Convenient synthesis, characterization and biological evaluation of novel 1-phenylcyclopropane carboxamide derivatives.

Small, strained ring molecules of phenylcyclopropane carboxamide have rigid, defined conformations and unique electronic properties. For these reasons many groups, seek to use these subunits to form biologically active compounds. Herein we report a generally applicable approach for preparing a small cyclopropane ring containing 1-phenylcyclopropane carboxamide derivatives to a wide range of the different aromatic compounds by α-alkylation of 2-phenyl acetonitrile derivatives with 1, 2-dibromo ethane in good yields followed by the conversion of cyano group to acid group by the reaction with concentrated hydrochloric acid. This obtained acid derivative undergoes acid amine coupling with various Methyl 2-(aminophenoxy)acetate to form 1-Phenylcyclopropane Carboxamide. These compounds possess distinct effective inhibition on the proliferation of U937, pro-monocytic, human myeloid leukaemia cell line while these compounds did not show cytotoxic activity on these cells. The structure-activity relationships of these compounds are discussed.

First report on co-isolation and whole-genomic characterisation of mammalian orthorubulavirus 5 and mammalian orthoreovirus type 3 from domestic pigs in India.

During a surveillance study to monitor porcine epidemic diarrohoea virus and transmissible gastroenteritis virus in India, a total of 1043 swine samples including faeces (n = 264) and clotted blood (n = 779) were collected and tested. Five samples (four faecal and one serum) showed cytopathic effects in Vero cells. Transmission electron microscopy of infectious cell supernatant revealed the presence of two types of virions. Next-generation sequencing (de novo) allowed the complete genome sequence of mammalian orthorubulavirus 5 (MRuV5; 15246 bp) and that of all 10 gene segments of mammalian orthoreovirus to be determined. Genetic analysis of MRuV5 revealed grouping of the Indian MRuV5 with isolates from various mammalian species in South Korea and China, sharing more than 99% nucleotide sequence identity. The deduced amino acid sequences of the HN, NP, and F genes of MRuV5 isolates showed three (92L, 111R, 447H), two (86S, 121S), and two (139T, 246T) amino acid substitutions, respectively, compared to previously reported virus strains. Phylogenic analysis based on S1 gene sequences showed the Indian MRV isolates to be clustered in lineage IV of MRV type 3, with the highest nucleotide sequence identity (97.73%) to MRV3 strain ZJ2013, isolated from pigs in China. The protein encoded by the MRV3 S1 gene was found to contain the amino acid residues 198-204NLAIRLP, 249I, 340D, and 419E, which are known to be involved in sialic acid binding and neurotropism. This is the first report of co-isolation and whole-genomic characterisation of MRuV5 and MRV3 in domestic pigs in India. The present study lays a foundation for further surveillance studies and continuous monitoring of the emergence and spread of evolving viruses that might have pathogenic potential in animal and human hosts.

Efficacy of misoprostol administration 24 hours after mifepristone for termination of early pregnancy.

INTRODUCTION: Mifepristone and misoprostol are the two drugs which are given at 36-48 h interval for medical abortion. This study was designed to study the efficacy of early administration of misoprostol (24 h after mifepristone) for medical termination of pregnancy less than 9 weeks and to compare this with standard protocol of mifepristone misoprostol combination at 48 h interval. MATERIALS AND METHODS: Subjects for this single center prospective randomized case-control study were enrolled from the family planning outdoor patient department at our hospital with gestational age of less than 9 weeks. All subjects initially received 200 mg of oral mifepristone and then were randomly assigned to receive per vaginal 400 µg misoprostol at 24 h (study group) and 48 h (control group). They were then followed up after 14 days with transvaginal sonography to confirm completion of expulsion. Treatment was considered failed if surgical evacuation was needed for any indication. Primary outcome measure was success rate of the two treatment regimens. RESULTS: Totally, 200 subjects were randomly allocated to each treatment arm (100 each). Complete expulsion was seen in 94% (94/100) in study group and 95% (95/100) in control group according to intention to treat analysis (P value ns). According to per protocol analysis success rate in study group was 93.6% and 94.3% in control group (P value ns). High failure rate after 7 weeks period of gestation in both the study and control group was found (26.3% and 30.0%; P value ns). Adverse effects were mostly similar in both the groups. CONCLUSION: Efficacy of mifepristone misoprostol combination at 24 h interval was similar to that at 48 h interval for medical abortion of pregnancy less than 9 weeks without compromising the safety .

Evaluation of mifepristone as a once a month contraceptive pill.

OBJECTIVE: The purpose of this study was to assess the efficacy and safety of mifepristone as a contraceptive pill. STUDY DESIGN: A prospective case-control study was conducted in a tertiary care center of North India. The study group (n = 86) was given 200-mg mifepristone tablets on the 16th day of the menstrual cycle. The control group (n = 92) received combined oral contraceptive (COC) as per protocol. Subjects were followed for drug compliance, satisfaction, side effects, and failure. RESULTS: Acceptability of mifepristone was significantly higher in educated population (P < .001), with fewer side effects (P = .001), good satisfaction (P < .001), and higher compliance rate (P = .05). The oral contraceptive pill group had higher adverse biochemical parameters. CONCLUSION: Mifepristone can be used as a monthly contraceptive pill effectively.