医薬品化学

2H-1-benzopyran-2-one (Coumarin), an important oxygen heterocyclic scaffold, widely distributed throughout the plant kingdom, displayed a wide range of potential biological activities such as anti-microbial, anti-inflammatory and antioxidant activities. In this paper, we have synthesized a novel class of 3,7-disubstituted 2H-1-benzopyran- 2-one derivatives (3aa-3hb) bearing a basic ether side chain at C-7 and a substituted phenyl ring at C-3 of the coumarin ring. These compounds have been evaluated for anti-microbial (antibacterial/antifungal) activities. Some of the compounds 3ac, 3ae, 3bb, 3bc have shown significant anti-fungal activities against selective strains. Compound 3ae and 3bc with the MIC values of 1.56 μg/mL displayed better antifungal activity than fluconazole against Trichophyton mentagrophytes.

Introduction: Nutritional deficiency, especially iron deficiency is the most common etiological factor for anemia, particularly in adolescent girls when the requirement for iron increases tremendously to physiological need.

Aim: This study not only would highlight the burden of nutritional anemia in them, but also it would aid in drawing recommendations and rendering suggestions to assess and maneuver the existing schemes. The aim was to estimate the prevalence of anemia among school going girls to associate anemia to their demographic profile and nutritional status.

Materials and methods: This was a community based cross sectional observational study. The demographic profile was collected followed by estimation of Iron profile and Vitamin B12 levels estimation among 382 adolescent girls aged 10 to 18 years, in schools at rural area of Raipur district, India.

Results: Iron and vitamin B12 deficiency was present in 11% and 58% respectively. Statistically significant association was observed between severity of anemia serum ferritin (p<0.01) but not with serum vitamin B12 levels.

Conclusion: Anemia in adolescent girls was found to be very common. Moreover, Vitamin B12 deficiency was more common than iron deficiency in adolescent girls. There is need to shift the focus from old paradigm of iron deficiency anemia to other forms of anemia basically vitamin B12 deficiency anemia, as observed from this study.

A series of spiro-indolin-2-one derivatives were designed and synthesized as p53-MDM2 binding inhibitors. Though p53-MDM2 binding inhibitory and activities against p53 wild-type cell lines of most compounds were not that promising, some obtained structures showed moderate to strong inhibitory activities (IC50<0.08 μM) against p53 mutant cell lines (SW620), suggesting that these compounds may have different modes of action to p53 pathway, further studies on treatment of p53 mutant tumors are under investigation.cc

Osteopontin (OPN) is an integrin-binding ligand belonged to the family of N-linked glycoprotein, which is produced by activated mononuclears and linking systemic inflammation, atherosclerosis, and vascular remodeling. There is a large body of evidence regarding the controversial role of OPN in vascular calcification, while OPN is considered a pretty accurate biomarker of vascular remodeling with promising predictive value for cardiovascular (CV) disease and CV events. The short communication depicts the discussion about some controversies regarding exclusive role of OPN in several phases of vascular remodeling.

A series of potential biologically active substituted 2,5-di(4 aryloylaryloxymethyl)-1,3,4-oxadiazoles 9a-j were evaluated for its potential antimicrobial activity comparing with the standard drugs-Streptomycin and Ketoconazole respectively. Compound 9a with fluoro group exhibited highest activity against both gram-positive and gramnegative bacteria. Compounds 9a with fluoro group and 9c with fluoro and bromo showed good activity against antifungal activities.