Terminalia ivoriensis A. Chev Combretaceae is a West African medicinal plant widely used by the Ijaws in the Niger Delta region of Nigeria for the treatment of malaria and management of erectile dysfunction in men. The Seeds were extracted using successive maceration at room temperature using n-hexane, dichloromethane and 70% methanol exhaustively and concentrated in vacuo, yielded 11.29, 10.03, and 0.954 percent of oily extracts respectively. The samples were subjected to physicochemical analysis and the following parameters were obtained; 0.9104-0.9303, 1.466-1.474, 38.15-58.34mg/KOH, 84.2-115mgKOH/g, 15.23-24g I2/100g and 26-80meq/Kg, for relative density, refractive index, acid value, saponification value, iodine value, peroxide value respectively. The GC-FID analysis of the oils showed that the oils contained 11 fatty acids and FT-IR result of the samples reveals that the oils contained fatty acid with a prominent characteristics peak at 1740 and 3004 cm-1 due to carbonyl and methoxyl group of esters respectively. The physicochemical analysis revealed that the oils could be used for skincare, emollient, vehicle for topical agents and as an insect repellant in agriculture because of the pungent and irritating odour produced by the oils.
Azibanasamesa D. C. Owaba*, Emmanuel I. Etim, Ekarika C. Johnson.
The literature survey done reveals that a simple, rapid and economic high-performance liquid chromatography (HPLC) method for simultaneous estimation of Azelastine HCl (AZE) and Fluticasone Furoate (FF) is yet not reported. So it is needed to develop and validate such method. Such stability-indicating HPLC method is developed by using a Inertsil, ODS, C18, 3V, 250×4.6mm, 5µ HPLC column, water: Acetonitrile (30:70) % V/V. The mobile phase A: 20.35mM Phosphate buffer (pH 3.0) and mobile phase B: 100% ACN is used with gradient at a constant flow rate of 1.0mL min-1. The composition was increased from0 to 15 min from 35 to 70% B and remained constant upto 20min. Further, decreased from 20 to 30 min to 35% with total run time of 30min at 236nm and successively validated. The main objective was to develop simultaneous method for estimation of AZE and FF with analysis of the stability profile of formulation under accelerated conditions. The retention time (Rt) of AZE and FF were observed as 8.5min and 18.5min respectively with the linearity range between 25-75µgmL-1 and 5-15µgmL-1 respectively. Forced degradation studies were performed on samples of AZE and FF Nasal Spray using acidic, basic, oxidative, thermal, photolytic and humid conditions. The resultant method was validated as per ICHQ2(R1) guidelines and successfully applied to the novel nasal spray for assessment of stability under accelerated conditions.
An improved process for amination of indanones for the synthesis of (R)-1-amino-2, 3 dihydro 1H-indene-4-carbonitrile, an important intermediate of pyridinyl-containing carboxamides as β2-adrenoceptor agonists for the treatment of inflammatory, allergic; Lung diseases; Respiratory distress syndrome1 and an important intermediate of Coronavirus disease 2019 (COVID-19) is an infectious disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and (R)-1-aminoindan which is key intermediate for Rasagiline (Azilect®) is a selective and irreversible monoamine oxidase B inhibitor, which is well tolerated, safe, improves motor symptoms, and prevents motor complications in Parkinson’s disease (PD)2, in a 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 TLC and HPLC.
An improved process for amination of 4-cyanoindanone for the synthesis of (S)-1-amino-2, 3 dihydro 1H-indene-4-carbonitrile, an important intermediate of Sphingosine-1-Phosphate receptor modulators, that are used for treatment of various neurodegenerative diseases has been developed. 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 TLC, Mass and HPLC.
An efficient Stereoselective reduction of 4-cyanoindanone for the synthesis of 1-hydroxy-2,3 dihydro-1H-indene-4-carbonitrile, has been developed. (S)-1-hydroxy-2,3 dihydro-1H-indene-4-carbonitrileplays an important role in synthesis of IDO1 inhibitors that are used for cancer treatment and chronic viral infections; synthesis of GPR40 receptor modulators for treating metabolic diseases, especially diabetes type 2; synthesis of pyrethroid compounds with insecticidal, nematocidal and acaricidal properties. Single step conversion was achieved using ketoreductase enzymes with better enantioselectivity and yield when compared to chemical processes. >96% chiral purity was obtained for (S)-alcohol using different ketoreductase enzymes, with 100% yield way better than that obtained in chemical route. This was further confirmed by TLC and HPLC.