3D-QSAR-based design, synthesis and biological evaluation of 2,4-disubstituted quinoline derivatives as antimalarial agents.

2,4-Disubstituted quinoline derivatives were designed based on a 3D-QSAR study, synthesized and evaluated for antimalarial activity. A large dataset of 178 quinoline derivatives was used to perform a 3D-QSAR study using CoMFA and CoMSIA models. PLS analysis provided statistically validated results for CoMFA (r2ncv = 0.969, q2 = 0.677, r2cv = 0.682) and CoMSIA (r2ncv = 0.962, q2 = 0.741, r2cv = 0.683) models. Two series of a total of 40 2,4-disubstituted quinoline derivatives were designed with amide (quinoline-4-carboxamide) and secondary amine (4-aminoquinoline) linkers at the -C4 position of the quinoline ring. For the purpose of selecting better compounds for synthesis with good pEC50 values, activity prediction was carried out using CoMFA and CoMSIA models. Finally, a total of 10 2,4-disubstituted quinoline derivatives were synthesized, and screened for their antimalarial activity based on the reduction of parasitaemia. Compound #5 with amide linker and compound #19 with secondary amine linkers at the -C4 position of the quinoline ring showed maximum reductions of 64% and 57%, respectively, in the level of parasitaemia. In vivo screening assay confirmed and validated the findings of the 3D-QSAR study for the design of quinoline derivatives.

Characterization of a novel seed protein of Prosopis cineraria showing antifungal activity.

An antifungal protein with a molecular mass of 38.6 kDa was isolated from the seed of Prosopis cineraria. The protein was purified using ammonium sulphate precipitation, ion exchange chromatography and gel filtration. The antifungal activity of purified protein was retained up to 50 °C for 10 min. The MALDI TOF mass spectroscopy revealed 15 assorted peptides. The molecular weight of the antifungal protein is different from antifungal proteins reported in seeds of other leguminous plants. The purified protein exerted antifungal activity against post-harvest fruit fungal pathogens Lasiodiplodia theobromae and Aspergillus fumigatus, isolated from the rotten fruits. The antifungal properties of this novel antifungal protein can be potentially exploited to manage post-harvest fungal disease of fruits through alternative means to reduce use of hazardous chemicals.

Suicide and family constellation in India.

The article first outlines historical suicide patterns. Case histories mirror a wide range of frustrations and family tensions in our present generation and show the socioeconomic, sociophilosophical, and cultural changes that are sweeping Indian society and are greatly adding to the tensions in life, resulting in a substantially higher occurrence of suicide. Varieties of family patterns are described that predispose an individual to suicidal behavior. It has been stressed that the single most important variable in the development of suicidal behavior remains the family unit.

Comparison of three treatment regimes in schizophrenia.

90 schizophrenic patients in three regimes of thirty patients each, were treated for a period of three weeks with haloperidol alone, E.C.T. alone and E.C.T. + haloperidol in combination respectively. Rating them on R. P. scale (Rockland and Pollin, 196a) & Disability Rating Scale (Gautam, 76) showed that the E.C.T. + haloperidol receiving group was significantly better on several measures on day 8 & day 15 and also had an earlier onset of beneficial responses on "Affect & Mood" & on scores of "General appearance and behaviour". However, at the end of three weeks these differences disappeared and the three groups did not differ significantly.

Post partum psychiatric syndromes-an analysis of 100 consecutive cases.

100 consecutive out patients with onset of Psychiatric illness within 40 days of child birth were studied by using Indian Psychiatric Interview Schedule and a specially designed Proforma. It was found that post partum psychiatric syndromes occurred most frequently in patients less than 25 years of age. Stress of Physical illness was present in a considerably high number of patients (74%). In 66% the Psychiatric illness was associated with first child birth and risk of Puerperal Psychosis in subsequent deliveries was found to be 32%.; Onset of illness is seen most frequently (85% cases) within 3 weeks of child birth. The Diagnostic breakup showed Schizophrenic reactions (68%) affective disorders (25%) and neurotic reactions (7%). Findings have been discussed.