Potential biologically active agents, XXVI. Synthesis of substituted 3-benzoyl/phenoxyacetylhydrazono-5-methyl-2-indolinones.
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Biomedical subjects
Publications and source records attributed to R K Pandey.
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The anti-cancer activity of dimers joined with ether, ester or carbon-carbon bonds by photodynamic therapy (PDT) was compared by using DBA/2 mice transplanted with SMT/F tumors. Dimers with ether and carbon-carbon linkages were found to be more effective than those linked with ester bonds. Variation of the substituents at peripheral positions made a significant difference in in vivo efficacy. Among the ether and carbon-carbon linked dimers, the divinyl analogs were found to be most effective. The preliminary in vivo results also suggest that the position(s) of the hydrophilic substituents in the molecules make a remarkable difference in photosensitizing activity. An unsymmetrical dimer with an amide linkage, obtained from 2-(1-hexyloxyethyl)-2-devinyl pyropheophorbide-a (HPPH) was found to be less effective than HPPH.
A series of mono- and disubstituted cationic porphyrins (1-8) were synthesized and investigated for their ability to bind and cleave DNA in the presence of light. In these porphyrins, the cationic substituents were introduced at various peripheral positions, i.e., the non-meso positions of the porphyrin system. The modes of binding of these porphyrins to DNA were investigated by UV-vis spectroscopy, circular dichroism, and an unwinding assay. The intrinsic binding constants Kb of these porphyrins to calf thymus DNA was found to be in the range 10(4)-10(5) M-1. Two of the zinc(II) complexes of non-meso-substituted cationic porphyrins (5 and 8) were found to bind to DNA via intercalation, which is in contrast to the previously reported outside-binding mode for the Zn(II) complexes of meso-substituted cationic porphyrins. Except for monocationic porphyrin 1 and Ni(II) dicationic porphyrin 6, all the other porphyrins were found to be efficient photocleavers of DNA. The DNA photocleavage characteristics of this series of cationic porphyrins were found to depend on the structural characteristics of the poprhyrins such as (a) length of the side chain of the cationic substituents (2 vs 4), (b) the position of the side chain on the porphyrin ring (4 vs 7), and (c) the presence of the chelating metal in 3, 5, and 8 as compared to the nonmetallo porphyrins 2, 4, and 7, respectively.
UNLABELLED: The cleft lip and palate patients usually present a number of problems viz. altered oral anatomy leading to changes in oral physiology diminishing the self-cleansing ability of individual. The handicapped children are unable to maintain their oral hygiene properly. The present study was formulated with the aim that does normalization of oral anatomy have its effect on improvement of oral hygiene? An assessment of oral hygiene index-simplified was performed between preoperative and postoperative values in the same patient at KGMU and KGDU. A total of 50 cases were recorded in two groups of 25 each: (i) 6 years. The observations are statistically analyzed by paired 't' test to get the significance of results. RESULTS: The data analyzed showed the significant decrease in oral hygiene indices observed in both groups. A relative significance in oral hygiene status following surgery was observed. Both groups expressed greater significance when compared pre and postoperatively which is indicative of considerable improvement of oral hygiene after surgical correction. The study concludes that oral hygiene improves more in older cleft lip-palate cases following reconstruction of palatal vault, premaxilla and anterior lip seal by secondary bone grafting method when compared with oral hygiene indices results in primary periosteoplasty cases. The surgical correction of cleft lip palate enhances self-cleaning ability and better compliance to maintain oral hygiene in children as the age advances.
Appropriate ventilatory intervention is life saving in acute respiratory distress syndrome (ARDS). Pressure controlled inverse ratio ventilation (PC-IRV) is the likely mode of ventilation benefiting in extreme conditions of ARDS. However, guidelines when to start PC-IRV is not yet well defined. The ventilation-related dilemma, which we faced in two illustrative cases of ARDS are presented. The first patient presenting clinically with ARDS but with high peak airway pressure (PIP) and low dynamic lung compliance, PC-IRV helped in reducing PIP, improved haemodynamics and the oxygenation of blood. In second patient with similar clinical presentation of ARDS, where although PIP was high but the dynamic compliance was better, the PC-IRV caused deterioration in PaO2. Here, patient rather did better with high PEEP (15 cm H2O) and usual I: E ratio (1:2). It is probable that the dynamic lung compliance (< 20ml/cmH2O), PIP (> 50 cm H2O) at conventional I: E ratio (1:2) ventilation (10 ml/kg) with hypotension might form the basis to develop a scoring system for guidance to switch over to PC-IRV ventilation. Further randomised prospective controlled clinical trials will then be required to establish indication to start PC-IRV in ARDS.