@kledeemeduniversity.edu.in
Professor, Department of Pharmaceutical Chemistry
KLE University of Higher education and Research
M. Pharm (Pharmaceutical Chemistry)
Ph. D
Synthesis of organic molecule
Scopus Publications
Scholar Citations
Scholar h-index
Scholar i10-index
S. K. Nimbal, Manjunath Patil, Pradeep Ronad, and Pradeep Kumar MR
A and V Publications
Purpose: The metal complexes of schiff bases have essential task during the field of chemistry and possess diverse pharmacological activities. Coumarin containing synthesized derivatives or plant extract may show analgesic effects Objective: Evaluating the analgesic activity of schiff base coumarins with metal complex. Materials and Methods: The study was conducted using Wister rats (150-250g) in both central and peripheral screening models of analgesics such as hot plate method, tail flick method (central) and writhing test (peripheral). The rats were pre administered with different derivatives of coumarins such as copper complex of schiff base of 2,5-dimethoxybenzaldehyde (Compound I), copper complex of schiff base of 4-dimethylaminobenzaldehyde (Compound II) and copper complex of the schiff base of 3-nitrobenzaldehyde (Compound III) for 14 days orally at the dose of 200mg/kg. Body weight, food and water consumption were continuously noted in chronic model. After the fourteen days rats were subjected to different screening models of pain and noted the reaction time. Gastro intestinal (GI) histopathological study was carried out to evaluate the GI toxicity. Results: Pretreatment with the different coumarin derivatives showed analgesic effect by increasing the reaction time to pain. In hot plate method, Compound II and III exhibited significant analgesic activity compared to Compound I whereas all three compounds showed significant increase in reaction time for tail flick method. In writhing test all compounds showed significant activity by reducing the pain perception induced by acetic acid. In histopathological study all compounds showed protective effect by reducing the ulceration and congestion of gastric mucosa. Conclusion: The screening model results and histopathological data evidently substantiate the analgesic effect of schiff base coumarins with metal complex.
Neelakanth M Jeedi, Sandeep Bajji, Pradeepkumar M Ronad, Shrishail K Nimbal, and Santosh B Patil
Medic Scientific
Pain and inflammation are the major devastating health problems commonly treated with NSAIDs. NSAIDs are regularly employed to relieve pain and inflammation. However, the 1,2,4-triazole derivatives have been scientifically evaluated for their use in relieving pain and inflammation. The current research plan is to explore the analgesic and anti-inflammatory properties of 1,2,4-triazole derivatives. 1,2,4-triazoles was tested for their anti-inflammatory properties using carrageenan and formalin-induced paw oedema, acetic acid-induced writhing investigation, while its peripheral and central analgesic actions were assessed using the hot plate method and Carrageenan induced Air Pouch model respectively. The test compounds were administrated at dose of 55 mg/Kg. The standard Diclofenac drug was administrated at dose of 10 mg/Kg for Acetic acid induced writhing investigation, Anti-inflammatory activity and 10 mg/Kg dose of pentazocine was administrated for hot plate method. Rats given with distilled water (10 mL/kg) were designated as the negative controls. Oral administration of all treatments was used. Evaluation of the analgesic and anti-inflammatory investigation showed that the second compound (5-(4-nitrophenyl)-1-phenyl-1H-1,2,4-triazole-3-(2H)–one declines the number of abdominal cramps caused by 1�etic acid and increases the time of response in hot plate method and decreased the edema induced by carrageenan, formalin also decreased volume of exudates in air pouch model. The results of the research indicate that compound 5-(4-nitrophenyl)-1-phenyl-1H-1,2,4-triazole-3-(2H)-one has shown more effective analgesic and Anti-inflammatory properties than the other two compounds.
Raj Sheena M., Jamakandi Vilas G., Jalalpure Sunil S., and Ronad Pradeepkumar M.
Journal of Applied Pharmaceutical Science
Mahesh B. Palkar, D. M. Praveen, Pradeepkumar M. Ronad, A. H. M. Viswanathswamy, Rajesh A. Rane, Harun M. Patel, Mahamadhanif S. Shaikh, Girish A. Hampannavar, Kavita S. Jain, and Rajshekhar Karpoormath
Springer Science and Business Media LLC
A novel series of methyl-2-(substituted benzylideneamino)-3-phenyl propionate (2a–j) derivatives have been synthesized. The title compounds (2a–j) were screened for in vivo acute anti-inflammatory and analgesic activities at a dose of 200 mg/kg b.w. Compound 2e exhibited the most promising and significant anti-inflammatory profile while compounds 2b, 2h, 2i, and 2j showed moderate to good inhibitory activity at 2nd and 4th h, respectively. These compounds were also found to have considerable analgesic activity (acetic acid-induced writhing model) and antipyretic activity (yeast-induced pyrexia model). In addition, the tested compounds were also found to possess less degree of ulcerogenic potential as compared to the standard NSAIDs. The synthesized compounds were further evaluated for their inhibitory activity against cyclooxygenase enzyme (COX-1/COX-2), by in vitro colorimetric COX (ovine) inhibitor screening assay method. The results revealed that the compounds 2b, 2e, 2h, 2i, and 2j exhibited selective and effective inhibition against COX-2. In an attempt to understand the ligand–protein interactions in terms of their binding affinity, docking studies were also performed using Molegro Virtual Docker (MVD-2013, 6.0) for the title compounds. It was observed that the binding affinities calculated were in agreement with the experimental IC50 values.Graphical Abstract
R.D. Hunashal, P.M. Ronad, V.S. Maddi, D. Satyanarayana, and M.A. Kamadod
Elsevier BV
Mahesh B. Palkar, Anuj S. Singhai, Pradeepkumar M. Ronad, A.H.M. Vishwanathswamy, Thippeswamy S. Boreddy, Veeresh P. Veerapur, Mahamadhanif S. Shaikh, Rajesh A. Rane, and Rajshekhar Karpoormath
Elsevier BV
Prashant Aragade, Mahesh Palkar, Pradeepkumar Ronad, and Darbhamulla Satyanarayana
Springer Science and Business Media LLC
The purpose of this study was to evaluate the antimycobacterial activity of various pyrazole derivatives derived from the isoniazid pharmacophore along with coumarin scaffold. The synthesized title compounds (4a–4k) were investigated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using Resazurin MIC assay. The synthesized compounds exhibited MIC ranging from 0.625 to 2.50 μg/ml. Among the series tested, compound 3-[3-(4-fluorophenyl)-1-isonicotinoyl-1H-pyrazol-5-yl]-2H-chromen-2-one 4i was found to be the most active with MIC of 0.625 μg/ml.Graphical AbstractSynthesis, spectral studies and antimycobacterial screening of a series of 11 new 2-pyrazole derivatives containing coumarin nucleus are described.
Nista Ingale, Veeresh Maddi, Mahesh Palkar, Pradeepkumar Ronad, Shivalingrao Mamledesai, A. H. M. Vishwanathswamy, and Darbhamulla Satyanarayana
Springer Science and Business Media LLC
A novel series of 3-[(5-substituted-1,3,4-oxadiazol-2-yl-thio)acetyl]-2H-chromen-2-one (7a–i) were synthesized by the condensation between the appropriately substituted 5-substituted-1,3,4-oxadiazolyl-2-thione (4a–i) derived from various existing NSAIDs and 3-(2-bromoacetyl)-2H-chromen-2-one (6) under reflux in the presence of sodium ethoxide. Structure of the synthesized compounds was established on the basis of physicochemical, elemental analysis, and spectral data. The title compounds were screened for in vivo acute anti-inflammatory and analgesic activities at a dose of 200 mg/kg bw. Among the series, four compounds 7c, 7e, 7f, and 7h were found to possess a significant anti-inflammatory and analgesic activity profile. In addition, these compounds were also found to possess a less degree of ulcerogenic potential as compared to standard NSAIDs.
A.H.M Viswanatha Swamy, BC Koti, P.M Ronad, U Wangikar, A.H.M Thippeswamy, and DV Manjula
Medknow
Objective: To investigate the preventive and curative role of ascorbic acid on doxorubicin (dox)-induced myocardial toxicity in rats. Materials and Methods: Animals were divided into five groups of six animals each. Group I served as normal control and received saline 5 ml/kg/day intraperitoneal (i.p.) for a period of 15 days. Group II animals received ascorbic acid 20 mg/kg per oral (p.o.) for 15 days as a pretreatment control (PR). Group III animals received dox 2.5 mg/kg body weight (b.w.), i.p., in six equal injections for two weeks for a total cumulative dose of 15 mg/kg b.w. Group IV animals received ascorbic acid 20 mg/kg p.o. for 15 days as a pretreatment followed by dox 2.5 mg/kg b.w., i.p., in six equal injections for two weeks for a total cumulative dose of 15 mg/kg body weight. Group V animals received dox 2.5 mg/kg b.w., i.p., in six equal injections for two weeks for a total cumulative dose of 15 mg/kg b.w. followed by ascorbic acid 20 mg/kg p.o for 15 days as post-treatment control (CR). The biochemical parameters such as tissue glutathione (GSH), malondialdehyde (MDA), catalase (CAT), and superoxide dismutase (SOD), and enzyme biomarkers such as creatine phosphokinase (CPK), lactate dehydrogenase (LDH), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) were monitored. Results: Pretreatment with ascorbic acid (20 mg/kg p.o.) significantly protected the myocardium from the toxic effect of dox (PR), by increasing the levels of antioxidant enzymes such as GSH, SOD, and CAT toward normal and decreased the levels of MDA, CPK, LDH, AST, and ALT as compared with dox-treated rats. Post-treatment with ascorbic acid to dox-treated group (CR) significantly increased the levels of tissue GSH, SOD, CAT and significantly decreased the level of MDA as compared with dox-treated group. It also reduced the severity of cellular damage of the myocardium as confirmed by histopathology. The restoration of the endogenous antioxidant system clearly depicts that ascorbic acid produced its protective effect by scavenging the reactive oxygen species. Conclusion: The results obtained in this study provide evidence for the usefulness of the ascorbic acid as a cardioprotective agent.
Pradeepkumar M. Ronad, Malleshappa N. Noolvi, Sheetal Sapkal, Satyanarayana Dharbhamulla, and Veeresh S. Maddi
Elsevier BV
Sandip Jaju, Mahesh Palkar, Veeresh Maddi, Pradeepkumar Ronad, Shivalingarao Mamledesai, Darbhamulla Satyanarayana, and Mangala Ghatole
Wiley
A novel series of 14 new isonicotinyl hydrazide derivatives 2a–g, 3a–g containing a 4‐thiazolidinone / 2‐azetidinone nucleus were synthesized by reacting N′‐substituted arylidene / heteroarylidene isonicotinyl hydrazide 1a–g with thioglycollic acid in the presence of dry benzene and with chloroacetyl chloride in the presence of triethylamine, respectively. Structures of all newly synthesized compounds were characterized on the basis of elemental analyses and spectral data (IR and 1H‐NMR). All the title compounds were tested for their in‐vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using Alamar‐Blue susceptibility test, and the activity is expressed as the minimum inhibitory concentration (MIC) in μg/mL. Among the series, compounds 2b, 2g, 3b, and 3g displayed an encouraging antimycobacterial activity profile as compared to that of the reference drugs isoniazid / rifampicin.
Prashant Aragade, Veeresh Maddi, Suresh Khode, Mahesh Palkar, Pradeepkumar Ronad, Shivalingarao Mamledesai, and Darbhamulla Satyanarayana
Wiley
A novel series of 3‐[3‐(substituted phenyl)‐1‐isonicotinoyl‐1H‐pyrazol‐5‐yl]‐2H‐chromen‐2‐one derivatives 4a–k have been synthesized by the reaction of 3‐[2,3‐dibromo‐3‐(substituted phenyl) propanoyl]‐2H‐chromen‐2‐one 3a–k and isonicotinic acid hydrazide in the presence of triethylamine in absolute ethanol, characterized by spectral data and screened for their in‐vitro antibacterial activity against Gram‐positive and Gram‐negative bacteria. Among the series, compounds 4e, 4i, and 4k displayed an encouraging antibacterial activity profile as compared to the reference drug ampicillin against tested bacterial strains.
Suresh Khode, Veeresh Maddi, Prashant Aragade, Mahesh Palkar, Pradeep Kumar Ronad, Shivalingarao Mamledesai, A.H.M. Thippeswamy, and D. Satyanarayana
Elsevier BV
Pradeepkumar Ronad, Satyanarayana Dharbamalla, Rajesh Hunshal, and Veeresh Maddi
Wiley
A series of novel Schiff' base‐containing a 7‐amino‐4‐methylcoumarin moiety have been synthesized III a–l, characterized by spectroscopic data and studied for their anti‐inflammatory and analgesic activity. The results of the anti‐inflammatory and analgesic activity evaluation of 7‐(substituted benzylideneamino)‐4‐methyl‐2H‐chromen‐2‐one derivatives III a–l proved to be comparable or more potent with respect to the reference drugs. In particular, compounds 7‐(4‐chlorobenzylideneamino)‐4‐methyl‐2H‐chromen‐2‐one III f, 7‐(2,4‐dichlorobenzylideneamino)‐4‐methyl‐2H‐chromen‐2‐one III g and 7‐(4‐bromobenzylideneamino)‐4‐methyl‐2H‐chromen‐2‐one III h exhibited potent anti‐inflammatory and analgesic activity.
Pradeepkumar Ronad, Rajesh Hunashal, Satyanarayana Darbhamalla, and Veeresh Maddi
Georg Thieme Verlag KG
A novel series of coumarinyl amides (IVa-l) have been synthesized by reacting 7-amino-4-methylcoumarin (III) with various substituted aromatic acid chlorides. IR, 1H NMR, 13C NMR and HRMS spectral data characterized the structure of the synthesized compounds. The title compounds were screened for in vivo acute anti-inflammatory activity using the carrageenan-induced rat paw edema assay model. Among the compounds tested, 2-chloro-N-(4-methyl-2-oxo-2H-chromen-7-yl)benzamide (IVb) and 4-chloro-N-(4-methyl-2-oxo-2H-chromen-7-yl)benzamide (IVc) showed 60.5 and 62.3% edema protection, respectively, as compared to the standard drug diclofenac (CAS 15307-86-5) (63.5%) after third hour. Compounds N-(4-methyl-2-oxo-2H-chromen-7-yl)-4-nitrobenzamide (IVf) and N-(4-methyl-2-oxo-2H-chromen-7-yl)cinnamamide (IVg) showed moderate activity. The new compounds have been also tested for in vivo analgesic activity. Quantitative structure-activity relationship studies indicated that the chloro substitution at the aromatic ring enhanced the anti-inflammatory activity (IVb and IVc). These compounds were also found to provide significant protection in acetic acid induced writhing animal model, showing remarkable analgesic activity. Compounds IVb and IVc showed 55.1% and 56.3% protection, respectively, as compared to acetylsalicylic acid (CAS 50-78-2) (57.7%).
Girish Bolakatti, Veeresh Maddi, Shivalingarao Mamledesai, Pradeep Ronad, Mahesh Palkar, and Shivakumar Swamy
Georg Thieme Verlag KG
A novel series of coumarinyl Mannich bases (3a-1) have been synthesized by reacting 3-acetyl coumarin (1) with various substituted secondary amines (2a-1) in presence of paraformaldehyde. The structures of the newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and HRMS (high resolution mass spectral) data. Title compounds were screened for in vivo acute anti-inflammatory activity using the carrageenan-induced rat paw edema assay model. Among the compounds tested, 3-[3-(diethylamino)propanoyl]-2H-chromen-2-one (3a)and 3-[3-(piperidine-1-yl) propanoyl]-2H-chromen-2-one (3c) showed 63.1 and 66.7% inhibition, respectively, as compared to the standard drug diclofenac (CAS 15307-86-5, 68.8%). These potent compounds showed encouraging analgesic andantipyretic activities.
S.S. Honnalli, P.M. Ronad, K. Vijaybhasker, V.I. Hukkeri, and Rajiv Kumar
Walter de Gruyter GmbH