Surendra Kumar Nayak

2,4-Disubstituted thiazoles as multitargated bioactive molecules

Thiazoles are important heterocyclics exhibiting boundaryless biological activities, such as antibacterial, antifungal, anti-inflammatory, antitumor, antitubercular, antidiabetic, antiviral, and antioxidant. Substituents on a particular position of the thiazole ring affect the biological outcomes to a great extent. Therefore, researchers have synthesized compounds containing the thiazole ring with variable substituents as target structures, and evaluated their biological activities. The present review describes the biological importance of recently developed 2,4-disubstituted thiazole derivatives. Moreover, we have thrown light on various targets of 2,4-disubstituted thiazoles through which they induce biological effects, which will be helpful to those who are working on the design and structure–activity relationship of bioactive molecules.

Dendrimers: A Review on Synthetic Approaches -

This review article is focused on different synthetic strategies used in dendrimer synthesis at commercial and laboratory scale. These synthetic strategies includes their own advantages and disadvantages. This review will cover divergent (from core to surface) and convergent (from surface to core) approaches used in dendrimer synthesis and the problems associated with these synthetic strategies. This article also covers the important applications of dendrimers in the field of pharmaceutical sciences. This data of review is collected from various articles, research papers and patents available on dendrimers.

Synthesis, molecular docking and QSAR studies of 2, 4-disubstituted thiazoles as antimicrobial agents

In present study a series of 2,4-disubstituted thiazole derivatives was synthesized and evaluated for their in vitro antibacterial and antifungal activities against B. subtilis, E. coli, S. aureus, C. albicans and A. niger by tube dilution method. The analysis of antimicrobial activity results indicated that the presence of NO2 and OCH3 groups at para position of phenyl group improved the antimicrobial activity significantly. Molecular docking studies also supported in vitro activity results and showed that NO2 and OCH3 groups containing compounds have greater affinity towards the target glucosamine-6-phosphate synthase. QSAR studies indicated that molecular connectivity index ( 2 χ v ) and Kier’s shape index (α3) are the key parameters for antimicrobial activity

Current Strategies and Drug Targets in the Management of Type 2 Diabetes Mellitus

BACKGROUND Diabetes is one of the major concerns worldwide which leads to increased level of blood glucose due to deficiency of insulin and the development of insulin resistance in diabetic individuals. Basically, its impact arises due to rapid urbanization, improper diet intake, and increasingly inactive lifestyle. Diabetic patients develop serious complications with the development of disease at later stages, such as obesity, the risk of stroke and heart failure. Globally, an estimated 422 million adults are living with type 2 diabetes mellitus. METHODS We searched the scientific database using relevant keywords. Among the searched literature, only peer-reviewed papers were collected which addresses our questions. The retrieved quality papers were screened and analyzed critically. The key findings of these studies are included along with the importance. RESULTS The quality research paper included in the review, particularly the antidiabetic drugs which account for the second largest market by sales in the pharmaceutical industry after cancer. So the research came up with several novel therapeutic targets for the management of type 2 diabetes, to produce newer generation antidiabetic drug by offering a new concept for developing new drug candidates. CONCLUSION This review discusses the strategies and future perspectives in the management of type 2 diabetes mellitus particularly antidiabetic agents which are helpful for the betterment of diabetic patients.

A Retrospect Study on Thiazole Derivatives as the Potential Antidiabetic Agents in Drug Discovery and Developments

BACKGROUND Heterocycles containing thiazole, a moiety with sulfur and nitrogen is a core structure which is found in a number of biologically active compounds. The thiazole ring is notable as a component of the certain natural products, such as vitamin B1 (thiamine) and penicillins. Thiazole is also known as wonder nucleus and has uses in different biological fields. A number of new compounds contain heterocycle thiazole moieties, thus it is one of the important areas of research. METHODS We searched the scientific database using relevant keywords. Among the searched literature only peer-reviewed papers were collected which addresses our questions. The retrieved quality research articles were screened and analyzed critically. The key findings of these studies were included along with their importance. RESULTS The quality research articles included in this review were selected for the lifethreatening diseases i.e. diabetes, which is one of the serious issues all over the globe with an estimated worldwide prevalence in 2016 of 422 million people, which is expected to rise double to by 2030. Since 1995, there has been an explosion of the introduction of new classes of pharmacological agents having thiazole moieties. However, most of the drugs can cause noncompliance, hypoglycemia, and obesity. Thus, new antidiabetic drugs with thiazole moieties came up with improved compliance and reduced side effects such as pioglitazone (Actos), rosiglitazone (Avandia), netoglitazone, DRF-2189, PHT46, PMT13, DRF-2519. With such a great importance, research in thiazole is part of many academic and industrial laboratories worldwide. CONCLUSION The present review describes the importance of thiazole nucleus and its derivatives as antidiabetic agents with an emphasis on the past as well as recent developments.

Role of Mdm2 Cascade in Human Cancers

Mdm2 is a well known oncogene which affects expression of various genetic factors. It encoded oncoprotein Mdm2 of 491 amino acids divided into four major domains (p53-binding, acidic, Zn-finger and ring finger). Acting as an E3-ubiquitin ligase, Mdm2 induced degradation of various proteins which affect the cellular transformation such as p53, p73, JMY, FOXO3a, HPIP, HDAC, p21Waf1/CIP1 etc. Thus, Mdm2 found to be responsible for up and down regulation proteins in cellular system and plays crucial role in several human cancers through variety of biological pathways. Here, we described the major classes of human cancers in which Mdm2 involved directly or indirectly. Moreover, mechanistic role of Mdm2 summarised along with intermediates of cellular biochemical pathways regulated or expressed by it.

Benzimidazole: Structure Activity Relationship and Mechanism of Action as Antimicrobial Agent

Benzimidazole is nitrogen containing heterocyclic organic compound. It is a bicyclic compound with fused benzene and imidazole nucleus. Various research groups revealed that benzimidazole is an important lead molecule for the development of anthelmintic, antibacterial, antifungal, antiprotozoal, antimycobacterial and antiviral agents. So, in present review, various biologically important derivatives of benzimidazole have been compiled. On the basis of their biological activity data and substitution pattern around the benzimidazole nucleus, structure activity relationship (SAR) has been analysed. An outline of mechanism of action of benzimidazole derivatives against various biological targets is also presented. Hence, present review can help the researchers in development of new benzimidazole derivative with significant biological activity.