C-2-Formyl glycals have sustained interest in carbohydrate chemistry as they afford valuable chiral building blocks for many biological-, pharmaceutical-, and industrial-based important molecules. Basically, C-2-formyl glycals are a class of carbohydrates incorporating an.,.-unsaturated aldehyde. Therefore in many organic reactions, the C2-formyl glycals can serve as an alpha,beta-unsaturated aldehyde core. In this review, we have compiled a literature survey covering the period 20132022, on the synthesis of C-2-formyl glycals and further discuss their importance for the synthesis of many medicinal, supramolecular, biological, organic, and material chemistry based molecules. 1 Introduction 2 Synthesis of C-2-Formyl Glycals 2.1 Vilsmeier-Haack Formylation 2.2 By Consecutive Cyclization 2.3 XtalFluor-E Based Synthesis 3 Applications of C-2-Formyl Glycals 3.1 C-2-Formyl Glycals as a Synthons 3.2 Anticancer 3.3 Anti-inflammatory 3.4 Antimicrobial 3.5 Glycosidase Inhibitors 3.6 Miscellaneous 4 Conclusion and Future Aspects

Background: Jumper's knee is the most frequent injuries in sports and it has upset many professional sporting careers. The term "jumper's knee" was first introduced by Blazina, a gradual insidious onset of aching in the knee centered over the infrapatellar or suprapatellar region, especially localized to the superior or inferior poles of the patella. Patellar tendinopathy is primarily a condition of relatively young (15 -30 years old) athletes, especially men, who participate in sports such as basketball, volleyball, athletic jump events, tennis, and football, which require repetitive loading of the patellar tendon. Basketball is the sport with the highest incidence of patellar tendonitis, hence why it is also known as Jumper's knee. Several studies identify the joints as the most damaged in sports injuries, with the knee and the ankle being the most affected in basketball. Studies show 32% of professional basketball players have patella tendonitis while amateur players have 11 -14% prevalence. NBA players with higher efficiency ratings and higher playing times are more at risk. For patients in the early stages of patellar tendinitis, conservative treatment is the method of choice. Patients with end -stage (Blazina III to IV) disease who have suffered a complete tendon rupture need surgery. Both arthroscopy and open surgery are commonly used. After surgery, dynamic balance and speed ability of the patient will be drastically reduced. It is necessary to improve the dynamic balance and speed among patients so that they can return to their sport. Hence, the need of the study is to find out the effectiveness of BOSU ball and agility training in enhancing dynamic balance and speed in post -operative jumper's knee among basketball players. Methodology: This is an experimental study design comparing the pre -post type done at Tagore College of Physiotherapy. In this study, 20 subjects were included based on the inclusion criteria. The study was conducted over a period of 12 weeks. The first 6 weeks dynamic balance training was given to the players using BOSU ball as three stages. Immediately, after completing the dynamic balance training, players were intended to start agility training for a period of 6 weeks. Total 72 sessions in 12 weeks for 35 -50 minutes, repetition 2 times per day, and 3 days a week. The pre -test and post -test values of dynamic balance on Star excursion balance test (SEBT) and Stork balance test were taken for analysis using paired t test. Similarly, pre -test and post -test values of speed on ¾ court sprint test and 30 -meter sprint test were taken for analysis using paired t test. Result: The statistical reports that the pre -test and post -test mean values and standard deviation values of SEBT were obtained. The pre -test mean and standard deviation values ofStork balance test were 36.55±5.92.The post -test mean and standard deviation values of Stork balance test were 139.65±22.25.The pre -test mean and standard deviation values of ¾ court sprint test were 3.9904±1.0703.The post -test mean and standard deviation values of ¾ court sprint test were 3.4452±0.477.The pre -test mean and standard deviation values of 30 meter sprint test were 5.5165±0.9409.The post -test mean and standard deviation values of 30 meter sprint test were 4.8040±0.8765.On the basis of results received, the study states that there was significant improvement in dynamic balance and speed.The result shows that, the effectiveness of BOSU ball and agility training in enhancing dynamic balance and speed in post -operative jumper's knee among basketball players.Conclusion: The study concludes that BOSU ball and agility training were effective on improving dynamic balance ad speed in post -operative jumper's knee among basketball players.

Carbohydrates and their analogues play a unique role in all living organisms and therefore have played a supremacy role in molecular recognition, energy supply, drug discovery, etc. During the last few decades, biocatalyst lipases have emerged as one of the greener and sustainable catalysts in comparison to traditional synthetic catalysts for the synthesis of modified carbohydrates and their analogues. Because lipase is a natural catalyst, it shows outstanding selectivity, reactivity, amazing tolerance, and assistance in carrying out eco-friendly greener methodology. The application of biocatalyst lipase as a chemo- and regio-selective catalyst is particularly relevant for organic chemists for the synthesis of modified carbohydrates, because carbohydrates contain several identical hydroxyl groups. Herein, we discussed the recent developments in the lipase Novozyme-435 mediated synthesis of modified carbohydrates and their biological significance.

A convergent route for the synthesis of a new class of bicyclic nucleosides has been developed. The synthetic route to the corresponding arabino-configured uracil and thymine bicyclic nucleosides proceeds in 24 and 27% overall yields, respectively, starting from 1,2,5,6-di-O-isopropylidene-α-d-glucofuranose. This synthetic protocol includes some crucial steps such as Vorbrüggen base coupling and chemo-enzymatic regioselective acetylation of the primary hydroxyl group by using Lipozyme® TL IM where it was found that Lipozyme® TL IM could be recovered and reused for selective acetylation without losing its selectivity.

This article covers the triazole-linked nucleic acids where the triazole linkage (TL) replaces the natural phosphate backbone. The replacement is done at either a few selected linkages or all the phosphate linkages. Two triazole linkages, the four-atom TL1 and the six-atom TL2, have been discussed in detail. These triazole-modified oligonucleotides have found a wide range of applications, from therapeutics to synthetic biology. For example, the triazole-linked oligonucleotides have been used in the antisense oligonucleotide (ASO), small interfering RNA (siRNA) and clustered regularly interspaced short palindromic repeats (CRISPR)-Cas9 technology as therapeutic agents. Due to the ease of the synthesis and a wide range of biocompatibility, the triazole linkage TL2 has been used to assemble a functional 300-mer DNA from alkyne- and azide-functionalized 100-mer oligonucleotides as well as an epigenetically modified variant of a 335 base-pair gene from ten short oligonucleotides. These outcomes highlight the potential of triazole-linked nucleic acids and open the doors for other TL designs and artificial backbones to fully exploit the vast potential of artificial nucleic acids in therapeutics, synthetic biology and biotechnology.

A facile and efficient methodology, comprised of a domino reaction, a Suzuki-Miyaura coupling reaction followed by an aldol condensation has been developed to synthesize novel 1-glycopyranosyl-4-biaryl butenone derivatives in a one-pot fashion. The reaction of C-glycosides 1-C-(β-D-glucosyl)propan-2-one, 1-C-(β-D-mannosyl)propan-2-one, 1-C-(β-D-galactosyl)propan-2-one, 1-C-(β-D-lactosyl)propan-2-one with 5-bromothiophene-2-carboxaldehyde or 4-bromobenzaldehyde and different boronic acids in the presence of Pd(II)-catalyst and a base in methanol at room temperature produced various chalcone type biphenyl C-glycosides in 75–85% yields.

A proficient approach has been developed for the synthesis of substituted 2H-chromenes from C1-substituted glucal. The key step of our synthetic methodology was C–H activation in propylene carbonate solvent followed by 6π-electrocyclization aromatization in ethylene glycol as greener substitutes to toxic aprotic solvents, to obtain 2H-chromenes in a stepwise manner. The application of the developed methodology was further explored with the synthesis of a small library of substituted 2H-chromenes in good yields.

A click chemistry-based protocol has been utilized for the synthesis of a series of twelve novel tert-butyldiphenylsilylated N1-(coumarin-4 '''-yl)-C4-(2 ' ,3'-di-deoxyuridin-3'-yl)-oxymethyl-1,2,3-triazoles and N1-(coumarin-4 '''-yl)-C4-(3 ' deoxythymin-3 '- yl)-oxymethyl-1,2,3-triazoles by utilising Cu(I)-catalyzed azidealkyne cycloaddition reaction of 4-azidocoumarins and 3 '-O- (prop-1-yn-3-yl)-5 '-O-(tert-butyldiphenylsilyl)-2 ' ,3 '-dideoxyuridin or 3'-O-(prop-1-yn-3-yl)-5 '-O-(tert-butyldiphenylsilyl)-3 '-deoxy-thymidin in 70-82% and 68-82% yields, respectively. The deprotection of resulted silylated uridine and thymidine conjugate with TBAF afforded title compounds in 81-91 % yield. The photophysical studies have been carried out on the synthesized coumarin-triazolylmethyl nucleoside conjugates which revealed a very high Stokes shift value ranging from 82- 215 nm.

Palladium catalysed C-H activation has been carried out on furanoid glycals to afford highly substituted and conjugated 2,3-dihydrofuran trienes and then its conversion into highly substituted 2,3-dihydrobenzofuran was achieved starting from commercially available, inexpensive sugar precursor diacetone-D-glucose. Claisen-Schmidt condensation reaction, Fujiwara-Moritani cross coupling reaction and 6 pi electro-cyclisation reaction were utilized as the key steps in this synthetic route. Diacetone-D-glucose was converted into dihydrofuran moiety via Claisen Schmidt condensation which was submitted to Fujiwara-Moritani C-C coupling reaction to afford 2,3-O-isopropylidine-4,5-disubstituted 2,3-dihydrofurans. Excellent yields (up to 97 %) were obtained during C-C coupling step which indeed is an accomplishment. Next, two step chemical route was established for conversion of these substituted and conjugated 2,3-dihydrofuran triene moieties into corresponding substituted 2,3-dihydrobenzofuran moiety.

A series of novel 1,2,3-triazole-linked hexopyranosyl mono/double-headed pyrimidine nucleosides from D-glucose was synthesized by Cu(I)-mediated [3+2] cycloaddition reactions (CuAAC) of mono/diazido 2,6-anhydro-glucoheptitol and propynylated pyrimidines in good yields. It was observed that all the four synthesized pyrimidine nucleosides were found to be non-cytotoxic upto 500 mu M concentration. The 1,2,3-triazole-linked hexopyranosyl mono/double-headed pyrimidine nucleosides have shown significant suppression of Hepatitis B surface antigen (HBsAg) and Hepatitis B e-antigen (HBeAg). Amongst all the synthesized compounds, nucleoside dimer 1-[1-(6 '-deoxy-6 '-(4-(1-methyluracil)-1,2,3-triazol-1-yl)-beta-D-glucopyranosyl methyl)-1,2,3-triazol-4-yl]methyl-uracil was found to be more effective against HBeAg. In the suppression of viral DNA level, all the four synthesized nucleoside analogues were comparable to known drug Entecavir (ETV) with IC50 value in the range of 8.39 mu M-18.58 mu M and are two folds significant as compared to control.

Dendrophthoe falcata is one of the hemiparasitic plants that belong to the mistletoe family Loranthaceae. Since ancient times, Dendrophthoe falcata extracts have been recognized for their medicinal importance and many of them have been used as traditional remedies for treatment of ailments like ulcers, impotence, asthma and wounds. As a result, the significance of this plant inspired us to conduct a literature review on the biochemical significance of its isolated phytochemicals. So, in the present review, an inclusive account of phytochemicals and biological activities of leaf, stem and fruit extracts of D. falcata are included in view of the many related recent findings.

A greener chemo-enzymatic methodology has been developed for the synthesis of conformationally restricted diastereomeric homolyxofuranosyl pyrimidines (AZT analogue), i.e., (5′R)-3′-azido-3′-deoxy-2′-O,5′-C-bridged-β-d-homolyxofuranosyl-uracil and thymine starting from inexpensive diacetone-d-glucofuranose in 18% and 21% overall yields, respectively. In one of the key steps in multistep synthesis of bicyclic AZT analogues, the primary hydroxyl group of 3′-azido-3′-deoxy-β-d-glucofuranosyl pyrimidines has been acetylated using Novozyme® 435 in THF in 92% and 97% yields, respectively. The monoacetylated nucleoside was converted to desired bicyclic AZT analogue in two steps in an overall yield of 82% and 83%, respectively.

Herein, we have summarized the vast array of synthetic processes that have been developed for the synthesis of C-glycopyranosyl aldehydes and diverse C-glycoconjugates derived from them by covering the literature reported from 1979 to 2023. Notwithstanding its challenging chemistry, C-glycosides are considered stable pharmacophores and are used as important bioactive molecules. The discussed synthetic methodologies to access C-glycopyranosyl aldehydes take advantage of seven key intermediates, viz. allene, thiazole, dithiane, cyanide, alkene, and nitromethane. Furthermore, the integration of complex C-glycoconjugates derived from varied C-glycopyranosyl aldehydes involves nucleophilic addition/substitution, reduction, condensation, oxidation, cyclo condensation, coupling, and Wittig reactions. In this review, we have categorized the synthesis of C-glycopyranosyl aldehydes and C-glycoconjugates on the basis of the methodology used for their synthesis and on types of C-glycoconjugates, respectively.

A highly stereoselective, efficient and facile route was achieved for the synthesis of novel and biochemically potent sugar fused pyrano[3,2-c]pyranone derivatives starting from inexpensive, naturally occurring d-galactose and d-glucose. First, β-C-glycopyranosyl aldehydes were synthesized from these d-hexose sugars in six steps, with overall yields 41-55%. Next, two different 1-C-formyl glycals were synthesized from these β-C-glycopyranosyl aldehydes by treatment in basic conditions. The optimization of reaction conditions was carried out following reactions between 1-C-formyl galactal and 4-hydroxycoumarin. Next, 1-C-formyl galactal and 1-C-formyl glucal were treated with nine substituted 4-hydroxy coumarins at room temperature (25 °C) in ethyl acetate for ∼1-2 h in the presence of l-proline to obtain exclusively single diastereomers of pyrano[3,2-c]pyranone derivatives in excellent yields. Four compounds were found to be active for the MCF-7 cancer cell line. The MTT assay, apoptosis assay and migration analysis showed significant death of the cancer cells induced by the synthesized compounds.

In the last decades, various efforts have been made to synthesize optimal glycotripods for targeting trimeric glycoproteins like asialoglycoprotein receptor, hemagglutinin, and langerin. All these trimeric glycoproteins have sugar binding pockets which are highly selective for a particular carbohydrate ligand. Optimized glycotripods are high affinity binders and have been used for delivering drugs or even applied as drug candidates. The selection of the tripodal base scaffold together with the length and flexibility of the linker between the scaffold and sugar residue, as important design parameters are discussed in this review.

A candidate molecule 1-(3-(1H-imidazol-1-yl) propyl)-3-(2,4-difluorophenyl) thiourea (coded as 'IR-415') exhibiting excellent antiviral efficacy in cell culture model was identified after a high-throughput screening of the Maybridge library.([7]) Twenty derivatives of IR-415 hereafter referred to as DSA-00 were synthesized and evaluated for their antiviral activity against hepatitis B virus (HBV) in cell culture. The HBV-expressing HepG2.2.15 cells or HBV-permissive HepG2-hNTCP-C4 cells were treated with DSA-00 or its new derivatives. A significant and improved inhibition in viral DNA replication and secretion of hepatitis B surface antigen were observed in the presence two derivatives, viz., 1-(2,4-Difluoro-phenyl)-3-(4-imidazol-1-yl-butyl)-thiourea and 1-(3,5-Difluoro-phenyl)-3-(4-imidazol-1-yl-butyl)-thiourea. Consistent with these antiviral properties, our molecular docking studies predicted a high affinity interaction of these derivatives with HBx protein. Importantly, DSA-00 and its derivatives exhibited minimal toxicity at higher concentrations. Thus, these derivatives have the potential to be developed as new therapeutics for mono or combination therapy for the management of HBV infection.

Multicomponent reactions (MCRs) cover strategically employed chemical transformations that incorporate three or more reactants in one pot leading to a functionalized final product. Thus, it is an ideal tool to achieve high levels of complexity, diversity, yields of desired products, atom economy, and reduced reaction times. Sugars belong to the class of naturally occurring compounds with fascinating applications in the field of drug discovery due to the presence of various hydroxy groups and well-defined stereochemistry. However, their potential in MCRs has been realized only recently. This account describes recent advances in the synthesis of sugar-derived heterocycles synthesized by MCRs. We hope to encourage the synthetic and medicinal chemistry community to apply this powerful MCR chemistry to generate novel glycoconjugate challenges.1 Introduction2 Synthesis of Various Functionalized Sugar Compounds2.1 Passerini and Ugi Multicomponent Reactions2.2 Petasis Reaction2.3 Hantzsch Reaction2.4 Domino Ferrier–Povarov Reaction2.5 Marckwald Reaction2.6 Groebke–Blackburn–Bienaymé (GBB) Reaction2.7 Prins–Ritter Reaction2.8 Debus–Radziszewski Imidazole Synthesis Reaction2.9 Mannich Reaction2.10 A3-Coupling Reaction2.11 [3+2]-Cycloaddition Reactions2.12 Miscellaneous Reactions3 Conclusion

A large number of Locked Nucleic Acids (LNAs) with variety of modifications and restricted conformations have been developed in the last few decades. These modifications have significantly improved the biological properties of oligonucleotides, when LNAs moieties were incorporated into them. Herein, the synthesis and applications of these modified locked nucleic acids as antisense oligonucleotides are discussed.Supplemental data for this article is available online at https://doi.org/10.1080/15257770.2022.2052316 .

Abstract Modified nucleosides are the core precursors for the synthesis of artificial nucleic acids, and are important in the field of synthetic and medicinal chemistry. In order to synthesize various triazolo-compounds, copper and ruthenium catalysed azide–alkyne 1,3-dipolar cycloaddition reactions also known as click reaction have emerged as a facile and efficient tool due to its simplicity and convenient conditions. Introduction of a triazole ring in nucleosides enhances their therapeutic value and various photophysical properties. This review primarily focuses on the plethora of synthetic methodologies being employed to synthesize sugar modified triazolyl nucleosides, their therapeutic importance and various other applications.