Sudhir Kumar Paidesetty

• M.PHARM. PhD
• Professor at Siksha O Anusandhan University

Molecules with potency and low toxicity are the leading army in the battlefield of multidrug resistance. Quercetin is found in abundance in the nature as a potent flavonoid and bears the tag of flavonoid paradox due to the poor bioavailability, however, it still possess distinct systemic actions, and this marks curiosity in the research field. The...

Superbugs are dominating the world due to misuse and overuse of the antibiotics. In the queue of design and synthesising new molecules with increased efficacy and capability to tackle microbial...

The briskened urge to develop potential antibacterial candidates against multidrug-resistant pathogens has motivated the present research study. Herein, newly synthesized coumarin derivatives with azomethine and amino-methylated as the functional groups have been focused on their antibacterial efficacy. The study proposed two distinct series: 3-ace...

The World Health Organization identifies breast cancer as the most prevalent cancer despite predominantly affecting women. Surgery, hormonal therapy, chemotherapy, and radiation therapy are the current treatment modalities. Site-directed nanotherapeutics, engineered with multidimensional functionality are now the frontrunners in breast cancer diagn...

Chemical, Material Sciences & Nano technology book series aims to bring together leading academic scientists, researchers and research scholars to exchange and share their experiences and research results on all aspects of Chemical, Material Sciences & Nano technology. The field of advanced and applied Chemical, Material Sciences & Nano technology...

Glycolipid-based biosurfactants (BSs), known for their intriguing and diverse properties, represent a largely uncharted territory in the realm of potential biomedical applications. This field holds great promise yet remains largely unexplored. This investigation provides new insights into the isolation, characterization, and comprehensive biomedica...

The Oscillatoria sp., a blue-green alga or cyanobacterium, consists of about 305 species distributed globally. Cyanobacteria are prokaryotes possessing several secondary metabolites that have industrial and biomedical applications. Particularly, the published reviews on Oscillatoria sp. have not recorded any pharmacology, or possible details, while...

Our cascading attempt to develop new potent molecules now involves designing a series of imidazole derivatives and synthesizing two sets of 2,4,5- tri-substituted (4a-4d) and 1,2,4,5-tetra-substituted (6a-6d) imidazole by the principle of Debus-Radziszewski multicomponent synthesis reaction. The structures of the obtained compounds were confirmed b...

Nowadays, bacterial multidrug resistance has become a commonplace problem in clinics due to several intrinsic factors mediated through resistance to antibacterials obtained via bacterial consortia and extrinsic factors, such as non-uniform antibacterial policy and migration of resistant bacteria through human and other routes. The development of ne...

Viral diseases are the most notorious infective agent(s) causing morbidity and mortality in every nook and corner for ages; viruses are active in host cells, and specific anti-virus medicines’ developments remain uncanny. In this century of the biological era, human viruses act predominantly as versatile spreaders. The infection of the present COVI...

Currently, cancer is the most grieving threat to society. The cancer‐related death rate has had an ascending trend, despite the implementation of numerous treatment strategies or the discovery of an array of potent molecules against several pathways of cancer growth. The need of the hour is to prevent the multidrug resistance toll, and the current...

Bioactive lipids are now widely accepted players in the field of cancer biology. Targeting components like enzymes, bioactive lipids and receptors are important for maintaining lipid homeostasis, metabolism, and signaling so that cell proliferation and metastasis can be reduced. This can be achieved through various means like modifying functions of...

A huge number of plant-derived essential oils (EOs) are reported to have lots of ethnomedicinal and biological properties with excellent antibacterial activities. Approximately three hundred EOs (ajowan, anise, basil, camphor, chamomile, clove, citronella, coriander, cumin, eucalyptus, lavender, lemon, orange, peppermint, thyme oils, etc.) are docu...

Nowadays, most anti-infective agents or antibiotics are becoming resistant to several uropathogenic microorganisms. Thus, there is an urgent need of new potent candidates for treating infectious diseases and overcome the antibiotic resistance. Nickel(II) complexes of composition [Ni(Lig2)·2H2O]X2 have been synthesized with the ligand substituted be...

With different nitrogen‐containing heterocyclic moieties, Indazoles earn one of the places among the top investigated molecules in medicinal research. Indazole, an important fused aromatic heterocyclic system containing benzene and pyrazole ring with a chemical formula of C7H6N2, is also called benzopyrazole. Indazoles consist of three tautomeric f...

Antibiotic resistance of bacteria and fungi has been brewing for decades and has now surfaced as a potential public health emergency, globally. Thus, newer potent drug candidates are needed urgently to overcome antibiotic-resistant episodes. As an attempt to overcome the antimicrobial multi-drug resistance problems, a new series of p-cuminal sulfon...

A series of N-heteroaryl substituted Gallamide derivatives 3a-3g were synthesized and the obtained structures were further confirmed by different spectral studies. For in-vitro antibacterial activity, the synthesized compounds were evaluated against three UTI (Urinary Tract Infection) bacterial strains including Staphylococcus aureus, Escherichia c...

The medicinally important species of the Solanaceae family belong to genera viz., Solanum, Atropa, Datura, Hyoscyamus, Nicotiana, etc. The active phytoalkaloids which are present in them are tropane, pyrrolidine–pyridine, and steroid alkaloids. Some of the pharmacologically potent alkaloids are scopolamine, atropine, hyoscyamine, nicotine, cocaine,...

2021) Biogenic synthesis of silver nanoparticles with the brackish water cyanobacterium Nostocsphaeroides and assessment of antibacterial activity against urinary tract infecting bacteria, Journal ABSTRACT The aim of this study was to isolate a filamentous nitrogen-fixing cyanobacterium Nostoc sphaeroides (NS) from brackish water of Chilika Lake, O...

A series of 4-hydroxy-3-methoxy benzaldehyde (vanillin) derivatives (3a–3r) was designed for the principle of Schiff base condensation with several individual sulfanilamide analogues. The inhibitory potencies of the designed compounds were evaluated through molecular docking simulation studies against the targets, breast cancer-topo isomerase-IIa a...

A series of 4-hydroxy-3-methoxy benzaldehyde (vanillin) derivatives (3a–3r) was designed for the principle of Schiff base condensation with several individual sulfanilamide analogues. The inhibitory potencies of the designed compounds were evaluated through molecular docking simulation studies against the targets, breast cancer-topo isomerase-IIα a...

Thymol (a phenol ring bearing active phytoconstituent) is a privileged scaffold, which is diversified in natural sources. This scaffold acts as an obligatory template for scheming and arriving at designing some newer drug‐molecules with potential biological activities. In the pharmacological perspective, the promising active sites of the scaffold a...

Antibacterial resistance has been brewing for decades and has now surfaced into potential public health emergency, everywhere. Thus, newer potent drug candidates are needed urgently that would help overcoming antibiotic resistances in bacteria and fungi. A series of thymol-bearing amino methylated sulfonamide congeners, 4a-4l were designed and synt...

Nowadays, bacterial infections epitomize significant health threats globally with an increased morbidity and mortality. Most contemporary antibacterial agents are resisted by patho-genic bacteria-the multidrug resistant (MDR) bacterial strains arising from cross resistances operative in natural bacterial consortia inside human body and in environme...

The manifestation of bacterial UTI (Urinary Tract Infection) has been predominantly endemic, globally; eventually, the development of new UTI anti-bacterial agent(s) remains the call of the day. Herein, two series of Mannich-based 4-hydroxy coumarin derivatives, 7a-m and 8a-m were designed by suitable heterocyclic amines condensed with aldehydes. T...

Background: The Gram-positive (GP) bacterium, methicillin resistant Staphylococcus aureus (MRSA) causes common infection, bacteremia at hospitals, and community sectors, with the simultaneous aggrandizement of resistance to several currently used antibacterials, resulting in additional morbidity and unexpected mortality. Since the last several deca...

The emergence and reemergence of multidrug‐resistant (MDR) bacteria and mycobacteria in community and hospital periphery have directly enhanced the hospitalization costs, morbidity and mortality, globally. The appearance of MDR pathogens, the currently used antibiotics, remains insufficient, and the development of potent antibacterial(s) is merely...

A series of eight quinoline-thiazole hybrid-bearing diazenylsulfonamides, 4a-4h, were synthesized and characterized by UV-Vis, FT/IR, 1H NMR and lC-MS. These compounds were formed when two prepared intermediate precursors of Schiff-base compounds, (E)-N-((2-chloroquinolin-3-yl)methylene)-4phenylthiazol-2-amine (3a) and (E)-N-((2-chloroquinolin-3-yl...

Mycobacterium tuberculosis (Mtb) causes one of the most grievous pandemic infectious diseases, tuberculosis (TB), with long-term morbidity and high mortality. The emergence of drug-resistant Mtb strains, and the co-infection with human immunodeficiency virus, challenges the current WHO-TB stewardship programs. The first- line anti-TB drugs, isoniaz...

Mycobacterium tuberculosis (Mtb) causes one of the most grievous pandemic infectious diseases, tuberculosis (TB), with long‐term morbidity and high mortality. The emergence of drug‐resistant Mtb strains, and the co‐infection with human immunodeficiency virus, challenges the current WHO‐TB stewardship programs. The first‐line anti‐TB drugs, isoniazi...

COVID-19 continues to be belligerent health threats nowadays and the Corona pandemic is the global burden. Herein, two series of chloroquine (CQ) and hydroxychloroquine (HCQ) derivatives were chemically conjugated with established small phenolic phytochemicals namely, thymol, vanillin, guaiacol, eugenol, 4-hydroxycoumarin and vanillin analogues by...

p>Dear Editor, Kindly find a research article entitled “Newly developed semi-synthetic chloroquine and hydroxychloroquine-phytochemical conjugates as prospective COVID-19 drug(s)”, submitted for consideration for publication. Kindly find the Herein, two series of chloroquine (CQ) and hydroxychloroquine (HCQ) derivatives were chemically conjugated...

Leprosy continues to be the belligerent public health hazard for the causation of high disability and eventual morbidity cases with stable prevalence rates, even with treatment by the on-going multidrug therapy (MDT). Today, dapsone (DDS) resistance has led to fear of leprosy in more unfortunate people of certain developing countries. Herein, DDS w...

The burden from microbial diseases has to be addressed in an increasing pace due to multidrug resistance, causing clinical annoyance, globally. Indeed, employing eco-friendly approaches by green syntheses of nanoparticles with metals/metalloids as antibacterial compounds would be continual and cost-effective. Herein, the synthesis of silver nanopar...

A series of Schiff base ciprofloxacin hydrazones with vanillin analogues were designed and validated for druggability properties by advanced computational tools, from which two shortlisted compounds were synthesized and characterized by different spectral studies. These compounds were used against bacterial DNA gyrase; purposedly attempted in molec...

Introduction: Due to heavy morbidity and mortality from cancer, the designing of newer drugable molecules against breast cancer is the call of day. As, Schiff-base sulfonamides have been widely used in tumor treatments. Methods: Nostocine-sulfonamide (NS) Schiff-base molecules were designed with tools of bioinformatics against the target enzyme, hu...

A series of N-(substituted benzylidene) thiazol-2-amines (3a-3d) and N-(substituted benzylidene) pyridyl-2-amines (3A-3D) were synthesized and individual structures were confirmed by several spectral techniques. Antibacterial activity of synthesized Schiff-base derivatives were performed by agar-diffusion method. These compounds were screened by in...

The current study aimed to identify a new strategy of FeCl3 catalyzed multicomponent synthesis of substituted 2H‐chromene–fused pyrrole derivatives. A series of chromene‐based pyrrole prepared by employing an array of 3‐nitro‐2H‐chromenes, aniline, and acetylacetone in toluene under microwave irradiation. Using FeCl3 as a prompt catalyst and microw...

A series of N-(substituted benzylidene) thiazol-2-amines (3a-3d) and N-(substituted benzylidene) pyridyl-2-amines (3A-3D) were synthesized and individual structures were confirmed by several spectral techniques. Antibacterial activity of synthesized Schiff-base derivatives were performed by agar-diffusion method. These compounds were screened by in...

Antipyrine (1,2-dihydro-1,5-dimethyl-2-phenylpyrazole-3-one) in a structural frame consists of a five membered lactam pyrazolone heterocyclic ring as a pharmacophore moiety. It is evident from literature that the molecules having nitrogen bearing heterocyclic nuclei clearly exhibit several biological actions. Commercially available pyrazolone deriv...

Cancer is a leading cause of death generally, and to overcome this problem the introduction of a new drug developing is a continuous endeavour. An alkaloid, norharmane and its derivatives, which have anticancer activities, widely distributed in several living and synthetic chemical sources. Herewith, the suggested mechanisms of organic reactions an...

The naturally occurring phyco‐constituent nostocine A, bearing the pyrazolotriazine scaffold in its structural frame, belongs to an organic class of pharmacologically curious candidates with a remarkable anticancer activity. This review summarizes the chemistry of numerous synthetic strategies of demethylated nostocine as “nornostocine derivatives,...

RESEARCH TITLE "THE DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF PYRAZOLE CONTAINING SULFONYLUREA DERIVATIVES AS POTENT GSK3Β INHIBITOR FOR BLOOD GLUCOSE LOWERING EFFECT"

Synthesis of novel thymol derivatives against MRSA and ESBL producing pathogenic bacteria, chemistry

Leprosy (causative, Mycobacterium leprae) continues to be the persisting public health problem with stable incidence rates, owing to the emergence of dapsone resistance that being the principal drug in the ongoing multidrug therapy. Hence, to overcome the drug resistance, structural modification through medicinal chemistry was used to design newer...

Background: Epilepsy is a common neurological disorder characterized by recurrent unprovoked seizures. Approximately 60 million people worldwide suffer from epilepsy, making this condition the second leading neurological disorder. Epilepsy also affects about 4% of individuals over their lifetime. The most commonly used anticonvulsant drugs are asso...

Twelve substituted aryl-azo-thymol derivatives (4a to 4 l) were synthesized and characterized by several spectral techniques such as, FTIR, UV-vis, proton NMR, Mass spectrometry and elemental analysis. Antimicrobial activities were evaluated by agar-well diffusion method against isolated MRSA, ESBL-producing pathogenic bacteria and antifungal resis...

Objective : Invasive microorganisms and free radicals are responsible for the delayed healing of various infections. It is necessary to discovery of novel molecules that are effective against invasive microorganisms and inhibit free radicals. Therefore, a series of metal complexes of 2-amino-4-substituted phenylthiazole Schiff bases were synthesize...

A series of diazotized sulfonamides have undergone azo coupling with the newly synthesized Schiff base ligand (E)-N-((2-chloroquinolin-3-yl)methylene)-4-phenylthiazol-2-amine 3a and (E)-4-(4-chlorophenyl)-N-((2-chloroquinolin-3-yl)methylene)-thiazol-2-amine 3b to give quinoline-thiazole based azo compounds. The solvent effect of the resulting compo...

To develop 6 conjugate agents of the moribund antibiotic sulfamethoxazole (SMZ) joined to 6 individual monoterpenes, followed by protocols of medicinal chemistry as potent antibacterials, against multidrug resistant (MDR) human gruesome pathogenic bacteria. Antibacterial activities of the proposed conjugates were ascertained by the ‘prediction of a...

Infections from multidrug resistant (MDR) pathogenic bacteria, fungi and Mycobacterium tuberculosis remain progressively intractable. The search of effective antimicrobials from other possible non-conventional sources against MDR pathogenic bacteria, fungi and mycobacteria is call of the day. This review considers 121 cyanobacterial compounds or cy...

Introduction: Novel Cu(II), Co(II) and Ni(II) complexes of 8-hydroxyquinolineazo analogues are synthesized from 5-((3-nitrophenyl)diazenyl) quinolin-8-ol (4a) and 5-((4-bromo-3-methylphenyl) diazenyl) quinolin-8-ol (4b). Methods: The structural environment and elemental composition of the synthesized metal complexes are confirmed by FT/IR,¹H NMR an...

Introduction: Mycobacterium tuberculosis has been a grievous pathogen causing staggering infections worldwide; especially its recently drug resistant strains are intractable. The MurA ligase of cell-wall peptidoglycan pathway is the suitable target often used for drug development. Methods: A homology model of MurA enzyme of M. tuberculosis was gene...

Background and objective: To develop 6 conjugate agents of the moribund antibiotic sulfamethoxazole (SMZ) joined to 6 individual monoterpenes, followed by protocols of medicinal chemistry as potent antibacterials, against multidrug resistant (MDR) human gruesome pathogenic bacteria. Methods: Antibacterial activities of the proposed conjugates were...

A series of several diazenyl Schiff base derivatives were designed and synthesized through azo coupling of diazotised primary amines with the novel synthesized Schiff base ligand (E)-N-((2-chloroquinolin-3-yl) methylene)-4-phenylthiazol-2-amine. All the synthesized compounds have been analysed by different spectral techniques such as elemental anal...

Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin resistant Enterococcus faecalis (VRE) are notorious pathogenic multidrug resistant (MDR) bacteria in both hospital and community sectors, and today the first antibacterial drug sulfamethoxazole is ineffective. The monoterpene phenol, thymol was conjugated with seven sulfa drug deriva...

A new series of 1-(4-substitutedphenyl)-3-(4-(4,6-dimethyl-6H-1,3-thiazin-2-yl)phenylsulfon-yl)urea/thiourea (3a-l) derivatives were synthesized and screened for anticonvulsant activity by maximal electro shock (MES) and pentylenetetrazole (PTZ) induced convulsant model. All the derivatives were evaluated for neurotoxicity measures by rotarod metho...

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The chemistry of heterocyclic compounds plays a crucial role in the synthesis of medicinals. This review focuses on the use of the thiazole nucleus for the synthesis of newer drug molecules through rational drug discovery. Here the synthetic feasibility, biochemical compatibility and the therapeutic utility of the thiazole derivatives is discussed...

A series of aryl / heteroarylazo substituted salicylaldehyde analogues along with the complexes of the composition [M (L-2)(H2O) (2)]center dot xH(2)O where L is deprotonated Schiff base ligand 2-[(E)-(4-methoxyphenylimino) methyl]-4-[(E)-(3-nitrophenyl) diazenyl] phenol 5a(Lig) and M = Cu(II), Ni(II) and Co(II) have been synthesized. The solvent e...

The azo derived products are versatile building blocker organic compounds used in drug research. In this review, we include the synthetic strategy and medicinal utility of some new azo derived candidates in recent years, which must be a good source of information to the researchers. A number of research articles explored with the help of different...

Eight different aryl / heteroarylazo substituted 2-naphthol congeners and complexes of the composition [M (L)2(H2O) 2]. x H2O where L is deprotonated ligands such as 4g (ligH): 4-((2-hydroxynaphthalen-1- yl) diazenyl)-1, 5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one and M= Cu(II), Ni(II) and Co(II) have been synthesized. The structures of the synthesize...

In the present study, a series of new bisazo dyes derived from dapsone have been synthesized in one step, using diazotized coupling reaction and evaluated for their in-vitro antimicrobial activity. Ampicillin and fluconazole have been taken as reference antibiotics (RA). The structure of synthesized compounds are confirmed by different spectral tec...

A series of aryl and heteroaryl substituted Oxychinolin derivatives have been synthesized and spectral characterizations have been conducted with different modern analytical techniques. The antimicrobial activities of the novel synthesized Oxychinolin analogues against different microbial strains have been screened by agar diffusion method. The com...

A newer series of 1-(4-substitutedphenyl)-3-(4-((2,4-dioxothiazolidin-5-lidene)methyl)phenyl sulfonyl)urea/thiourea (4a-l) were synthesized for their anticonvulsant activity. The activity is been attributed due to its potential to restrain astrocytic Na+, 2HCl, K+ co-transport same as torasemide which having sulfonylurea in its structure. Torasemid...

A series of azosalicylic acid analogs were newly synthesized by coupling various aryl and heteroarylamine functionalities with salicylic acid nucleus. All the synthesized compounds were structurally confirmed by various modern analytical methods. The said synthesized compounds were screened to investigate their antimicrobial, analgesic and antioxid...

Aim of the present study was to synthesize 5-aryl/heteroaryl azo pyrimidine analogues and to explore their antibacterial activity. A series of 5-aryl/heteroaryl azo bearing pyrimidine analogues (4i-4xii) were synthesized. The compounds were characterized by different modern analytical techniques. Solvatochromic behaviours of these compounds were ch...

In the present study a series of new N4-(4-substituted benzylidene)-N1-([1,3,4]thiadiazino[6,5-b]indol-3-yl)semicarbazide (1-6), N4-([1,3,4]thiadiazino[6,5-b]indol-3-yl)-N1-(1-(4-substituted phenyl)ethylidene)semicarbazide (7-10), N4-([1,3,4]thiadiazino[6,5-b]indol-3-yl)-N1-((4-substituted phenyl)(phenyl)methylene) semicarbazide.(11-14) have been s...

Abstract Objective The development of antibiotic resistance has recently been recognized as a global health problem. This study was designed to develop new potent molecules that are economic and minimally toxic. The research examined a novel one-step synthetic procedure of bioactive 3-arylazo-substituted coumarin derivatives (4i-4v) and further eva...

A series of substituted 8-arylazo 7-hydroxy 4-methyl coumarin (4a-4g) were synthesized and in-vitro evaluation for their preliminary antibacterial activities against E.coli, Staphylococcus aurous, Bacillus subtilis and Pseudomonas aeroginosa were carried out by agar-well diffusion method. Initially, the diazotized primary aryl amines, 3a-3g were sy...

Three new, simple, sensitive and economical methods (Method I, II and III) were developed for the determination of aripiprazole in pure and pharmaceutical formulation. Method-1 is based on the formation of condensed product obtained when Aripiprazole in acidic conditions reacted with 2, 4-dinitrophenylhydrazine in methanol to form yellowish orange...