Medicinal Chemistry

The synthesis of enantioselective β-amino acids is being reported in this review on account of their significant properties as proteinogenic, non-proteinogenic role such as neurotransmitter, biosynthesizer and nutritional supplementing materials etc. They are extensively used as chiral starting materials, auxiliariesand catalystsin organic synthesis. According to literature evidences, extensive research has been carried out to develop the methodologies for the synthesis of stereoselective β-amino acids. In this review, we describe recent advances in synthetic routes of enantioselective β-amino acids derivatives with chemical reactions during the last decades and to provide the most suitable route of their synthesis to compete the future challenges.

Steroidsform a group of secondary metabolites having diversity in their structure and biological functions. These natural products, although often linked with the deleterious effect on health, have many medicinal applications and the research is still continued in search of these secondary metabolites as potential lead in drug design/discovery. The Aim of this review is to systematically compile the basic information related to this class of natural products.

Benzimidazoleis an important pharmacophore which was included in several biologically active compounds resulted in the development of several classes of drugs. This review discusses the synthesis of benzimidazole derivatives as a target agents for antidiabeticby different mechanism such as peroxisome proliferator – activated receptor α transcriptional activity, glycosidases receptor, dipeptidyl peptidase IV, glucokinase, human glucagon receptor (hGCGR) antagonist , aldose reductase enzyme and stearoyl- CoA desaturase.

Rhipicephalus microplus is a monoxenous species whose main hosts are bovines, leading to considerable losses in cattle production worldwide. In addition, this tick is the transmitter of pathogenic agents responsible for the bovine babesiosis and anaplasmosis (BBA) complex. These ectoparasites are still mainly controlled with chemical products. The constant exposure of ticks to acaricides, associated with the lack of adequate application procedures, accelerates the selection pressure of resistant individuals in the population, inevitably increasing resistance, as reported by many authors around the world. This article presents current information about the resistance situation of R. microplus in Brazil. We identify and discuss the main chemical bases being used as a means to guide new research.

Thalidomide is an immunomodulatoryagent with anti-inflammatory activity, however it may also cause serious side effects. New compounds derived from thalidomide effective in modulating inflammatory responses and having an improved safety profile is being investigated. In this study, two thalidomide analogs, GI-16 and SC-15, were evaluated using the carrageenan-induced paw swelling and the lipopolysaccharide (LPS)-induced lung inflammation in mice. Acute and sub-chronic toxicity of the compounds were investigated in blood and serum samples of Wistar rats by measurements of hematological and biochemical parameters. Histopathological analyses were conducted to assess inflammatory cell infiltration in heart, liver and kidneys. Our results show that treatment with GI-16 and SC-15 reduced the carrageenan-induced paw edema over a 24 hour period. GI-16 and SC-15 treatments inhibited LPS-induced TNF-α and IL-6 in lung homogenates. In contrast, thalidomide and SC-15 enhanced IL-10 (p<0.05). Histopathological analysis showed reduction in LPS–induced lung inflammation after treatment with GI-16 and SC-15. Wistar rats treated with the compounds did not develop any clinical signs of acute or sub-chronic toxicity. No mortality occurred in both control and treated animals and body weight gain over time was similar in all groups. In addition, no significant alterations were detected in enzyme activity of aspartate aminotransferase, alanine aminotransferase or alkaline phosphatase, and no significant alterations were found in glucose, urea, creatinine, total cholesterol or triglyceride levels. GI-16 and SC-15 treatments did not modify hemoglobin, red and white blood cell count, and sections of liver, kidneys and heart tissues showed no pathological alterations under light microscopy. In conclusion, the remarkable in vivo anti-inflammatory activity and low toxicity of SC-15 and GI-16 makes them promising drug candidates to treat inflammatory conditions.

Metronidazole and tinidazole are widely used antimicrobial drugs against Gram-negative and Gram-positive anaerobic bacteria. The present study was aimed to evaluate the impact of biofield treatment on metronidazole and tinidazole using FT-IR and UV spectroscopy. The study was carried out in two groups i.e. control and treatment. Treatment groups were subjected to Mr. Trivedi’s biofield treatment while no treatment was given to control group. FT-IR spectrum of treated metronidazole showed the impact of biofield treatment on frequency of characteristic functional groups such as C=C (imidazole ring) stretching was appeared at lower frequency i.e. from 1600 cm-1 to 1553 cm-1. Likewise, NO2 asymmetric stretching and C-N symmetric stretching were appeared at higher wave number i.e. 1479 cm-1 to 1501 cm-1 and 1070 cm-1 to 1077 cm-1, respectively. FT-IR spectrum of tinidazole showed shifting in absorption peak of C-N stretching to higher wavenumber from 1002 cm-1 (control) to 1022 cm-1. The wavenumber of aromatic C=C bond (in imidazole) was shifted to lower frequency, which could be due to increases in conjugationeffect. Further, increases in wavenumber of NO2 and C-N in treated sample suggested the increased force constant and bond strength as compared to control. Because of higher conjugation effect and increased bond strength, the molecule supposed to be more stable. The UV spectra of both metronidazole and tinidazole showed the similar patterns of lambda max (λmax) with respect to their control. The FT-IR results of both drugs suggest that there was an impact of biofield treatment on atomic level of metronidazole and tinidazole, as compared to control.