Medicinal Chemistry of Drugs Affecting Cardiovascular and Endocrine Systems

Anticoagulants, Antiplatelets and Thrombolytic Agents

Author(s): M. O. Faruk Khan* and A. R. M. Ruhul Amin

Pp: 107-159 (53)

DOI: 10.2174/9789815179729124030007

* (Excluding Mailing and Handling)

Abstract

This chapter is a comprehensive account of the medicinal chemistry of anticoagulants, antiplatelets and thrombolytic agents and related drugs. It provides the mechanism of drug action and detailed structure-activity relationship (SAR) of the drugs affecting in these clinical areas to give the knowledge base for pharmacists. After studying this chapter, students will be able to:

• Describe the historical background of the anticoagulants, antiplatelets and thrombolytic agents and and related drugs.

• Describe the mechanism of action, pharmacokinetics (PK), and adverse drug reaction (ADR) of the anticoagulants, antiplatelets and thrombolytic agents.

• Explain the physiology and pathophysiology of clotting cascades and identify the components of a blood clot. • Classify major anticoagulant drugs and their structures and binding.

• Discuss in detail the chemistry and SAR of these drugs.

• Distinguish among drugs used as antiplatelets, anticoagulants and fibrinolytic agents.

 • Delineate the clinical significance and therapeutic evaluations of these classes of drugs by solving case studies.

• Explain the discovery process of a few specific drugs in these classes. 

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      • 14. app/Models/UserAccess/UserAccess.php:784
      • 15. middleware::check_user_access:114
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      • 18. vendor/laravel/framework/src/Illuminate/Pipeline/Pipeline.php:183
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      • 20. vendor/laravel/framework/src/Illuminate/Routing/Route.php:206
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      • 17. app/Http/Controllers/ChapterController.php:1434
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      • 17. vendor/laravel/framework/src/Illuminate/Routing/ControllerDispatcher.php:43
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      • 11. app/Models/ContentAccess.php:647
      • 12. app/Http/Controllers/ChapterController.php:1465
      • 13. vendor/laravel/framework/src/Illuminate/Routing/Controller.php:54
      • 14. vendor/laravel/framework/src/Illuminate/Routing/ControllerDispatcher.php:43
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      230μsalphaeurekaselec_live_10_06_2022ContentAccess.php#647
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      • 11. app/Models/ContentAccess.php:647
      • 12. app/Http/Controllers/ChapterController.php:1478
      • 13. vendor/laravel/framework/src/Illuminate/Routing/Controller.php:54
      • 14. vendor/laravel/framework/src/Illuminate/Routing/ControllerDispatcher.php:43
      • 15. vendor/laravel/framework/src/Illuminate/Routing/Route.php:260
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      • 13. app/Models/UserAccess/UserAccess.php:1266
      • 14. app/Http/Controllers/ChapterController.php:1518
      • 15. vendor/laravel/framework/src/Illuminate/Routing/Controller.php:54
      • 16. vendor/laravel/framework/src/Illuminate/Routing/ControllerDispatcher.php:43
      • 17. vendor/laravel/framework/src/Illuminate/Routing/Route.php:260
    • (select j.user_access_id,j.volume_id,j.user_id,j.from_ip,j.to_ip,j.type,j.track,"Trial Access" as access_base_text, CASE j.type WHEN 111 THEN true ELSE false END as terms_popup, "S" as content_download_type, null as restricted_user_access_key, null as restricted_user_access_type, CASE j.track WHEN 0 THEN false ELSE true END as tracksAccessByVolume,"chapter" as access_level, j.chapter_id from `user_access_chapter_trail` as `j` inner join `user_access_info` as `info` on `j`.`user_access_id` = `info`.`user_access_id` where ((j.from_ip <= 221967817 and j.to_ip >=221967817 )) and ((j.from_date <= 1740074209 and j.to_date >= 1740074209 and j.perpetual= 0) or (j.from_date is null and j.to_date is null and j.perpetual= 1)) and j.chapter_id = 21548) union (select j.user_access_id,j.volume_id,j.user_id,j.from_ip,j.to_ip,j.type,j.track,"Subscribed" as access_base_text, false as terms_popup, "S" as content_download_type, null as restricted_user_access_key, null as restricted_user_access_type, CASE j.track WHEN 0 THEN false ELSE true END as tracksAccessByVolume,"chapter" as access_level, j.chapter_id from `user_access_chapter_corporate` as `j` inner join `user_access_info` as `info` on `j`.`user_access_id` = `info`.`user_access_id` where ((j.from_ip <= 221967817 and j.to_ip >=221967817 )) and ((j.from_date <= 1740074209 and j.to_date >= 1740074209 and j.perpetual= 0) or (j.from_date is null and j.to_date is null and j.perpetual= 1)) and j.chapter_id = 21548) union (select j.user_access_id,j.volume_id,j.user_id,j.from_ip,j.to_ip,j.type,j.track,"Token Based Access" as access_base_text, false as terms_popup, "R" as content_download_type, j.uc_id as restricted_user_access_key, "v" as restricted_user_access_type, CASE j.track WHEN 0 THEN false ELSE true END as tracksAccessByVolume,"chapter" as access_level, j.chapter_id from `user_access_chapter_token` as `j` inner join `user_access_info` as `info` on `j`.`user_access_id` = `info`.`user_access_id` where ((j.from_ip <= 221967817 and j.to_ip >=221967817 )) and ((j.from_date <= 1740074209 and j.to_date >= 1740074209 and j.perpetual= 0) or (j.from_date is null and j.to_date is null and j.perpetual= 1)) and j.chapter_id = 21548)
      580μsalphaeurekaselec_live_10_06_2022UserAccess.php#1266
      Backtrace
      • 13. app/Models/UserAccess/UserAccess.php:1266
      • 14. app/Http/Controllers/ChapterController.php:1549
      • 15. vendor/laravel/framework/src/Illuminate/Routing/Controller.php:54
      • 16. vendor/laravel/framework/src/Illuminate/Routing/ControllerDispatcher.php:43
      • 17. vendor/laravel/framework/src/Illuminate/Routing/Route.php:260
    • select b.banner_link, b.banner_name, b.banner_script, b.banner_remarks, b.banner_file_name, b.banner_placement, bd.content_type, bd.content_id from `tbl_banner` as `b` inner join `tbl_banner_detail` as `bd` on `bd`.`banner_id` = `b`.`banner_id` inner join `users` as `u` on `u`.`id` = `b`.`updated_by` where `b`.`banner_ebook` = 1 and `bd`.`content_type` = 'B' and `bd`.`content_id` = 3664 and `b`.`banner_from_date` <= 1740074209 and `b`.`banner_to_date` >= 1740074209 and `b`.`banner_status` = 'A' order by `b`.`banner_id` desc
      1.05msalphaeurekaselec_live_10_06_2022Banner.php#95
      Bindings
      • 0: 1
      • 1: B
      • 2: 3664
      • 3: 1740074209
      • 4: 1740074209
      • 5: A
      Backtrace
      • 13. app/Models/Banner.php:95
      • 14. app/Http/helpers.php:404
      • 17. vendor/laravel/framework/src/Illuminate/Filesystem/Filesystem.php:124
      • 18. vendor/laravel/framework/src/Illuminate/View/Engines/PhpEngine.php:58
      • 19. vendor/laravel/framework/src/Illuminate/View/Engines/CompilerEngine.php:73
    • select count(*) as aggregate from `uc_cart_products` where cart_id='9fe05265fef67bf9efde1336b3253d34'
      190μsalphaeurekaselec_live_10_06_2022Cart.php#271
      Backtrace
      • 15. app/Models/Cart.php:271
      • 16. view::layouts._header:260
      • 18. vendor/laravel/framework/src/Illuminate/Filesystem/Filesystem.php:124
      • 19. vendor/laravel/framework/src/Illuminate/View/Engines/PhpEngine.php:58
      • 20. vendor/laravel/framework/src/Illuminate/View/Engines/CompilerEngine.php:73
    App\Models\Chapter
    1Chapter.php#?
    App\Models\Ebook
    1Ebook.php#?
        _token
        2Z1NloYwLVoq1oNltgDMexsHpH2lLqXnvrMjDAW8
        uc_cart_id
        9fe05265fef67bf9efde1336b3253d34
        _previous
        array:1 [ "url" => "http://alpha.eurekaselect.com/chapter/21548" ]
        _flash
        array:2 [ "old" => [] "new" => [] ]
        PHPDEBUGBAR_STACK_DATA
        []
        path_info
        /chapter/21548
        status_code
        200
        
        status_text
        OK
        format
        html
        content_type
        text/html; charset=UTF-8
        request_query
        []
        
        request_request
        []
        
        request_headers
        0 of 0
        array:8 [ "accept-encoding" => array:1 [ 0 => "gzip, deflate" ] "accept" => array:1 [ 0 => "text/html,application/xhtml+xml,application/xml;q=0.9,image/avif,image/webp,image/apng,*/*;q=0.8,application/signed-exchange;v=b3;q=0.7" ] "user-agent" => array:1 [ 0 => "Mozilla/5.0 AppleWebKit/537.36 (KHTML, like Gecko; compatible; ClaudeBot/1.0; +claudebot@anthropic.com)" ] "upgrade-insecure-requests" => array:1 [ 0 => "1" ] "cache-control" => array:1 [ 0 => "no-cache" ] "pragma" => array:1 [ 0 => "no-cache" ] "connection" => array:1 [ 0 => "keep-alive" ] "host" => array:1 [ 0 => "alpha.eurekaselect.com" ] ]
        request_cookies
        []
        
        response_headers
        0 of 0
        array:5 [ "content-type" => array:1 [ 0 => "text/html; charset=UTF-8" ] "cache-control" => array:1 [ 0 => "no-cache, private" ] "date" => array:1 [ 0 => "Thu, 20 Feb 2025 17:56:49 GMT" ] "set-cookie" => array:2 [ 0 => "XSRF-TOKEN=eyJpdiI6InNOVEpiRjdld0J2MzQ3WXprN0hOa2c9PSIsInZhbHVlIjoiQnRBWU1nU1BncDZ1eGszc1dNSVV0eWxiL0FLNEZic1VrQ2puZnl6SDY3YkRBb29NdjJWZzRtYkpFZmZqbTNtU1ZORWdDYVBpbUFBaXdxY2dNbG93UGZSYk1YbDRvdXVEOHVibVNNMU9BSzJudkVXYjhkOFhQdFMvcE1ETHgzaDEiLCJtYWMiOiI0NjBhMGJkYTk1YjA5MjFiMjU1MDdjZmE3Y2ZmNDg3ZWE3MTdlZGRiYjkxM2ZiZTVjNWJkYjI2MjAzNGM3MjRkIiwidGFnIjoiIn0%3D; expires=Sun, 23 Feb 2025 05:56:49 GMT; Max-Age=216000; path=/; secure; samesite=laxXSRF-TOKEN=eyJpdiI6InNOVEpiRjdld0J2MzQ3WXprN0hOa2c9PSIsInZhbHVlIjoiQnRBWU1nU1BncDZ1eGszc1dNSVV0eWxiL0FLNEZic1VrQ2puZnl6SDY3YkRBb29NdjJWZzRtYkpFZmZqbTNtU1ZORWdDY" 1 => "alphaeurekaselectnet_session=eyJpdiI6Ii9FR3pXTW40aUVzd1I2NEtxU1BjNUE9PSIsInZhbHVlIjoiaVFnTGFkYk1RS0JOV3dUV1AzSHJKQ21KM3c5UXdaUVFhY0tGLzdkVzJCZXJnQktyc1hpUnc5amtlNGZDbExMUGZTZTdPMDV4ZzRocndHRGwybDlzWVE0YVU5RU1FeHdPYmlJTWpoUkhyV1l5ME9WczNHZ0NKOHBtMDBuT1REYkwiLCJtYWMiOiI0MmM4MDE1ZTdkMWFlOWViYzdjMDZjYTcyZGE1YTdlMjE1Y2NjMjFkNDY4MDJhMjA2NmNlODA3NjBmNjRiY2QyIiwidGFnIjoiIn0%3D; path=/; secure; httponly; samesite=laxalphaeurekaselectnet_session=eyJpdiI6Ii9FR3pXTW40aUVzd1I2NEtxU1BjNUE9PSIsInZhbHVlIjoiaVFnTGFkYk1RS0JOV3dUV1AzSHJKQ21KM3c5UXdaUVFhY0tGLzdkVzJCZXJnQktyc1hpUnc5amt" ] "Set-Cookie" => array:2 [ 0 => "XSRF-TOKEN=eyJpdiI6InNOVEpiRjdld0J2MzQ3WXprN0hOa2c9PSIsInZhbHVlIjoiQnRBWU1nU1BncDZ1eGszc1dNSVV0eWxiL0FLNEZic1VrQ2puZnl6SDY3YkRBb29NdjJWZzRtYkpFZmZqbTNtU1ZORWdDYVBpbUFBaXdxY2dNbG93UGZSYk1YbDRvdXVEOHVibVNNMU9BSzJudkVXYjhkOFhQdFMvcE1ETHgzaDEiLCJtYWMiOiI0NjBhMGJkYTk1YjA5MjFiMjU1MDdjZmE3Y2ZmNDg3ZWE3MTdlZGRiYjkxM2ZiZTVjNWJkYjI2MjAzNGM3MjRkIiwidGFnIjoiIn0%3D; expires=Sun, 23-Feb-2025 05:56:49 GMT; path=/; secureXSRF-TOKEN=eyJpdiI6InNOVEpiRjdld0J2MzQ3WXprN0hOa2c9PSIsInZhbHVlIjoiQnRBWU1nU1BncDZ1eGszc1dNSVV0eWxiL0FLNEZic1VrQ2puZnl6SDY3YkRBb29NdjJWZzRtYkpFZmZqbTNtU1ZORWdDY" 1 => "alphaeurekaselectnet_session=eyJpdiI6Ii9FR3pXTW40aUVzd1I2NEtxU1BjNUE9PSIsInZhbHVlIjoiaVFnTGFkYk1RS0JOV3dUV1AzSHJKQ21KM3c5UXdaUVFhY0tGLzdkVzJCZXJnQktyc1hpUnc5amtlNGZDbExMUGZTZTdPMDV4ZzRocndHRGwybDlzWVE0YVU5RU1FeHdPYmlJTWpoUkhyV1l5ME9WczNHZ0NKOHBtMDBuT1REYkwiLCJtYWMiOiI0MmM4MDE1ZTdkMWFlOWViYzdjMDZjYTcyZGE1YTdlMjE1Y2NjMjFkNDY4MDJhMjA2NmNlODA3NjBmNjRiY2QyIiwidGFnIjoiIn0%3D; path=/; secure; httponlyalphaeurekaselectnet_session=eyJpdiI6Ii9FR3pXTW40aUVzd1I2NEtxU1BjNUE9PSIsInZhbHVlIjoiaVFnTGFkYk1RS0JOV3dUV1AzSHJKQ21KM3c5UXdaUVFhY0tGLzdkVzJCZXJnQktyc1hpUnc5amt" ] ]
        session_attributes
        0 of 0
        array:5 [ "_token" => "2Z1NloYwLVoq1oNltgDMexsHpH2lLqXnvrMjDAW8" "uc_cart_id" => "9fe05265fef67bf9efde1336b3253d34" "_previous" => array:1 [ "url" => "http://alpha.eurekaselect.com/chapter/21548" ] "_flash" => array:2 [ "old" => [] "new" => [] ] "PHPDEBUGBAR_STACK_DATA" => [] ]
        ClearShow all
        Date ↕MethodURLData
        #12025-02-20 17:56:49GET/chapter/21548112192