Dithiin diisoimides: Synthesis and their antimicrobial studies.

Sixteen derivatives of dithiin diisoimide 2a-2p have been synthesized and screened for antibacterial and antifungal activity. Compounds 2a-2g and 2i-2p are almost same or more active than gentamicine against Acinetobacter. Whereby compound 2,6-didodecyl-1H,5H-pyrrolo[3',4',5,6][1,4]dithiino[2,3-c]pyrrole-1,3,5,7(2H,6H)-tetrone (2d) having zone of inhibition 20 mm against Acinetobacter is the most potent among all these compounds and can be used as lead compound for the treatment of Acinetobacter infection.

Synthesis of Novel Triazinoindole-Based Thiourea Hybrid: A Study on α-Glucosidase Inhibitors and Their Molecular Docking.

A new class of triazinoindole-bearing thiosemicarbazides (1-25) was synthesized and evaluated for α-glucosidase inhibitory potential. All synthesized analogs exhibited excellent inhibitory potential, with IC50 values ranging from 1.30 ± 0.01 to 35.80 ± 0.80 µM when compared to standard acarbose (an IC50 value of 38.60 ± 0.20 µM). Among the series, analogs 1 and 23 were found to be the most potent, with IC50 values of 1.30 ± 0.05 and 1.30 ± 0.01 µM, respectively. The structure-activity relationship (SAR) was mainly based upon bringing about different substituents on the phenyl rings. To confirm the binding interactions, a molecular docking study was performed.

Prevalence of obesity and central obesity among adolescent girls in a district school in Bangladesh.

INTRODUCTION: The prevalence of childhood obesity has increased over the last two decades. Obesity is a major risk factor for chronic diseases and plays a central role in insulin resistance or metabolic syndrome. METHODS: The aim of the study was to assess the prevalence of obesity and abdominal obesity by means of body mass index (BMI) and waist-to-height ratio (WHtR) in adolescent girls in a district school in Bangladesh. Based on age and sex specific BMI percentiles, the students were classified as normal weight (5(th)-<85(th) percentile), overweight (85(th)-<95(th) percentiles), and obese (≥95(th) percentile). Central obesity was categorized as WHtR ≥ 0.5. Adolescent girls (aged 9-17 years) attending the sixth to twelfth grades (n = 501) in a Bengali medium school participated in the study. RESULTS: The prevalence of obesity and overweight were 23% and 14% among the girls. The prevalence of central obesity was 26%. Around 14% of girls in the normal weight group were centrally obese. There was a significant relationship between WHtR and BMI status (P = 0.0001). CONCLUSION: Our study provides evidence showing a high prevalence of overall and central obesity in adolescent girls in our population. We emphasize the need for further large scale surveillance programs and preventive strategies in our population to reduce the incidence of obesity.

Synthesis of novel bisindolylmethane Schiff bases and their antibacterial activity.

In an effort to develop new antibacterial drugs, some novel bisindolylmethane derivatives containing Schiff base moieties were prepared and screened for their antibacterial activity. The synthesis of the bisindolylmethane Schiff base derivatives 3-26 was carried out in three steps. First, the nitro group of 3,3'-((4-nitrophenyl)-methylene)bis(1H-indole) (1) was reduced to give the amino substituted bisindolylmethane 2 without affecting the unsaturation of the bisindolylmethane moiety using nickel boride in situ generated. Reduction of compound 1 using various catalysts showed that combination of sodium borohydride and nickel acetate provides the highest yield for compound 2. Bisindolylmethane Schiff base derivatives were synthesized by coupling various benzaldehydes with amino substituted bisindolylmethane 2. All synthesized compounds were characterized by various spectroscopic methods. The bisindolylmethane Schiff base derivatives were evaluated against selected Gram-positive and Gram-negative bacterial strains. Derivatives having halogen and nitro substituent display weak to moderate antibacterial activity against Salmonella typhi, S. paratyphi A and S. paratyphi B.

Synthesis and in vitro urease inhibitory activity of N,N'-disubstituted thioureas.

Thiourea derivatives (1-38) were synthesized and evaluated for their urease inhibition potential. The synthetic compounds showed a varying degree of in vitro urease inhibition with IC50 values 5.53 ± 0.02-91.50 ± 0.08 µM, most of which are superior to the standard thiourea (IC50 = 21.00 ± 0.11 µM). In order to ensure the mode of inhibition of these compounds, the kinetic study of the most active compounds has been carried out. Most of these inhibitors were found to be mixed-type of inhibitors, except compounds 13 and 30 which were competitive, while compound 19 was identified as non-competitive inhibitor with Ki values between 8.6 and 19.29 µM.

Acylhydrazide Schiff bases: DPPH radical and superoxide anion scavengers.

Acylhydrazide Schiff bases 1-27 were evaluated for their in vitro DPPH radical and superoxide anion scavenging activity. They showed a varying degree of DPPH radical scavenging activity with IC(50) values between 31.25-473.59 µM. Compounds 8, 2, and 10 have IC(50) values 31.25 ± 1.32, 34.40 ± 0.66, and 37.24 ± 0.4 µM, respectively. Standard npropylgallate showed an IC(50) value 30.12 ± 0.27 µM. Acylhydrazides 1-27 exhibited in vitro superoxide anion scavenging activities with IC(50) values in the range of 175.6-450.89 µM. Results demonstrated that acylhyrazides 8, 2, and 10 have DPPH scavenging activity, comparable to standard n-propyl gallate while acylhyrazides 1-27 were found to be less superoxide anion scavenging active than the standard n-propyl gallate (IC(50) = 106.34 ± 1.6 µM).

Synthesis and in vitro leishmanicidal activity of disulfide derivatives.

Disulfides 1-30 have been synthesized and their in vitro leishmanicidal activity has been evaluated. Compounds 18 (IC50 = 2.70 ± 0.044 µM), 19 (IC50 = 2.85 ± 0.02 µM), 20 (IC50 = 2.92 ± 0.01 µM), 26 (IC50 = 3.69 ± 0.01 µM), 21 (IC50 = 4.45 ± 0.029 µM), and 29 (IC50 = 4.46 ± 0.025 µM) showed a remarkable leishmanicidal activity if compared with standard pentamidine (IC50 = 5.09 ± 0.04 µM). This study has discovered a series of possible molecules as antileishmanial agents. A structure-activity relationship study has also been carried out. The structures of all the synthesized compounds were identified by using spectroscopic techniques, including 1H-NMR and EI MS.