TB patients treated at eight PMDT units in Pakistan. Patients' data from baseline until treatment outcomes were collected from Electronic Nominal Recording and Reporting System. The treatment outcomes of "cured" and "treatment completed" were grouped together as successful, whereas "death," "treatment failure," and "lost to follow-up" were collectively grouped as unsuccessful outcomes. Time to sputum culture conversion (SCC) was analyzed using the Kaplan-Meier method and the differences between groups were compared through the log-rank test. Multivariate Cox proportional hazards and binary logistic regression analyses were used to find predictors of time to SCC and unsuccessful treatment outcomes. A p-value < 0.05 was considered statistically significant. Results: A total 701 eligible MDR-TB patients [313 treated with shorter treatment regimen (STR) and 388 treated with LTR at eight centres in Pakistan were evaluated]. Time to achieve SCC was significantly shorter in STR group [mean: 2.03 months, 95% confidence interval (CI):1.79-2.26] than in LTR group (mean: 2.69 months, 95% CI: 2.35-3.03) (p-value<0.001, Log-rank test). Treatment success was higher in STR (83.7%) than in LTR (73.2%) group (p-value <0.001) due to high cure (79.9% vs. 70.9%, p-value = 0.006) and low death (9.9% vs. 18.3%, p-value = 0.002) rates with STR. Treatment with STR emerged the only predictor of early SCC [adjusted Hazards ratio (aHR) = 0.815, p-value = 0.014], whereas, patient's age of 41-60 (OR = 2.62, p-value<0.001) and >60 years (OR = 5.84, p-value<0.001), baseline body weight of 31-60 (OR = 0.36, p-value = 0.001) and >60 kg (OR = 0.23, p-value <0.001), and treatment with LTR (OR = 1.88, p-value = 0.001) had statistically significant association with unsuccessful treatment outcomes. Conclusion: STR exhibited superior anti-microbial activity against MDR-TB. When compared LTR, treatment with STR resulted in significantly early SCC, high cure, and lower death rates among MDR-TB patients who had no documented resistance and history of treatment with any SLD ≥ 1 month.

In Vitro Anti-Inflammatory, Anticancer (MCF-7, 3T3, and HeLa Cell Lines), and Brine Shrimp Lethality Assay and FTIR Analysis of the Extract and Fractions of the Whole Plant of Heliotropium europaeum.

In this study, anti-inflammatory, anticancer, brine shrimp lethality, and FTIR studies were evaluated. The oxidative burst assay using the chemiluminescence technique, MTT assay, brine shrimp lethality assay, and FTIR analysis were the methods used for the evaluation of anti-inflammatory, anticancer, brine shrimp lethality, and FTIR studies, respectively. The whole-plant butanol fraction of Heliotropium europaeum (WBFHE) showed anti-inflammatory activity on ROS having IC5014.7 ± 2.5 while the extract and other fractions of the whole plant of Heliotropium europaeum exhibited no anti-inflammatory activity. None of the extract and fractions of the whole plant of Heliotropium europaeum exhibited anticancer (MCF-7, 3T3, and HeLa cell lines) activities. The whole-plant aqueous fraction of Heliotropium europaeum (WAFHE) and whole-plant butanol fraction of Heliotropium europaeum (WBFHE) showed lethality at high concentration while at low concentration, no toxicity was shown. The whole-plant methanolic extract of Heliotropium europaeum (WMEHE) and whole-plant n-hexane fraction of Heliotropium europaeum (WHFHE) exhibited no toxicity. FTIR interpretation showed the functional groups for the aromatic compounds, phenols, carboxylic acids, esters, alkanes, alkenes, alcohols, alkyl halides, sulfate esters, phosphines, silanes, nitriles, thiols, amines, phosphoric acids, and nitro compounds.

Synthesis, characterization and antihypertensive activity of 2-phenyl substituted benzimidazoles.

Hypertension is one of cardiovascular disease that is not sufficiently prevented and controlled at both hospital and community levels. Hypertension resulted in significant morbidity and mortality. The benz-imidazole ring is very important pharmacophore in modern drug discovery. The substituted benzimidazoles are the important for medicinal research. Researchers have reported that substituted Benzimidazoles are the structural isosteres of nucleotides, and easily allow them to interact with the different biopolymers, possess pharmacological activity especially antihypertensive activity. Angiotensin II Receptor Antagonists/Blockers (ARBs) compete with angiotensin II at the receptor site and block the contractile effect of angiotensin II in all vascular smooth muscles. Among all Angiotensin II Receptor Antagonists/Blockers (ARBs), Telmisartan, Milfasartan and many others have benzimidazole ring in their structure. In this study Angiotensin II Receptor Antagonists/Blockers (ARBs) have been prepared. Synthesized compounds were characterized by physical data and FTIR spectroscopic technique. Synthesized compounds studied were finally screened for their antihypertensive activity by tail cuff method of measurement of blood pressure by NIBP apparatus (None Invasive Blood Pressure) using Chart 5.0 software. The compounds synthesized were 2-(3-nitrophenyl)-1Hbenzimidazole (1a), 3-(1H benzimidazol-2-yl)aniline (1b) and 5-(1H-benzimidazol-2-yl)-2-methoxyphenol (1c). The synthesized compounds have shown antihypertensive activity by taking Losartan as lead compound.