Mini Reviews in Medicinal Chemistry - Volume 18, Issue 9, 2018

Matrine-type alkaloids belong to quinolizidine analogues from Sophora flavescens Ait, Sophora subprostrata and Sophora alopecuroides L. possess numerous therapeutic properties and have attracted continuous attention over the past few decades. In order to improve the activities and amplify their applicants, many matrine-type derivatives have synthesized and evaluated for their biological activities in recent years. These structural modifications have resulted in stronger activities and improvement of the pharmacokinetic properties. The structure and activity relation studies based on matrine- type semi-synthetic derivatives have immensely contributed to the understanding of their mechanism of actions and molecular targets. This review mainly summarizes recent progress in the structural modifications of matrine-type alkaloids based on the alteration of C-13 or C-14 position, opening D ring, fusing D ring and structural simplification.

Steroid and its derivatives have been proved to have important and diverse biological functions, which present the wide spectrum of biological activities such as antitumor, antiviral, antibacterial, antimicrobial, antifungal, antioxidant, insecticidal, aromatase inhibitors, 5α-reductase inhibitors and neuromuscular blocking agents etc. Versatile features of steroid-derived compounds have emerged, so the aim of the present paper is to review the recent advances of steroid-based derivatives mainly focused on their structures and biological applications, which can be employed for further development to discover potential drug candidates.

Chagas disease is caused by the parasite Trypanosoma cruzi and is regularly found among particular people living in Central and South America. Paediatric Chagas disease occurs in 1-10% of infants of infected mothers. The major important point considered in the treatment of congenital Chagas disease focuses on killing the parasite in acute infection and managing signs and symptoms in later stages. Nowadays, two drugs benznidazole and nifurtimox are currently available in the market for the treatment of paediatric Chagas disease.

The triazolopyrimidine ring is a ubiquitous structural feature of many active compounds with diversified pharmacology efficacy. These structures have aroused our / researchers interests in the development of novel compounds with anticancer, anti-inflammatory, antibacterial, antifungal, and other activities. A large number of published literatures were reviewed during the last few decades. This review contains various pharmacological and agrochemical activities of triazolopyrimidine and it may be regarded as the lead compound for the new research towards future medicinal and agrochemical development.

Background: Several commercial drugs utilized in the treatment of HSV containing pyrimidine moiety. Because of the ineffectiveness of virus drugs due to the resistance of the patient's immune system, there is a pressing need to prepare new compounds that are effective in the treatment of various viruses. Results: Merged pyrimidine derivatives were designed by one pot synthesis of pyrimidinethione derivative with halogenated compounds. The structure of all prepared compounds was characterized by their spectroscopic data and also, their ability to inhibit the in vitro replication of HSV-1 was estimated. Amongst the tested compounds 2-acetyl-3-methyl-5-(p-tolyl)indeno[1,2-d]thiazolo[3,2- a]pyrimidin-6(5H)-one (9b) and ethyl 3-methyl-6-oxo-5-(p-tolyl)-5,6-dihydroindeno[1,2-d]thiazolo- [3,2-a]pyrimidine-2-carboxylate (9c), caused viral inhibition over 90%. Furthermore, the selectivity indices of the tested compounds are high and have weak cytotoxicity (all samples were checked, not chosen on cytotoxicity basis, we only utilize secure concentrations of every compound). Conclusion: We succeeded in this context to synthesize a new series of potent fused pyrimidine derivatives as anti-HSV-1.

Background: A library of compounds related to the new benzoxepine-oxime-1,2,3-triazole hybrid was created as probable antibacterial agents. Their synthesis involved a Cu-catalyzed azidealkyne cycloaddition (CuAAC) as a key step to construct the desired 1,2,3-triazole ring. Thus the click reaction between the appropriate alkyne containing the benzoxepine-oxime framework with aryl azides afforded the target compounds in good yields. Method: To assess their antibacterial properties all the synthesized compounds were tested using four bacterial strains consisting of one Gram-positive and three Gram-negative species. Results & Conclusion: These compounds were generally found to be effective towards gram -ve species and one of them showed selective cytotoxicity against lung cancer cell line.