Medicinal Chemistry

An efficient total synthesis of amentoflavone, a valuable natural product, utilizing Suzuki coupling with pinacolatoboronflavone derivatives and iodoflavone was reported for the first time in this work. The method can be applied to the synthesis of various other C-C biflavonoidsand biphenyls, therefore the current work could serve as an excellent solution to the availability of many bioactive natural biflavonoids.

Background: Carissa edulis is used traditionally for the treatment of HIV/AIDS symptoms, rheumatism, gonorrhea, syphilis, rabies, malaria, epilepsy, chronic joint pain, and as a diuretic.

Objective: The present study investigates the diuretic activity of different solvent fractions of 80% methanol Soxhlet extract of Carissa edulis root bark in normal wistar rats.

Materials and methods: The volumes of urine output and urinary electrolyte were the parameters determined by oral administration of single doses of different solvent fractions of 80% methanol Soxhlet extract of Carissa edulis root bark at three dose levels (50, 500 and 1000 mg/kg) in normal wistar rats.

Results: The petroleum ether and n-butanol fractions showed no significant effect on the urine output and urinary excretion of K+ and Cl- at all tested doses. Urinary excretion of Na+ was, however, affected by the petroleum ether fraction (p<0.002 at 1000 mg/kg) and n-butanol fraction (p<0.05 at 50 mg/kg; p<0.03 1000 mg/kg). The aqueous fraction significantly increased urine output in a dose dependent manner (p<0.005 at 50 mg/kg; p<0.001 at 500 and 1000 mg/kg). It also significantly increased urinary excretion of Na+ (p<0.006 at 500 mg/kg; p<0.001 at 1000 mg/kg) and Cl- (p<0.05 at 50 mg/kg; p<0.001 at 500 and 1000 mg/kg) in a dose dependent manner. Moreover, the aqueous fraction produced no acute toxicity at the assayed dose, which was also consistent with previous results from mice model.

Conclusion: These findings collectively indicate that aqueous fraction exhibited significant diuretic activity, providing evidence, at least in part, for its folkloric use.

Aryl urea is an entity which is being synthesized in many of its derivative form from past few years; the entity is major source of interest for many of medicinal chemist to explore its various biological activities. In present study, we review the chemistry of aryl urea and its pharmacological actions as an anticonvulsant, antimicrobial, antiviral andanti inflammatory agent by studying its various synthesized derivatives. This review can be helpful to develop various more new compounds possessing aryl urea moiety that could be better in terms of efficacy and lesser toxicity.

An atom economic and facile synthesis of novel thiadiazolidine-1-oxides has been achieved via using 1,3-dipolar cycloaddition reactions. The salient features of synthetic procedure are characterized by the good yields, high regio- and stereoselectivity, one-pot procedure, and operational simplicity. The regiochemistry and structures of the cycloadducts were determined by using various spectroscopic techniques (IR, 1H-NMR, ESI-MS) and elemental analyses data.

As a part of an ongoing research program to achieve new chemical entities suitable for development as new class of antimicrobial agents, the present work describes the design and synthesis of a new series of substituted-1-methyl- 1,2,4-triazolo[4,3-a]quinoxalines, The newly synthesized compounds were screened for their in vitro antimicrobial activity. The results revealed that the compounds demonstrated significant activity against Gram negative bacteria. Compounds 3 and 11b exhibited twice the activity of ampicillin against Pseudomonas aeruginosa, while compounds 4, 5b, 7, 9a, 10d, 11a, 11c and 12 were equipotent to ampicillin. On the other hand, the tested compounds demonstrated mild antifungal activity. Compound 11d exhibited nearly one-half the activity of clotrimazole against Candida albicans. The structures of the synthesized compounds have been confirmed by elemental analyses, IR, MS, 1H-NMR and 13 C-NMR spectral data.

1,3-diaryl-1-propen-3-ones 1a-h, were used as building blocks for a large range of nucleoside analogs incorporating five and six-membered heterocyclic rings. Heterocyclic compounds incorporating aromatic moieties (2-11) and their N-nucleoside analogs (13-20) were synthesized. New compounds were evaluated for their potential antimicrobial, antifungal activities and for their in vitro cytotoxic activity against three cell lines: human breast cancer cell line (MCF- 7), colon carcinoma cells (HCT) and human epidermid/arynx carcinoma cell line (HEp2).