Synthesis and in vitro antitubercular activity of pyridine analouges against the resistant Mycobacterium tuberculosis.

Mycobacterium tuberculosis (MTB) infection has become a growing health risk as multi-drug resistant strain (MDR-MTB) has emerged worldwide. The development of isoniazid (INH)-resistant M. tuberculosis strains dictate the need to re-design this old drug to create effective analogs against the resistant INH strains. Synthesis and the biological activity of isoniazid and pyridine derivatives were successfully carried out with elaborated characterization by spectral data. Amongst the synthesized compounds; 1 and 2 displayed encouraging antimycobacterial activity with IC50 of 3.2 µM and 1.5 µM against the H37Rv strain. The MIC of test compounds 1 and 2 were also assessed against the 5 drug resistant isolates (FQ-R1, INH-R1, INH-R2, RIF-R1 and RIF-R2) of MTB strains under aerobic conditions and compound 1 [MIC = 3.2 µM for FQ-R1; MIC = 140 µM for INH-R1; MIC = 160 µM for INH-R2; MIC = 2.4 µM towards RIF-R1; MIC = 4.2 µM for RIF-R2] and 2 [MIC = 3.3 µM for FQ-R1; MIC = 170 µM for INH-R1; MIC = 190 µM for INH-R2; MIC = 1.8 µM for RIF-R1; MIC = 8.4 µM for RIF-R2] have shown significant activity at non-cytotoxic concentration in comparison to the standard drug.

Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.

New classes of drugs are needed to treat tuberculosis (TB) in order to combat the emergence of resistance (MDR and XDR) to existing agents and shorten the duration of therapy. Mycobacterial DNA gyrase B subunit has been identified to be one of the potentially under exploited drug targets in the field of antitubercular drug discovery. In the present review, we discussed the synthesis, structural optimization and docking study of effective potent DNA gyrase inhibitor against M. tuberculosis, with improved properties such as enhanced activity against MDR strains, reduced toxicity. Based on this progress, if we can successfully leverage the opportunities in this target, there is hope that we will be able to raise novel gyrase inhibitor in earnest in the long.

Primary vaginal myeloid sarcoma: a rare case report and review of the literature.

Myeloid sarcoma (chloroma, granulocytic sarcoma, or extramedullary myeloid tumour) is an extramedullary mass forming neoplasm composed of myeloid precursor cells. It is usually associated with myeloproliferative disorders but very rarely may precede the onset of leukemia. Here, we are presenting a rare case of primary vaginal myeloid sarcoma in a geriatric female patient without initial presentation of acute myeloid leukemia (AML). A 68-year-old female patient with ECOG Performance Score of 1 presented with pervaginal bleeding for 20 days. On colposcopic examination, she was found to have mass in the anterior fornix of vagina. A punch biopsy specimen revealed chloromatous infiltration of the vagina. LCA (leukocyte common antigen), MPO (myeloperoxidase), and c-kit were strongly positive on IHC (immunohistochemistry). The patient's routine blood investigations were normal including peripheral smear, lactose dehydrogenase, uric acid, 2D echocardiography, conventional cytogenetics, bone marrow aspiration, and biopsy. The patient was given 4 cycles of decitabine (Decitex, manufactured by Sun Pharmaceutical Industries Limited, India), 20 mg/m(2) for 5 days at an interval of 28 days. There was a partial response to decitabine according to RECIST criteria. As decitabine therapy was well tolerated, we are continuing in the same way until disease progression without any complications. The patient is undergoing regular follow-up at our centre.

Determination of azathioprine in bulk and pharmaceutical dosage form by HPTLC.

INTRODUCTION: An HPTLC method for analysis of Azathioprine in bulk and pharmaceutical formulation has been established and validated. MATERIALS AND METHODS: The analyte was separated on aluminium plates precoated with silica gel 60 F254. The mobile phase was Ethyl acetate: Methanol: Triethylamine (4:1:0.5v/v). Quantification was done by densitometric scanning at 300nm. RESULTS: Response was a linear function of Azathioprine concentration in the range of 200-1200 ng/band. The limit of detection and quantification for Azathioprine were 18.58 and 59.14 ng/band, respectively. Average recovery was 100.1% which shows that the method was free from interference from excipients present in the formulation. CONCLUSION: The established method enabled accurate, precise, and rapid analysis of Azathioprine in bulk as well as pharmaceutical formulation.

Validated stability-indicating high-performance thin-layer chromatographic method for estimation of cefpodoxime proxetil in bulk and in pharmaceutical formulation according to International conference on harmonization guidelines.

AIM: A simple, selective, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for analysis of cefpodoxime proxetil both in bulk and in pharmaceutical formulation has been developed and validated. MATERIALS AND METHODS: The method employed HPTLC aluminum plates precoated with silica gel 60 RP-18 F(254) as the stationary phase. The solvent system consisted of toluene:methanol:chloroform (4:2:4 v/v). The system was found to give compact spot for cefpodoxime proxetil (R(f) value of 0.55 ± 0.02). Densitometric analysis of cefpodoxime proxetil was carried out in the absorbance mode at 289 nm. RESULTS: The linear regression analysis data for the calibration plots showed good linear relationship, with r(2) = 0.998 ± 0.0015 with respect to peak area in the concentration range of 100-600 ng per spot. The mean value±SD of slope and intercept were 3.38 ± 1.47 and 986.9 ± 108.78 with respect to peak area. The method was validated for precision, recovery, and robustness. The limits of detection and quantification were 3.99 and 12.39 ng per spot, respectively. Cefpodoxime proxetil was subjected to acid and alkali hydrolysis, oxidation, and thermal degradation. The drug undergoes degradation under acidic and basic conditions, indicating that the drug is susceptible to both acid and base. The degraded product was well resolved from the pure drug, with significantly different R(f) value. Statistical analysis proves that the method is repeatable, selective, and accurate for the estimation of the investigated drug. CONCLUSION: The proposed HPTLC method can be applied for identification and quantitative determination of cefpodoxime proxetil in both bulk drug and pharmaceutical formulation.

Spectrophotometric determination of ethacridine lactate in infusion.

AIM: A simple, rapid, selective, accurate, and precise UV spectrophotometric method has been developed for the estimation of ethacridine lactate from bulk and pharmaceutical formulation. MATERIALS AND METHODS: Appropriate aliquot portions of stock standard solution of ethacridine lactate were transferred into five separate 10 ml volumetric flasks, and the volume was adjusted to the mark with double distilled water to obtain concentrations of 0.2, 0.4, 0.6, 0.8, 1.0, and 1.2 µg/ml. The λmax of ethacridine lactate in double distill water was found to be 271 nm with an apparent molar absorptivity of 59.781 × 10(3) l/mol cm. The drug follows linearity in the concentration range 2-12 µg/ml with a correlation coefficient value of 0.998. RESULTS: The proposed method was applied to pharmaceutical formulation and % amount of drug estimated 99.71% was found to be in good agreement with the label claim. The accuracy of the method was checked by recovery experiment performed at three different levels, i.e., 80%, 100%, and 120%. The % recovery was found to be in the range 99.26-100.25%. The low values of % RSD are indicative of the accuracy and reproducibility of the method. The precision of the method was studied as intraday, interday variations and repeatability. The % RSD value less than 2 indicates that the method is precise. Ruggedness of the proposed method was studied with the help of two analysts. CONCLUSION: The results indicated that the method could be used for the routine estimation of ethacridine lactate from tablet formulations.

Development and validation of the UV-spectrophotometric method for determination of terbinafine hydrochloride in bulk and in formulation.

BACKGROUND: The main objective was to develop and validate the UV-spectrophotometric method for the estimation of terbinafine hydrochloride in bulk and pharmaceutical formulations as per ICH guidelines. MATERIALS AND METHODS: A simple, rapid, accurate, and economical UV-spectrophotometric method has been developed for the estimation of terbinafine hydrochloride from bulk and pharmaceutical formulation. RESULTS: The λmax of terbinafine hydrochloride in water was found to be 283 nm. The drug follows linearity in the concentration range 5-30 µg/ml with a correlation coefficient value of 0.999. The proposed method was applied to pharmaceutical formulation and % amount of drug. estimated was 99.19% and was found to be in good agreement with the label claim. The accuracy of the method was checked by recovery experiment performed at three different levels, i.e., 80%, 100%, and 120%. The % recovery was found to be in the range of 98.54- 99.98%. The low values of % RSD are indicative of the accuracy and reproducibility of the method. The precision of the method was studied as an intraday; interday variations, and repeatability. The % RSD value < 2 indicates that the method is precise. Ruggedness of the proposed method was studied with the help of two analysts. CONCLUSION: The above method was a rapid tool for routine analysis of terbinafine hydrochloride in the bulk and in the pharmaceutical dosage form.

Spectrophotometric method for simultaneous estimation of atenolol in combination with losartan potassium and hydrochlorothiazide in bulk and tablet formulation.

AIM: To develop a simple, accurate, rapid and precise UV spectrophotometric method for the estimation of atenolol in combination with losartan potassium and hydrochlorothiazide. MATERIALS AND METHODS: The method employs formation and solving simultaneous equation using 251.60 nm and 224.20 nm for losartan potassium and atenolol, 224.20 and 271.60 for atenolol and hydrochlorothiazide as two analytical wavelengths, using methanol water as a solvent. RESULTS AND CONCLUSION: The linearity was observed in the concentration range of 5-30 µg/ml (r=0.9991) for losratan pottassium, 2 - 12 µg/ml (r = 0.9995) for atenolol and 2 - 14 µg/ml (r = 0.9993) for hydrochlorothiazide. The results of the method were validated statistically and by recovery studies.

Evaluation of wound healing effect of petroleum ether and methanolic extract of Abelmoschus manihot (L.) Medik., Malvaceae, and Wrightia tinctoria R. Br., Apocynaceae, in rats / Avaliação do efeito de cicatrização dos extratos de éter de petróleo e metanol de Abelmoschus manihot (L.) Medik., Malvaceae, e Wrightia tinctoria R. Br., Apocynaceae, em ratos

In recent years, oxidative stress and free radicals have been implicated in impaired wound healing. Abelmoschus manihot (L.) Medik., Malvaceae, and Wrightia tinctoria R. Br., Apocynaceae, plants widely used in Ayurveda, possesses anti-inflammatory and antimicrobial properties. The present study was undertaken to assess the potential of petroleum ether and methanolic extracts in wound healing in Wistar albino rats. The rats were divided into six groups of six animals each. Group 1 is normal wounded control, group 2 received standard drug and the other four groups were treated with two different doses each of petroleum ether and methanolic extract of A. manihot and W. tinctoria. The wound healing parameters were evaluated by using incision wounds in extract-treated rats, standard and controls. Both the doses of petroleum ether and methanolic extract significantly increased wound breaking strength when compared with the control group.

Nos últimos anos, o estresse oxidativo e radicais livres têm sido implicados na cicatrização. Abelmoschus manihot (L.) Medik., Malvaceae e Wrightia tinctoria R. Br., Apocynaceae, plantas utilizadas na medicina Ayurveda, possuem propriedades antiinflamatórias e antimicrobianas. O presente estudo foi realizado para avaliar o potencial dos extratos de éter de petróleo e metanólico na cicatrização de feridas em ratos Wistar. Os ratos foram divididos em seis grupos com seis animais cada. O grupo 1 foi utilizado como controle, o grupo 2 recebeu a droga padrão e os outros quatro grupos foram tratados com duas doses diferentes de cada um dos extratos de A. manihot e W. tinctoria. Os parâmetros de cicatrização foram avaliados através da incisão feridas em ratos tratados com extrato, padrões e controles. Ambas as doses dos extratos de éter de petróleo e metanólico aumentaram significativamente força de ruptura da ferida quando comparados ao grupo controle.