A drug-like molecule could be considered as a congregation of small fragments which are chemically linked to each other and the biological effect of such molecule is due to the contribution of these small fragments working together. This molecular unit has been constructed gradually through a multi-step synthesis route. Assessment of the biological activity of all the intermediary compounds of a multi-step synthesis process helps to track down the emergence of biological activity alongside the synthesis process and the results provide valuable clues about the SAR of the compounds. Furthermore unanticipated findings may be encountered if such approach is exercised. A two-step synthesis route was employed to make a few 2-aminopyrimidines from their corresponding enamine precursors. Both aminopyrimidines and enamines were subjected to antiproliferative and antimicrobial tests. Hit compounds with acceptable activities were found in both aminopyrimidine and enamine series. With respect to antimicrobial activity, enamine series were found more promising. This experiment sets an example for the applicability of our new approach called "Synthesis route-based hit identification" as a tool in medicinal chemistry to increase the hit rate in drug discovery processes.

L-asparaginase (L-asparagine amido hydrolase, E.C.3.5.1.1) is a promising chemotherapeutic agent which plays a vital role in treatment of a variety of lymphoproliferative disorders, lymphosarcoma and acute lymphoblastic leukemia in particular. An attempt is made in the present study to optimize the production of L-asparaginase by Fusarium equiseti using soya bean meal under solid state fermentation (SSF). The maximum yield of L-asparaginase (8.51 IU) was achieved with the following optimized fermentation parameters: incubation period (48 hrs), initial moisture content (70% v/w), particle size (3 mm), inoculum volume (20%), supplemented with glucose (0.5% w/v), ammonium sulphate (0.5% w/v) and yeast extract (0.5% w/v).

Candidiasis is recognized worldwide as an opportunistic infection. The severities of the infection increase in immunosuppression conditions with possible occurrence of visceral mycoses and sometimes are widespread and systemic. Increased resistance in strains of Candida albicans is a major obstacle to antifungal therapy. The aim of this study was to correlate the chemical structure of compounds with experimental data from biological activity anti-Candida albicans. We performed classical QSAR for a series of twenty derivatives of ketone -β unsaturated against resistant strains of Candida albicans. Ninety-four descriptors were calculated and multiparameter model was obtained through Partial Least Squares (PLS) method. The results showed that thermodynamic, dimensional and steric parameters are important in elucidating of action mechanism compounds. Four descriptors (molar refractivity, ionization potential, molecular length and Verloop B4) were selected and good model (n= 20; R2 = 0.776; SEC = 0.229; F(3,16) = 14.172; Q2LOO = 0.609; SEV = 0.295; Q2pred = 0.709; SEP = 0.091; k = 0.709; k’ = 1.00; ׀R20 – R’20׀ = 0.0009) was built with three latent variables describing 96.14% of the original information. Leave-N-out cross validation and Y-randomization analysis were performed in order to confirm the robustness of the model. The proposed model may provide a better understanding of the anti-Candida albicans activity of chalcones and can be used as guidance for proposition of new chemopreventive agents.

In past few years the use of organometallics in medicinal purpose takes the full attention of researchers to work in this field. The present work deals the synthesis of some new organobismuth amides having a pyramidal geometry as resulted by their characterization with the help of different techniques along with spectral analysis. The compounds are also screened for their biological studies against different bacterial and fungal strains along with human breast adenocarcinoma and mammary cancer cell lines in-vitro and the results are surprising that these compounds plays significant role in biomedicinal activities.