An Update on Recent Advances for the Treatment of Cerebral Malaria.

Among all the parasitic diseases in humans, malaria is the most significant and malicious one. The widespread species are Plasmodium falciparum and Plasmodium vivax, but the infection caused by the former is the deadliest. According to the November 2018 report of the World Health Organization (WHO), a total of 219 million cases of malaria were reported globally in 2017, which led to an estimated 435,000 deaths.

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery.

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as an anticancer drug specifically to the colon for the proficient treatment of colon cancer.

Background: Colon Cancer (CC) is the third commonly detected tumor worldwide and makes up about 10% of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells.

Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.

In the present study, a series of steroidal tetrazole derivatives of androstane and pregnane have been prepared in which the tetrazole moiety was appended at C-3 and 17a-aza locations. 3-Tetrazolo-3,5-androstadien-17-one (6), 3-tetrazolo-19-nor-3,5-androstadien-17-one (10), 3-tetrazolo-3,5-pregnadien-20-one (14), 17a-substituted 3-tetrazolo-17a-aza-D-homo-3,5-androstadien-17-one (26-31) and 3-(2-acetyltetrazolo)-17a-aza-d-homo-3,5-androstadien-17-one (32) were synthesized from dehydroepiandrosterone acetate (1) through multiple synthetic steps. Some of the synthesized compounds were evaluated for their in vitro 5α-reductase (5AR) inhibitory activity by measuring the conversion of [(3)H] androstenedione in human embryonic kidney (HEK) cells.

An overview of phytotherapeutic approaches for the treatment of benign prostatic hyperplasia.

Benign prostatic hyperplasia (BPH) is the noncancerous growth of the prostate gland resulting due to overproliferation of the stromal and glandular elements of the prostate and is associated with lower urinary tract symptoms. Natural products, containing inherently vast structural diversity than synthetic compounds, have been the major resources of bioactive agents and will continue to play as protagonists for discovering new drugs. Phytotherapeutic products have been used traditionally in developing countries while the use of them as complementary alternative medicine is increasing rapidly in developed countries for the management of BPH.

3D QSAR studies on 1, 3, 4-thiadiazole derivatives: an approach to design novel anticonvulsants.

A three-dimensional quantitative structure-activity relationship (3D-QSAR) study was performed on a series of 1, 3, 4-thiadiazole derivatives reported as anticonvulsant employing self-organizing molecular field analysis (SOMFA) techniques to investigate the structural requirements for the design of novel anticonvulsant. The training set composed of twenty two 1, 3, 4-thiadiazole derivatives that exhibit a potent activity in MMS test while predictive power was evaluated using a test set of 7 molecules. Physicochemical determinants of binding, such as steric and electrostatic properties, were mapped onto the molecular structures of 1, 3, 4-thiadiazole in order to interpret graphically the SOMFA results in terms of master grids showing various field contributions.

Sulphonamides as inhibitors of protein tyrosine phosphatase 1B: a three-dimensional quantitative structure-activity relationship study using self-organizing molecular field analysis approach.

Protein tyrosine phosphatase 1B (PTP 1B), a cytosolic PTP involved in down-regulation of receptor tyrosine kinase activity following stimulation of the insulin or leptin receptors. Thus, PTP 1B inhibitors could potentially ameliorate insulin resistance and normalize plasma glucose and insulin levels without inducing hypoglycemia, and could therefore be a major advancement in the treatment of type 2 diabetes. A three-dimensional quantitative structure-activity relationship (3D-QSAR) study has been performed on a novel class of sulphonamides using self-organizing molecular field analysis (SOMFA) to correlate their chemical structures with their observed PTP 1B inhibitory activities.

3D-QSAR studies on a series of 5-arylidine-2, 4-thiazolidinediones as aldose reductase inhibitors: a self-organizing molecular field analysis approach.

Aldose Reductase (AR), the key enzyme of the polyol pathway catalyzes the reduction of glucose to sorbitol using nicotinamide adenine dinucleotide phosphate as an essential cofactor, has been demonstrated to play an important role in the pathogenesis of diabetic complications. Self Organizing Molecular Field Analysis (SOMFA), a novel three-dimensional quantitative structure activity relationship (3D-QSAR) method has been used in present case to study the correlation between the molecular properties and the aldose reductase inhibitory activities on a series of 5-arylidine-2, 4-thiazolidinedione. SOMFA calculations for both shape and electrostatic potentials were carried out.

Saxagliptin: a new drug for the treatment of type 2 diabetes.

Saxagliptin (BMS-477118) has been recently FDA approved drug for the management of T2DM developed by Bristol-Myers Squibb and AstraZeneca under the trade name Onglyza. Saxagliptin is a nitrile-containing selective, potent, reversible and durable DPP IV inhibitor developed as an alternative second-line adds on to Metformin in place of a sulphonylurea. Saxagliptin increases and prolongs the action of incretin hormones by inhibiting the DPP IV enzyme that inactivates incretins usually within minutes.

Hypolipidemic effect of ethanolic extract from the leaves of Hibiscus sabdariffa L. in hyperlipidemic rats.

The present study is designed to investigate the hypolipidemic effect of ethanolic extract from the leaves of Hibiscus sabdariffa L. (HSEE) in hyperlipidemic rats. In the present work, HSEE was evaluated at three doses (i.

3D-QSAR Studies on a Series of 5-Arylidine-2, 4-Thiazolidinediones as Aldose Reductase Inhibitors: A Self-Organizing Molecular Field Analysis Approach.

Aldose Reductase (AR), the key enzyme of the polyol pathway catalyzes the reduction of glucose to sorbitol using nicotinamide adenine dinucleotide phosphate as an essential cofactor, has been demonstrated to play an important role in the pathogenesis of diabetic complications. Self Organizing Molecular Field Analysis (SOMFA), a novel three-dimensional quantitative structure activity relationship (3D-QSAR) method has been used in present case to study the correlation between the molecular properties and the aldose reductase inhibitory activities on a series of 5-arylidine-2, 4-thiazolidinedione. SOMFA calculations for both shape and electrostatic potentials were carried out.

Self-organizing molecular field analysis on pregnane derivatives as human steroidal 5alpha-reductase inhibitors.

Normal growth and development of human prostate is regulated by the androgens which balances cell proliferation and apoptosis. Testosterone (T) and dihydrotestosterone (DHT) are the two key androgens that stimulate most of the androgen action in prostate. Testosterone is converted to DHT by the membrane bound NADPH-dependent 5alpha-reductase enzyme.

An overview on 5alpha-reductase inhibitors.

Benign prostatic hyperplasia (BPH) is the noncancerous proliferation of the prostate gland associated with benign prostatic obstruction and lower urinary tract symptoms (LUTS) such as frequency, hesitancy, urgency, etc. Its prevalence increases with age affecting around 70% by the age of 70 years. High activity of 5alpha-reductase enzyme in humans results in excessive dihydrotestosterone levels in peripheral tissues and hence suppression of androgen action by 5alpha-reductase inhibitors is a logical treatment for BPH as they inhibit the conversion of testosterone to dihydrotestosterone.