Molecular modification for Synergism against Drug Resistant Bacteria: A Combinatorial Synthesis Approach using Calitropis Procera Extract with Ampicillin.

Identifying novel methods to develop lead compounds for selectivity, efficacy, and safety for a clinical trial candidate remains a scientific challenge, Natural products offer novel pharmacophores, chemotypes, and scaffolds that can be amplified into efficient drugs for various infections and disease. This study present a simple, basic and eco-friendly method for boosting the antimicrobial activity of two less effective antimicrobial agents to obtain repetitive constant synergism in combat drug resistant clinical bacteria. Aqueous extract of fresh C. procera leaves and flowers was made to react with 1 mg/mL ampicillin solution under heat and acidic condition. The prepared sample was synergistic and highly susceptible to resistant S. aureus and Salmonella spp, moving their zones of inhibition from 0 mm to 16.8 mm and from 5.3 mm to 21.4 mm respectively. Gas chromatography mass spectrometry, GC-MS analysis reveals the presence of 53 phytochemicals, oleic acid 13.04 %, 1,1,1,3,5,5,7,7,7-Nonamethyl-3-(trimethylsiloxy)tetrasiloxane 9.50 %, 9-Heptadecanone 3.75%, Cystamine 3.35 % and Tetrahydro-4H-pyran-4-ol 3.15 % were where the five (5) most abundant phytochemicals. Eighteen (18) out of the 53 phytochemicals were reported to have known biological activities thus, some undergo molecular transformation to a new molecule and/or analogue to existing biologically active compound due to the reaction condition used. Farnesol, Cystamine, Cystine, Metaraminol, dl-phenylephrine and two different substituted amphetamine compounds were discovered. Three (3) phytochemicals present were reported to exhibit anticancer properties (Farnesol, 4-amino-1-pentanol and the of imidazole derivative similar to the drug Ribavir). The results of this study reveals that medicinal plants phytochemicals can be used in synthetic combination reactions with themselves or other drug/reagent to produce vast array of compounds with good pharmacological activities or compounds which can be used as starting material, intermediates or derivatives in pharmaceutical production.