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Nachiket S. Dighe ¹, Shashikant R. Pattan ², Sanjay B. Bhawar ³, Santosh B. Dighe ², Mayur S. Bhosale ⁴, Vishal B. Tambe ², Vinayak M. Gaware ², Mangesh B. Hole ², Sapana M. Nagare ²

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar A/P- Loni Bk. Taluka-Rahata, Dist-Ahmednagar 413736, (MS), IN
2 Department Of Medicinal Chemistry, Pravara Rural College Of Pharmacy, Pravaranagar, M.S., IN
3 Department of Pharmacology, Pravara Rural College of Pharmacy, Pravaranagar, M.S., IN
4 Department of Medicinal Chemistry, Pravara Rural College of Pharmacy, Pravaranagar, M.S., IN
5 Department Of Medicinal Chemistry, Pravara Rural College Of Pharmacy,Pravaranagar, M.S., IN

Abstract

Rocky Mountain spotted fever (RMSF) is a disease caused by the bacterium Rickettsia rickettsii which is spread to humans by ticks. Symptoms include the sudden onset of fever, headache and muscle pain followed by the development of a rash. In the laboratory, rickettsiae cannot be cultivated on agar plates or in broth, but only in viable eukaryotic host cells. Rocky Mountain spotted fever and Mediterranean spotted fever are rickettsial infections primarily of endothelial cells that normally have a potent anticoagulant function. As a result of endothelial cell infection and injury, the hemostatic system is perturbed and shows changes that vary widely from a minor reduction in the platelet count to severe coagulopathies, such as deep venous thrombosis and disseminated intravascular coagulation. Animals probably become infected by aerosol and by the bite of any of the 40 species of ticks that carry the organisms. From the portal of entry in the skin, rickettsiae spread via the bloodstream to infect the endothelium and sometimes the vascular smooth muscle cells, brain, lungs, heart, kidneys, liver, gastrointestinal tract and other organs. Rickettsia species enter their target cells, multiply by binary fission in the cytosol and damage heavily parasitized cells directly. The target cells are macrophages in the lungs, liver, bone marrow, spleen, heart valves and other organs. Clinico-epidemiologic diagnosis is ultimately a matter of suspicion. Empirical treatment and later laboratory confirmation gives specific diagnosis. Some laboratories are able to identify rickettsiae by immunohistology in skin biopsies as a timely, acute diagnostic procedure, but to establish the diagnosis; physicians usually rely on serologic demonstration of the development of antibodies to rickettsial antigens in serum collected after the patient has recovered. Currently, assays that demonstrate antibodies to rickettsial antigens themselves are preferable to the nonspecific, insensitive Weil-Felix test that is based on the crossreactive antigens of OX-19 and OX-2 strains. Tetracycline, Doxycycline and chloramphenicol are the drugs of choice for treatment. Control of the tick population on the property, keeping pets tick-free are some measures to control the disease.

Keywords

Black Measles, Chloramphenicol, Rickettsia, Tetracycline.

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Jiban Debnath ¹, Santosh B. Dighe ², Nachiket S. Dighe ³, Supriya Mana ⁴

Affiliations
1 Department of Pharmacology, Girijananda Chowdhury Institute of Pharmaceutical Science, Azara, Guwahati, Assam, IN
2 Department of Pharmacology, Pravara Rural College of Pharmacy, Pravaranagar, Maharashtra, 413736, IN
3 Department of Medicinal Chemistry, Pravara Rural College of Pharmacy, Pravaranagar, Maharashtra, IN
4 Department of Pharmacology, NSHM, College of Pharmaceutical Technology, Kolkata, IN

Abstract

In present study the anticonvulsant activity of ethanolic extract of Holarrhena antidysenterica was carried out in swiss albino mice. The anticonvulsant activity of ethanolic extract of seeds of Holarrhena antidysenterica (250 and 500 mg/kg, p.o.) in mice was assessed by using maximum electroshock seizure (MES) test, pentylenetetrazol (PTZ), and bicuculine (BC) test. The ethanolic extract of H. antidysenterica significantly reduced the duration of seizures induced by maximal electroshock (MES). The ethanol extract in doses of 250 and 500 mg/kg conferred protection (17 and 50%, respectively) on the mice. The same doses also protected animals from tonic seizures induced by Pentylenetetrazol and significantly delayed the onset of tonic seizures produced by Pentylenetetrazol. The extract had no effect on bicuculine induced seizure. The ethanolic extract of H. antidysenterica (EEHA) reduced MES, PTZ induced convulsions.

Keywords

Anticonvulsant, H. antidysenterica, MES, PTZ, BC.

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Shashikant R. Pattan ¹, Nachiket S. Dighe ², Deepak S. Musmade ¹, Manisha S. Kedar ¹, Smita K. Parjane ¹, Priyanka P. Gadhave ¹, Manjusha S. Sanap ¹

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar, 413736 (MS), IN
2 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar, A/PLoni Bk., Taluka -Rahata, Dist-Ahmednagar 413736, IN

Abstract

The present review article on tools for synthesis of natural products is to significantly facilitate organic synthesis of natural products which are of significant biological importance by the implementation of new concepts for catalysis. We focus on the recent development in natural product synthesis with the help of newer methods of organic synthesis.

Keywords

Natural Products, Methods of Synthesis, Combinatorial Chemistry.

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Nachiket S. Dighe ¹, Shashikant R. Pattan ², Deepak S. Musmade ², Abhijeet N. Merekar ³, Manisha S. Kedar ², Deepak K. Thakur ², Pratik V. Patel ²

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar, A/PLoni Bk., Taluka -Rahata, Dist-Ahmednagar 413736, IN
2 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar, 413736 (MS), IN
3 Department of Pharmaceutics, Pravara Rural College of Pharmacy, Pravaranagar, 413736 (MS), IN

Abstract

Many natural products from marine sources are endowed with promising anti cancer activity, thus representing invaluable leads in the plans for drug discovery. In this context, organic synthesis plays a decisive role in confirming (or revising) the chemical structures of the natural compounds allowing also access to suitable amounts of the target (and its analogs) for structure activity relationship (SAR) investigations. In this overview, we focus on the total and partial synthesis of anti cancer marine metabolites and their related compounds discussing the retro synthetic analysis of the strategies adopted.

Keywords

Marine, Anti Cancer Activity, Synthesis of Dictyostatin.

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Shashikant R. Pattan ¹, Nachiket S. Dighe ², H. V. Shinde ¹, Deepak S. Musmade ¹, Mangesh B. Hole ¹, Vinayak M. Gaware ¹

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar, 413736 (MS), IN
2 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar A/P- Loni Bk. Taluka -Rahata, Dist-Ahmednagar 413736, IN

Abstract

The present review article on Umpolung chemistry is to significantly facilitate organic synthesis by the implementation of new concepts for catalysis. We focus on the recent development of N- heterocyclic carbenes mediated organic reaction and its implementation to the synthesis of heterocycles of biological importance.

Keywords

Umpolung, N-Heterocyclic Carbenes, Organomettalic Catalyst.

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Nachiket S. Dighe ¹, Ravindra B. Saudagar ², Ramesh S. Kalkotwar ³, D. A. Jain ⁴

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Loni, MS -413736, IN
2 Department of Pharmaceutical Chemistry, R.G. Sapkal College of Pharmacy, Nashik, M.S, IN
3 Department of Pharmaceutical Chemistry, S.N.D. College of Pharmacy, Yeola, Dist-Nashik, MS, IN
4 Department of Pharmaceutical Sciences and Research, Bhagwant University, Ajmer, Rajasthan, IN

Abstract

Mercaptooxadiazole is a five membered heterocyclic system consists of two nitrogen and one oxygen atoms along with acidic thiol group. As it increases the acidity of the titled compounds. It can be easily synthesized from hydazides using potassium hydroxide in presence of carbon disulphide. Mercaptooxadiazoles posses wide spectrum of biological activities like antibacterial, antifungal, antiviral, anti-inflammatory, anticonvulsant, antidepressant, antihypertensive, analgesic, and hypoglycemic properties. The present review is an attempt made to reveal the therapeutic and synthetic profiles of the mercaptooxadiazole ring.

Keywords

Mercaptooxadiazole, Synthesis, Biological Evaluation.

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Shashikant R. Pattan ¹, Nachiket S. Dighe ², Sunil A. Nirmal ¹, Prerana A. Chavan ¹, Sanjay B. Bhawar ¹, Nilesh Jadhao ¹, Santosh B. Dighe ¹

Affiliations
1 Pravara Rural College of Pharmacy, Loni, M.S., IN
2 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar A/PLoni Bk. Taluka -Rahata, Dist- Ahmednagar 413736, (MS), IN

Abstract

Cassia fistula Linn (Leguminosae) is a shrub, extensively used in traditional medicine in tropical and warm subtropical countries. C. Fistula commonly found in waste grounds and secondary forest. The chemical constituents reported from this plant belong to different classes such as glycosides, flavonoides, steroids, mucilage and sugars. C. Fistula has number of medicinal uses, many of which have been verified by scientific methods. This review article summarizes the chemistry and pharmacological profile of C. Fistula.

Keywords

Cassia fistula, Phytochemistry, Pharmacological Activities.

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Nachiket S. Dighe ¹, Shashikant R. Pattan ², Sunil A. Nirmal ², Vipul V. Dhasade ², Shruti G. Dake ², Madhuri U. Shelar ², Mangesh B. Hole ², Vinayak Gaware ²

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Pravaranagar A/PLoni Bk.Taluka -Rahata,Dist- Ahmednagar 413736, (MS), IN
2 Pravara Rural College of Pharmacy, Pravaranagar, M.S, IN

Abstract

Cassia tora Linn (Leguminosae) is a shrub, extensively used in traditional medicine in tropical and warm substropical countries. C. tora commonly found in waste grounds and secondary forest. The chemical constituents reported from this plant belong to different classes such as glycosides, tannins, flavonoides, steroids, resins, mucilage and sugars. C. tora has number of medicinal uses, many of which have been verified by scientific methods. This review article summarizes the chemistry and pharmacological profile of C. tora.

Keywords

Cassia tora, Phytochemistry, Pharmacological Activity, Anthraquinone Glycoside.

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Nachiket S. Dighe ¹, Ravindra B. Saudagar ², Ramesh S. Kalkotwar ³, D. A. Jain ⁴

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Loni, MS-413736, IN
2 Department of Pharmaceutical Chemistry, R.G.Sapkal College of Pharmacy, Nashik, M.S., IN
3 Department of pharmaceutical Chemistry, S.N.D. College of Pharmacy, Yeola, Dist-Nashik, MS, IN
4 Department of Pharmaceutical Sciences and Research, Bhagwant University, Ajmer, Rajasthan, IN

Abstract

Triazole is a five membered heterocyclic system consisting of two carbon atoms and three nitrogen atoms shows wide range of biological activities. Triazoles can be synthesized using Einhorn-Brunner reaction or the Pellizzari reaction from acyl hydrazides. Triazoles posses wide spectrum of biological activities like including antibacterial, antifungal, antiviral, anti-inflammatory, anticonvulsant, antidepressant, antihypertensive, analgesic, and hypoglycemic properties. The present reviews attempted to gather the various developments in synthesis and biological activities of triazole derivatives.

Keywords

1, 2, 4-Triazole, Pharmacological Activity, SAR, Total Synthesis.

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Nachiket S. Dighe ¹, Pankaj Shinde ¹, Harshali Anap ¹, Sanjay Bhawar ², Deepak S. Musmade ³

Affiliations
1 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Loni 413736, MS, IN
2 Department of Pharmacology, Pravara Rural College of Pharmacy, Loni 413736, MS, IN
3 Department of Pharmaceutical Chemistry, Sanjivani College of Pharmaceutical Education and Research, Kopargaon, MS, IN

Abstract

The synthesis, structure and biological activity of Oxadiazole derivatives have long been the focus of research interests in the field of Medicinal Chemistry. A number of Oxadiazole derivatives have been reported to possess interesting biological activities such as Antimicrobial, Anti-inflammatory and Antifungal activities etc. All synthesized compound were characterized by IR, H¬1-NMR and elemental Analysis. All the compounds were evaluated for Antibacterial and Anti-inflammatory at the concentration of 200 μcg/mL by using cup-plate agar diffusion method. The activity was carried out on different micro-organisms (E.coli, S. aureus, A.niger, C. albicans) measured in terms of zone of inhibition and compared the standard drug Ciprofloxacin and Amphotericin B for antimicrobial activity. All the newly synthesized derivatives were screened for Anti-inflammatory activity by an in-vitro method of Inhibition of protein denaturation using Zaltoprofen as a standard.

Keywords

Anti-Inflammatory, Antimicrobial and Oxadiazole.

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Ravindra B. Saudagar ¹, Nachiket S. Dighe ², Deepak S. Musmade ³, Vinayak M. Gaware ⁴, D. A. Jain ⁵

Affiliations
1 Department of Pharmaceutical Chemistry, R.G. Sapkal College of Pharmacy, Nashik, M.S., IN
2 Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Loni-413736, MS, IN
3 Department of Pharmaceutical Chemistry, Sanjivani College of Pharmaceutical Education and Research, Kopargaon, MS, IN
4 Department of Pharmaceutical Chemistry, College of Pharmacy, Chincholi, MS, IN
5 Department of Pharmaceutical Sciences and Research, Bhagwant University, Ajmer, Rajasthan, IN

Abstract

Selective estrogen receptor modulators are the class of a chemical compounds acting on a estrogen receptors. These are selectively inhibit or stimulate the estrogen like actions in various tissues. SERMs play a key role in breast cancer chemoprevention. These agents antagonize estrogens in some tissues and mimic their action in others. The mechanism for tissue selectivity appears to be related to differences in their molecular and three-dimensional structures, which affect the transcriptional activity of the activated estrogen receptor. For example, tamoxifen and toremifene act as estrogen antagonists in breast tissue and as estrogen agonists in the endometrium. The present review article is directed towards highlighting the importance of SERMs in treatment of breast cancer.

Keywords

Selective Estrogen Receptor Modulators (SERM’s), Breast Cancer, Hormone Replacement Therapy (HRT).

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Shashikant R. Pattan ¹, V. D. Pujar ², Nachiket S. Dighe ¹, Deepak S. Musmade ¹, S. N. Hiremath ³, H. V. Shinde ¹, R. B. Laware ¹

Affiliations
1 Pravara Rural College of Pharmacy, Loni-413736, M.S., IN
2 KLE’S College of Pharmacy, Belgaum, IN
3 College of Pharmacy, Chincholi, Nashik, M.S., IN

Abstract

A new series of 2-amino substituted benzothiazoles and their derivatives were prepared by multiple steps. The structures of the synthesized compounds were confirmed by Melting point, TLC, IR, and H¹NMR. The compounds were screened for their anti-inflammatory activity, all the compounds shown promising anti-inflammatory activity.

Keywords

2-Amino-Substituted-Benzothiazoles, Anti-Inflammatory, CHN Analysis.

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Shashikant R. Pattan ¹, Nachiket S. Dighe ¹, Deepak S. Musmade ¹, Vinayak M. Gaware ¹, S. G. Jadhav ¹, Medha A. Khade ¹, S. N. Hiremath ²

Affiliations
1 Pravara Rural College of Pharmacy, Pravaranagar, A/P-Loni Bk-413736, Tal Rahata, Dist Ahmednagar, (MS), IN
2 College of Pharmacy, Chincholi, Nashik, M.S., IN

Abstract

A new series of benzopyrone derivatives were synthesized and the structure of these compounds was established on the basis of spectral data. The title compounds were evaluated for antidiabetic activity. Some of these compounds have shown excellent antidiabetic activity.

Keywords

Benzopyrone, Antidiabetic, CHN Analysis.

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Shashikant R. Pattan ¹, Nachiket S. Dighe ¹, Anand A. Bukitagar ¹, Prerana A. Chavan ¹, Snehlata K. Tambe ¹, Deepak S. Musmade ¹, S. V. Hiremath ²

Affiliations
1 Department of Medicinal Chemistry, Pravara Rural College of Pharmacy, Pravaranagar, M.S., IN
2 Department of Pharmacology, JNMC, Belgaum, Karnataka, IN

Abstract

A new series of substituted phenylthiazole derivatives were synthesized and the structures of these compounds were established on the basis of spectral and elemental analysis. All the compounds were evaluated for anti-convulsant activity by Maximal Electroshock Induced Convulsions in Rats, Pentylenetetrazole- Induced Convulsions in Rats, and Strychnine Induced Convulsions in Rats methods. Compounds C₁, C₂, C₃, C₄, C₅, D₁, D₂, D₃, D₄, D₅, E₁, E₂, E₃, and E₄ have been found to exhibit excellent anti-convulsant activity.

Keywords

Phenylthiazole, Anti-Convulsant.

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