Mayuri A. Borad

Recent advances in the synthesis of 2-substituted benzothiazoles: a review

Benzothiazole can serve as unique and versatile scaffolds, especially in synthetic and pharmaceutical chemistry because of their potent and significant pharmacological activities. This important class of derivatives possess numerous pharmacological activities like antitumor, antimicrobial, anti-inflammatory, anticonvulsant, antidiabetic activities and so on. Many scientists have developed a wide range of methodologies for the synthesis of the 2-substituted benzothiazole nucleus and its derivatives using different types of catalysts to improve the selectivity, purity and yield of the products. Thus, the present review article focuses mainly on the different kind of reactions involved in synthesis of the 2-substituted benzothiazole nucleus and its derivatives.

Review of Synthesis of Multispiro Heterocyclic Compounds from Isatin

Abstract Because of its various biological activities, isatin plays important roles in organic chemistry. The C-3 carbonyl group of the isatin possesses very high reactivity and thus isatin possesses many diverse applications in organic synthesis. This carbonyl group reacts like a prochiral center. For the organic synthetic chemist, the conception of a spiroheterocyclic building block has always been interesting, as it often requires synthetic design based on specific strategies. This review summarizes the synthesis of various multispiro heterocyclic compounds by using isatin through 1,3-dipolar cycloaddition reactions and multicomponent reactions. GRAPHICAL ABSTRACT

Synthetic Strategies for Fused Benzothiazoles: Past, Present, and Future

Abstract Benzothiazole is used as a building block in organic synthesis, which serves as a key template for the development of various therapeutic agents and shows a wide spectrum of activities. The attractive application of benzothiazole in organic synthesis is undoubtedly due to the highly reactive C-2 amino group, which is responsible for the change in its bioactivity. The construction of a poly-heterocyclic compound with the fused hetero-systems has attracted increasing attention because of the diverse range of potential therapeutic activities. Significant efforts have been undertaken to exploit different synthetic routes to these compounds. This article gives a comprehensive account of the synthetic utility of benzothiazole employed in the design and synthesis of different types of compounds containing fused heterocyclic rings with greater emphasis on recent literature. GRAPHICAL ABSTRACT

Drug development against tuberculosis: Past, present and future

Infection of Mycobacterium tuberculosis (MTB) was observed as early as 5000 years ago with evidence, which is a primeval enemy of the humanoid race. MTB is the pathogen which is responsible for causing the infectious disease tuberculosis; it remains a major cause of morbidity and mortality in poor low-income countries as well as in developing countries because of non-availability of reliable laboratory facilities. The current treatment for drug-resistant tuberculosis (TB) is lengthy, complex, and connected with severe harmful side effects and poor outcomes. The present cure against tuberculosis has substantial restrictions, in terms of their efficiency, side-effect outline, and complication of handling. Furthermore, the emergence of multi-drug resistant tuberculosis (MDR-TB) outbreaks during the 1990s and additionally in recent times the vast deadly strains of extensively drug-resistant tuberculosis (XDR-TB) and totally drug resistance tuberculosis (TDR-TB) is hampering efforts to control and manage tuberculosis (TB). As a result, novel methodologies for the treatment of multi-drug-resistant and extensive drug-resistant tuberculosis (TB) are severely desired. A number of new potential anti-tuberculosis drug candidates with novel modes of action have been entered in clinical trials in recent years. These agents are most likely to be effective against resistant strains. The treatment landscape is beginning to shift, with the recent approvals by Food and Drug Administration to the new TB drugs bedaquiline and delamanid. Also, the pipeline of potential new treatments has been fulfilled with several compounds in clinical trials or preclinical development with promising activities against sensitive and resistant MTB bacteria. An additional new chemical entity is also under development. The already existing drugs with their suggested mode of treatment as well as new probable anti-tuberculosis drug moieties which are at present in the pipeline has been summarized in this review.

Microwave-Assisted ZrSiO2 Catalysed Synthesis, Characterization and Computational Study of Novel Spiro[Indole-Thiazolidines] Derivatives as Anti-tubercular Agents

In the current investigation, we prepared a series of novel spiro[indole-thiazolidines] derivatives (5a–5h) from 5-substituted isatin derivatives and thioglycolic acid (TGA) with ZrSiO2 as an efficient catalyst under microwave irradiation. The significant merits of this protocol have some significant merits such as simplicity in operation, simple, efficient workup, good practical yields of product and the employment of recyclable catalyst. All the new synthesized scaffold has been well characterized by various spectroscopic methods and elemental analysis. All the spiro scaffolds were subjected to in vitro anti-mycobacterial activity against the Mycobacterium tuberculosis (H37Rv) strain. We have carried out molecular docking study of our synthesized compounds. We also calculated theoretically ADME–Tox parameters for synthesized compounds.

Recent advances in the synthesis of C-5-substituted analogs of 3,4-dihydropyrimidin-2-ones: A review

ABSTRACT 3,4-Dihydropyrimidin-2-ones act as a versatile scaffold in organic synthesis, which serves as a significant template for the development of various therapeutic agents and shows a wide spectrum of activities. The attractive application of 3,4-dihydropyrimidin-2-ones in organic synthesis is undoubtedly owing to C-5 ester group, which is responsible for the change in its bioactivity. Introduction of various groups like electron-withdrawing and electron-donating groups at positions 1, 2, 3, 5, and 6 greatly increased biological activity. Significant efforts have been undertaken to exploit different synthetic routes to synthesize various derivatives of 3,4-dihydropyrimidin-2-ones. This review article gives a comprehensive account of the synthetic utility of C-5 substitution of 3,4-dihydropyrimidin-2-ones used in the design and synthesis of different types of compounds with greater emphasis on recent literature. GRAPHICAL ABSTRACT