Carbazole is an aromatic heterocyclic organic compound. It has a tricyclic structure, consisting of 2 six membered benzene ring fused on either side with a five membered nitrogen containing ring. Carbazole and its derivatives are an important class of nitrogen containing heterocyclic compounds that are wide spread in nature. The N-substituted derivatives have acquired the attention of researchers due to their therapeutic potential. Hence here an attempt is made to synthesize some novel N- substituted carbazole derivatives for its antitumor activity.
A novel and easy enzymatic process for the stereoselective reduction of 1-Hydroxypropan-2-one for the synthesis of (R)-propane-1, 2-diol (Scheme-1) was identified. (R)-propane-1, 2-diol can serve as a key intermediate of many pharmaceutically active compounds. Single step conversion was achieved using Ketoreductase enzymes with high enantioselectivity and better yield in comparison with chemical process. 100% chiral purity has been obtained for the enantiomerically pure intermediate, confirmed by both TLC and Chiral HPLC.
A novel enzymatic process for amination of 1-hydroxypropan-2-one for the synthesis of (R)-2-aminopropan-1-ol (Figure No.1) was identified. (R)-2-aminopropan-1-ol can serve as a key intermediate of many pharmaceutically active compounds and ithas been used as a derivatizing agent for gossypol during the analysis of gossypol enantiomers in cottonseed by high-performance liquid chromatography1. Single step complete conversion was achieved using Transaminase enzymes with high enantioselectivity and better yield in comparison with chemical processes. 100% chiral purity has been obtained for the enantiomerically pure intermediate, confirmed by both TLC and Chiral HPLC. Performed same reaction in flow reactor and observed lesser time for same reaction.
A novel and simple Zero order derivative spectroscopic method was developed and validated of Diltiazem hydrochloride an absorption maximum at 236nm using distilled water. The Linearity was found to be in the concentration range of 2-10μg/ml and the correlation coefficient was found to be 0.999 and it has showed good linearity, reproducibility, precision in this concentration range. The regression equation was found to be Y = 0.568x + 0.009. The % recovery values were found to be within 100.8-101.37% showed that the method was accurate. The LOD and LOQ were found to be 0.00871 and 0.02640μg/ml respectively. The %RSD values were found to be less than 2. The developed method was validated according to ICH guidelines for linearity, accuracy, precision and ruggedness. Limit of detection and limit of quantitation. The developed method was successfully applied for the quantitative estimation of Diltiazem hydrochloride.
C. S. Jagadeesh*, V. K. Girish, A. R. Sowjanya, M. S. Prasanth Gowda.
A novel series ofsome Xanthone conjugated amino acids derivatives as depicted as in the scheme and all are synthesized by conventional method. The synthesized compounds were characterized by physical methods like melting point, Rf value, % yield and solubility. Synthesized structures are conformed by UV, FT-IR, 1HNMR and MASS spectral analysis. The synthesized analogs were evaluated for their antioxidant activity by DPPH and H2O2 methods. From the results compound 3b, 3e and 3i exhibited significant antioxidant activity due to presence of higher hydrophobic planar substitutions.